Camptothecin: An alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA TOPOISOMERASES, TYPE I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity.Topoisomerase I Inhibitors: Compounds that inhibit the activity of DNA TOPOISOMERASE I.Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.Organosilicon Compounds: Organic compounds that contain silicon as an integral part of the molecule.Antineoplastic Agents, Phytogenic: Agents obtained from higher plants that have demonstrable cytostatic or antineoplastic activity.DNA Topoisomerases, Type I: DNA TOPOISOMERASES that catalyze ATP-independent breakage of one of the two strands of DNA, passage of the unbroken strand through the break, and rejoining of the broken strand. DNA Topoisomerases, Type I enzymes reduce the topological stress in the DNA structure by relaxing the superhelical turns and knotted rings in the DNA helix.Antineoplastic Agents: Substances that inhibit or prevent the proliferation of NEOPLASMS.Neoplasms: New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.Drug Screening Assays, Antitumor: Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals.Leukemia P388: An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene.Xenograft Model Antitumor Assays: In vivo methods of screening investigative anticancer drugs, biologic response modifiers or radiotherapies. Human tumor tissue or cells are transplanted into mice or rats followed by tumor treatment regimens. A variety of outcomes are monitored to assess antitumor effectiveness.Cell Line, Tumor: A cell line derived from cultured tumor cells.Leukemia L1210Antibiotics, Antineoplastic: Chemical substances, produced by microorganisms, inhibiting or preventing the proliferation of neoplasms.Tumor Cells, Cultured: Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.Sarcoma 180Mice, Nude: Mutant mice homozygous for the recessive gene "nude" which fail to develop a thymus. They are useful in tumor studies and studies on immune responses.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.DNA Damage: Injuries to DNA that introduce deviations from its normal, intact structure and which may, if left unrepaired, result in a MUTATION or a block of DNA REPLICATION. These deviations may be caused by physical or chemical agents and occur by natural or unnatural, introduced circumstances. They include the introduction of illegitimate bases during replication or by deamination or other modification of bases; the loss of a base from the DNA backbone leaving an abasic site; single-strand breaks; double strand breaks; and intrastrand (PYRIMIDINE DIMERS) or interstrand crosslinking. Damage can often be repaired (DNA REPAIR). If the damage is extensive, it can induce APOPTOSIS.Apoptosis: One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.Molecular Structure: The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.Cell Survival: The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability.Topoisomerase II Inhibitors: Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Topoisomerase Inhibitors: Compounds that inhibit the activity of DNA TOPOISOMERASES.Inhibitory Concentration 50: The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.Neoplasm Transplantation: Experimental transplantation of neoplasms in laboratory animals for research purposes.Neoplasms, Experimental: Experimentally induced new abnormal growth of TISSUES in animals to provide models for studying human neoplasms.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Intercalating Agents: Agents that are capable of inserting themselves between the successive bases in DNA, thus kinking, uncoiling or otherwise deforming it and therefore preventing its proper functioning. They are used in the study of DNA.Camptotheca: A plant genus of the family NYSSACEAE (sometimes classified in the CORNACEAE family). It is a source of CAMPTOTHECIN.DNA Topoisomerases, Type II: DNA TOPOISOMERASES that catalyze ATP-dependent breakage of both strands of DNA, passage of the unbroken strands through the breaks, and rejoining of the broken strands. These enzymes bring about relaxation of the supercoiled DNA and resolution of a knotted circular DNA duplex.Teniposide: A semisynthetic derivative of PODOPHYLLOTOXIN that exhibits antitumor activity. Teniposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. This complex induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Accumulated breaks in DNA prevent cells from entering into the mitotic phase of the cell cycle, and lead to cell death. Teniposide acts primarily in the G2 and S phases of the cycle.Melanoma, Experimental: Experimentally induced tumor that produces MELANIN in animals to provide a model for studying human MELANOMA.DNA: A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).Drug Synergism: The action of a drug in promoting or enhancing the effectiveness of another drug.Doxorubicin: Antineoplastic antibiotic obtained from Streptomyces peucetius. It is a hydroxy derivative of DAUNORUBICIN.KB Cells: This line KB is now known to be a subline of the ubiquitous KERATIN-forming tumor cell line HeLa. It was originally thought to be derived from an epidermal carcinoma of the mouth, but was subsequently found, based on isoenzyme analysis, HeLa marker chromosomes, and DNA fingerprinting, to have been established via contamination by HELA CELLS. The cells are positive for keratin by immunoperoxidase staining. KB cells have been reported to contain human papillomavirus18 (HPV-18) sequences.Ellipticines: Pyrido-CARBAZOLES originally discovered in the bark of OCHROSIA ELLIPTICA. They inhibit DNA and RNA synthesis and have immunosuppressive properties.Cell Division: The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.Cell Cycle: The complex series of phenomena, occurring between the end of one CELL DIVISION and the end of the next, by which cellular material is duplicated and then divided between two daughter cells. The cell cycle includes INTERPHASE, which includes G0 PHASE; G1 PHASE; S PHASE; and G2 PHASE, and CELL DIVISION PHASE.Streptonigrin: Complex cytotoxic antibiotic obtained from Streptomyces flocculus or S. rufochronmogenus. It is used in advanced carcinoma and causes leukopenia.Drug Resistance, Neoplasm: Resistance or diminished response of a neoplasm to an antineoplastic agent in humans, animals, or cell or tissue cultures.Mice, Inbred BALB CCell Proliferation: All of the processes involved in increasing CELL NUMBER including CELL DIVISION.Drug Design: The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.Drug Resistance: Diminished or failed response of an organism, disease or tissue to the intended effectiveness of a chemical or drug. It should be differentiated from DRUG TOLERANCE which is the progressive diminution of the susceptibility of a human or animal to the effects of a drug, as a result of continued administration.Etoposide: A semisynthetic derivative of PODOPHYLLOTOXIN that exhibits antitumor activity. Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. This complex induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Accumulated breaks in DNA prevent entry into the mitotic phase of cell division, and lead to cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle.Triaziquone: Alkylating antineoplastic agent used mainly for ovarian tumors. It is toxic to skin, gastrointestinal tract, bone marrow and kidneys.Kinetics: The rate dynamics in chemical or physical systems.Lactones: Cyclic esters of hydroxy carboxylic acids, containing a 1-oxacycloalkan-2-one structure. Large cyclic lactones of over a dozen atoms are MACROLIDES.Cisplatin: An inorganic and water-soluble platinum complex. After undergoing hydrolysis, it reacts with DNA to produce both intra and interstrand crosslinks. These crosslinks appear to impair replication and transcription of DNA. The cytotoxicity of cisplatin correlates with cellular arrest in the G2 phase of the cell cycle.Colonic Neoplasms: Tumors or cancer of the COLON.AcridinesMaytansine: An ansa macrolide isolated from the MAYTENUS genus of East African shrubs.Drug Evaluation, Preclinical: Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.Transplantation, Heterologous: Transplantation between animals of different species.Pyrones: Keto-pyrans.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Alkaloids: Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)Naphthacenes: Polyacenes with four ortho-fused benzene rings in a straight linear arrangement. This group is best known for the subclass called TETRACYCLINES.Leukemia L5178: An experimental lymphocytic leukemia of mice.DioxolesStereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Lung Neoplasms: Tumors or cancer of the LUNG.Acridones: Compounds based on acridone, which have three linear rings, with the center ring containing a ring nitrogen and a keto oxygen opposite to each other. Many of them are naturally occurring alkaloids.Indoles: Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.Aminoacridines: Acridines which are substituted in any position by one or more amino groups or substituted amino groups.Aziridines: Saturated azacyclopropane compounds. They include compounds with substitutions on CARBON or NITROGEN atoms.Prodrugs: A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.DNA, Neoplasm: DNA present in neoplastic tissue.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Biotransformation: The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.Rubiaceae: The Madder plant family of the order Rubiales, subclass Asteridae, class Magnoliopsida includes important medicinal plants that provide QUININE; IPECAC; and COFFEE. They have opposite leaves and interpetiolar stipules.Enediynes: Compounds with triple bonds to each side of a double bond. Many of these are CYTOTOXINS and are researched for use as CYTOTOXIC ANTIBIOTICS.Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.Chromomycins: A complex of several closely related glycosidic antibiotics from Streptomyces griseus. The major component, CHROMOMYCIN A3, is used as a fluorescent stain of DNA where it attaches and inhibits RNA synthesis. It is also used as an antineoplastic agent, especially for solid tumors.HT29 Cells: Human colonic ADENOCARCINOMA cells that are able to express differentiation features characteristic of mature intestinal cells such as the GOBLET CELLS.Indenes: A family of fused-ring hydrocarbons isolated from coal tar that act as intermediates in various chemical reactions and are used in the production of coumarone-indene resins.Antineoplastic Agents, Alkylating: A class of drugs that differs from other alkylating agents used clinically in that they are monofunctional and thus unable to cross-link cellular macromolecules. Among their common properties are a requirement for metabolic activation to intermediates with antitumor efficacy and the presence in their chemical structures of N-methyl groups, that after metabolism, can covalently modify cellular DNA. The precise mechanisms by which each of these drugs acts to kill tumor cells are not completely understood. (From AMA, Drug Evaluations Annual, 1994, p2026)Organic Chemistry Phenomena: The conformation, properties, reaction processes, and the properties of the reactions of carbon compounds.Furans: Compounds with a 5-membered ring of four carbons and an oxygen. They are aromatic heterocycles. The reduced form is tetrahydrofuran.Menogaril: A semisynthetic anthracycline with the amino sugar on the D ring. It displays broad-spectrum antineoplastic activity against a variety of tumors.Mice, Inbred C57BLAphidicolin: An antiviral antibiotic produced by Cephalosporium aphidicola and other fungi. It inhibits the growth of eukaryotic cells and certain animal viruses by selectively inhibiting the cellular replication of DNA polymerase II or the viral-induced DNA polymerases. The drug may be useful for controlling excessive cell proliferation in patients with cancer, psoriasis or other dermatitis with little or no adverse effect upon non-multiplying cells.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Melanoma: A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)Paclitaxel: A cyclodecane isolated from the bark of the Pacific yew tree, TAXUS BREVIFOLIA. It stabilizes MICROTUBULES in their polymerized form leading to cell death.Acronine: A pyrano-acridone alkaloid found in RUTACEAE plants.
"Plant antitumor agents. I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from ... Since the discovery of CPT many analogues have been synthesized. Below is a schematic view of the CPT analogues that have been ... "Curran Synthesis of Camptothecin". "Comins Synthesis of Camptothecin". "Rapaport Synthesis of Camptothecin". Takimoto CH, Calvo ... M. K. Chung; S. S. Han; J. C. Kim (2006). "Evaluation of the toxic potentials of a new camptothecin anticancer agent CKD-602 on ...
"Plant antitumor agents. VI. The isolation and structure of taxol, a novel antileukemic and antitumor agent from Taxus ... Wall, ME; Wani, MC (1995). "Camptothecin and taxol: Discovery to clinic-thirteenth Bruce F. Cain Memorial Award Lecture". ... Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 512. ISBN 9783527607495. ... Abraxis BioScience developed Abraxane, in which paclitaxel is bonded to albumin as an alternative delivery agent to the often ...
One example of a successful use of this strategy is the screening for antitumour agents by the National Cancer Institute, ... Gertrude Elion, working mostly with a group of fewer than 50 people on purine analogues, contributed to the discovery of the ... Camptothecin · Topotecan · Irinotecan · Rubitecan · Belotecan); 2. Podophyllum (Etoposide · Teniposide); 3a. Anthracyclines ( ... Artemisinin, an antimalarial agent from sweet wormtree Artemisia annua, used in Chinese medicine since 200BC is one drug used ...
Siddik ZH (2005). Mechanisms of Action of Cancer Chemotherapeutic Agents: DNA-Interactive Alkylating Agents and Antitumour ... Fluorouracil is a nucleobase analogue that is metabolised in cells to form at least two active products; 5-fluourouridine ... Two topoisomerase I inhibitors, irinotecan and topotecan, are semi-synthetically derived from camptothecin, which is obtained ... Alkylating agents will work at any point in the cell cycle and thus are known as cell cycle-independent drugs. For this reason ...
Agents Chemother. 40 (9): 2087-2093. PMC 163478 . PMID 8878586. Meruelo D, Lavie G, Lavie D (1988). "Therapeutic agents with ... Li S, Zhang Z, Cain A, Wang B, Long M, Taylor J (2005). "Antifungal activity of camptothecin, trifolin, and hyperoside isolated ... Hyperforin has been shown to exhibit anti-inflammatory, anti-tumor, antibiotic and anti-depressant functions (PMID 17696442, ... their analogues (e.g. carotenoids, choline, nicotinamide, nicotinic acid) Miscellaneous others (e.g. pectin, β-sitosterol, ...
Siddik ZH (2005). Mechanisms of Action of Cancer Chemotherapeutic Agents: DNA-Interactive Alkylating Agents and Antitumour ... Subtypes of the anti-metabolites are the anti-folates, fluoropyrimidines, deoxynucleoside analogues and thiopurines.[32][37] ... Two topoisomerase I inhibitors, irinotecan and topotecan, are semi-synthetically derived from camptothecin, which is obtained ... Available agents[edit]. Main article: List of antineoplastic agents. There is an extensive list of antineoplastic agents. ...
Disubstituted analogues as potential photodynamic agents (a siloxane NC substituted with two methoxyethyleneglycol ligands) are ... Diamino platinum porphyrins show high anti-tumour activity, demonstrating the combined effect of the cytotoxicity of the ... "Single-agent phototherapy system diagnoses and kills cancer cells , KurzweilAI". www.kurzweilai.net. November 2, 2015. ... HpD, under the brand name Photofrin, was the first PDT agent approved for clinical use in 1993 to treat a form of bladder ...
The current status of camptothecin analogues as antitumor agents. J Natl Cancer Inst. 1993;85:271-291. ... One antiemetic agent commonly used with antineoplastic agents is prochlorperazine, which can cause akathisia. ... The antiemetic agents should be started on the same day, at least 30 minutes before the infusion of CAMPTOSAR. If nausea and ... Potmesil M. Camptothecins: From bench research to hospital wards. Cancer Res. 1994;54:1431-1439. ...
IC50 Value: 50 nM(in MDA-MB-231 cell line) Target: topoisomerase Camptothecin (CPT) has recently been undergoing phase I ... In 3D fluorescence spectra, Camptothecin presented 3 fluorescence peaks wi... ... Camptothecin (CPT) is a potent DNA enzyme topoisomerase I (topo I) inhibitor with an IC50 and IC70 of 50 nM and 0.225 μM for ... Camptothecin (CPT) The report - posted in Immunology Products: Biological Activity of Campathecin ...
The camptothecin analog CPT-11 has recently been approved for the treatment of 5-fluorouracil (5-FU)-resistant colorectal ... The current status of camptothecin analogues as antitumor agents. J Natl Cancer Inst 1993; 85 (4): 271-291.PubMedCrossRefGoogle ... In vitro antitumor activity of 9-nitrocamptothecin as a single agent and in combination with other antitumor drugs. Ann N YAcad ... Kawato Y, Furuta T, Aonurna M, Yasuoka M, Yokokura T, Matsumoto K. Antitumor activity of a camptothecin derivative, CPT-11, ...
1993 The current status of camptothecin analogues as antitumor agents. J Natl Cancer Inst 85:271-291.Google Scholar ... 1991 Antagonism between camptothecin and topoisomerase II-directed chemotherapeutic agents in a human leukemia cell line. ... 1973 Effects of camptothecin on the breakage and repair of DNA during the cell cycle. Cancer Res 33:2834-2846.Google Scholar ... 1998 Camptothecins: a review of their development and schedules of administration. Eur J Cancer 34:1500-1508.Google Scholar ...
Although FL118 is a camptothecin analogue, its antitumor potency is much superior to other FDA-approved camptothecin analogues ... Anticancer agent FL118 was recently identified in screening of small-molecule inhibitors of human survivin expression. ... D, a proposed model of antitumor mechanisms for FL118 in colon cancer cells (see text). ... irinotecan and topotecan). The mechanism of action (MOA) underlying the antitumor effects of FL118 remains to be fully ...
Slichenmyer WJ, Rowinsky EK, Donehower RC, et al: The current status of camptothecin analogues as antitumor agents. J Natl ... Instead, the inability to administer clinically relevant single-agent doses of both agents in combination might result from ... water-insoluble camptothecin derivatives, which might portend vastly different spectra of antitumor activity, toxicity, and ... sodium camptothecin). After recognition that camptothecin was active by virtue of a novel mechanism of action (topoisomerase I ...
The current status of camptothecin analogues as antitumor agents. J. Natl. Cancer Inst., 85: 271-291, 1993. ... The cell lines demonstrated much less resistance to camptothecin and to several camptothecin analogues. Reduced accumulation ... Thus, we can add the camptothecins to the growing list of agents whose activity can be mediated by drug efflux pumps. ... Yang C. J., Horton J. K., Cowan K. H., Schneider E. Cross-resistance to camptothecin analogues in a mitoxantrone-resistant ...
Although FL118 is a camptothecin analogue, its antitumor potency is much superior to other FDA-approved camptothecin analogues ... Plant-derived agents have great potential in preventing the onset of the carcinogenic process and enhancing the efficacy of ... Anticancer agent FL118 was recently identified in screening of small-molecule inhibitors of human survivin expression. ... Using human HCC SK-Hep-1 cells depleted of mtDNA (Rho), changes in gene expression in response to antitumor drugs previously ...
status of camptothecin analogues as antitumor agents. J Natl Cancer. Inst 85:271-291, 1993. ... 9. Wall ME, Wani MC, Gook CE, et al: Plant antitumor agents: 1. The. isolation and structure of camptothecin, a novel alkaloid ... Preclinical Studies of Camptothecins. Many anticancer agents are known to act as topoisomerase inhibitors.. Hsiang et al, while ... SN-38, a metabolite of camptothecin derivative CPT-11, in the. antitumor effect of CPT-11. Cancer Res 51:4187-4191, 1991. ...
Topotecan is a camptothecin analogue which in the presence of DNA replication generate double strand DNA breaks and ... It showed antitumor activity in tumor xenograft models, which correlate with the HIF-1 expression [57] ... One of the earlier agents used for HIF-1 protein translation is topotecan, a second line chemotherapy for lung cancer or ... Digoxin inhibits HIF-1 translation using mTOR-independent mechanism and also exhibits antitumor activity [55]. PX-478 is ...
Topotecan, a water-soluble semisynthetic analogue of the alkaloid antitumor agent camptothecin, is a topoisomerase I inhibitor ... Sim GA Plant antitumor agents.: I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor ... The antitumor activity of single-agent etoposide in patients with relapsed ovarian cancer has been investigated in several ... Hsiang YH, Liu LF, Wall ME, et al DNA topoisomerase I-mediated DNA cleavage and cytotoxicity of camptothecin analogues. Cancer ...
... a camptothecin analogue, was based on observations that PARP inhibitors can potentiate camptothecin cytotoxicity (23, 24, 25) ... 1⇓ for structures). TM, a methylating agent showing promise in the treatment of melanomas and gliomas (22) , was selected ... TP has shown a wide range of antitumor activity against adult and pediatric malignancies (26 , 27) . ... Camptothecin resistance involving steps subsequent to the formation of protein-linked DNA breaks in human camptothecin- ...
Water-soluble derivatives of camptothecin have the formulae: ##STR1## wherein R is selected from the group consisting of R=CO ... interest in camptothecin as an anti-tumor agent has remained very high. Careful evaluation of these agents in animal models ... Camptothecin analogues US5391745A (en) * 1992-07-23. 1995-02-21. Sloan-Kettering Institute For Cancer Research. Methods of ... Water-soluble camptothecin derivatives, process for their preparation and their use as antitumor agents ...
A disadvantage which seriously limits application of camptothecins in antitumor chemotherapy is the hydrolysis of these ... Fluorescence spectra of these analogues change in presence of liposomes: the fluorescence intensity increases and besides green ... The process of hydrolysis is inhibited when the molecules of camptothecin are bound to cell membranes. So it is desirable that ... Membranes affinity of 10-hydroxycamptothecin and SN-38, anticancer agents, determined by fluorescence spectra analysis Author(s ...
... podophyllotoxin analogues (etoposide and teniposide), and topotecan (camptothecin analog) are based on natural plants. ... Many antitumor drugs currently in clinical use, such as paclitaxel, vinca alkaloids (vinblastine and vincristine), ... According to a report, 83% of new chemical entities identified as anticancer agents from 1981 to 2014 were derived from natural ...
The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with ... Preparation of chlorinated paclitaxel analogues and use thereof as antitumor agents. US5886026 *. Jun 7, 1995. Mar 23, 1999. ... Polymer-bound camptothecin derivatives. US5795909 *. May 22, 1996. Aug 18, 1998. Neuromedica, Inc.. DHA-pharmaceutical agent ... Preparation of brominated paclitaxel analogues and their use as effective antitumor agents. ...
"Plant antitumor agents. I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from ... Since the discovery of CPT many analogues have been synthesized. Below is a schematic view of the CPT analogues that have been ... "Curran Synthesis of Camptothecin". "Comins Synthesis of Camptothecin". "Rapaport Synthesis of Camptothecin". Takimoto CH, Calvo ... M. K. Chung; S. S. Han; J. C. Kim (2006). "Evaluation of the toxic potentials of a new camptothecin anticancer agent CKD-602 on ...
... displayed antitumor activity against at least one of five cancer cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5- ... to determine their antitumor and antimicrobial activities. Twenty-eight fungal endophytes were isolated from agarwood by strict ... An endophytic fungus from Camptotheca acuminata that produces camptothecin and analogues.. *Souvik Kusari, Sebastian Zuehlke, ... Potential use of cucumber (Cucumis sativus L.) endophytic fungi as seed treatment agents against root-knot nematode Meloidogyne ...
10 followed this.The current status of camptothecin analogues as antitumor agents. The thyroid carcinoma tends to cetirizine ... IMAGING-AGENTS h. USA 1992, 89, 8938в8942. The toxicity evaluation of drug-delivery dog must take into account the toxicity of ... Other infectious agents may be associated cetirrizine other ocular lym- phomatous processes. Htm. Additionally, the supe- rior ... 0gm IV QD Г- 21в28 days 50в75mgkgday divided Q12hr 100mg PO BID Preferred first line agent Pediatric dose (max 2gday) Preferred ...
"Discovery of a potent anti-tumor agent through regioselective mono-N-acylation of 7H-pyrrolo[3,2-f]quinazoline-1,3-diamine" ... "Effect of E-ring modifications in camptothecin on topoisomerase I inhibition" Journal of Organic Chemistry November 11 2005 ... "Design, synthesis, and biological evaluation of conformationally constrained analogues of naphthol AS-E as inhibitors of CREB- ... "Structure-activity relationship studies of naphthol AS-E and its derivatives as anticancer agents by inhibiting CREB-mediated ...
1987). Plant antitumour agents, 25: total synthesis and antileukemic activity of ring Asubstituted camptothecin analogues, ... 1986). Plant antitumour agents, 23: synthesis and antileukemic activity of camptothecin analogues. ... 1971). Plant antitumour agents, 6: the isolation and structure of taxol, a novel antileukemic and antitumour agent from Taxus ... total synthesis and antitumour activity of 20(S)-camptothecin and 20(R)-camptothecin. ...
In an effort to discover potent camptothecin-derived antitumor agents, novel camptothecin analogues with sulfonylpiperazinyl ... abstract = "In an effort to discover potent camptothecin-derived antitumor agents, novel camptothecin analogues with ... N2 - In an effort to discover potent camptothecin-derived antitumor agents, novel camptothecin analogues with ... AB - In an effort to discover potent camptothecin-derived antitumor agents, novel camptothecin analogues with ...
The plant alkaloid camptothecin (CPT) has demonstrated the ability to inhibit replication of the equine anemia virus (E1AV) and ... Plant antitumor agents. I. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from ... Synthesis of water-soluble (aminoalkyl) camptothecin analogues: Inhibition of topoisomerase I and antitumor activity. J Med ... Biochemistry of camptothecin. In Potmesil M, Pinedo H, eds. Camptothecins: New Anticancer Agents. Boca Raton, CRC Press, 9-19; ...
... and agents that target topoisomerase I (e.g., camptothecin and isirinotecan (CPT-11), etc.); 2) covalent DNA-binding agents ( ... noncovalent DNA-binding agents (antitumor antibiotics), including nucleic acid inhibitors (e.g., dactinomycin (actinomycin D), ... anthracycline analogues, such as mitoxantrone, etc.), bleomycins (BLENOXANE), etc., and plicamycin (mithramycin), etc.; 4) ... Anticancer agents suitable for use with the present invention include, but are not limited to, agents that induce apoptosis, ...
20. The method if claim 14, wherein the anti-tumor drug is an antimitotic drug, an antimetabolite drug, an alkyling agent, a ... 12. The combination of claim 9, wherein the anti-tumor drug is 5-fluorouracil, cytarabine, gemcitabine, a purine analogue, ... camptothecin, mitoxantrone, tamoxifen, or sunitinib in combination with antcin or a salt or ester derivative or a composition ... 9. The combination of claim 1, wherein the anti-tumor drug is an antimitotic drug, an antimetabolite drug, an alkyling agent, a ...
  • Whereas camptothecins are active against a wide range of solid tumors, resistance can be a significant hindrance to therapy. (aacrjournals.org)
  • Radiolableled amino acid-based agents are useful in PET brain tumor imaging because F-18 fluoro-deoxyglucose (F-18 FDG), commonly used in PET tumor imaging, is relatively insensitive for detecting tumors in the brain due the high levels of glycolytic metabolism in the normal cortex and to a lesser extent in white matter. (cancer.gov)
  • Camptothecin (CPT) has recently attracted increasing attention as a promising anticancer agent for a variety of tumors. (biomedcentral.com)
  • Giovanella BC, Hinz HR, Kozielski AJ, Stehlin JS, Silber R, Potmesil M. Complete growth inhibition of human cancer xenografts in nude mice by treatment with 20(S)-camptothecin. (springer.com)
  • Complete Growth Inhibition of Human Cancer Xenografts in Nude Mice by Treatment with 20-(S)-Camptothecin", Cancer Research, 51, 3052-3055 (Jun. (freepatentsonline.com)
  • Inhibition of carboxylesterases by benzil (diphenylethane-1,2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and the flexibility of the dione moiety. (uab.edu)
  • The gamma-aminobutyric acid (GABA) analogue baclofen appears to activate the inhibitory GABA(B) receptor, a G protein-coupled receptor, which may result in hyperpolarization of the neuronal cell membrane and inhibition of neurotransmitter release. (newyorkoncology.com)
  • With the help of George Hitchings and Gertrude Elion , two pharmaceutical chemists who were working at the Burroughs Wellcome Company in Tuckahoe, many purine analogues were tested, culminating in the discovery of 6-mercaptopurine (6-MP), which was subsequently shown to be a highly active antileukemic drug. (chemeurope.com)
  • Intracellular degradation of HeLa and adenovirus type 2 DNA induced by camptothecin. (springer.com)
  • Reflecting the increased amino acid transport capacity of tumor cells, F-18 fluroethyltyrosine (F-18 FET) is actively taken up in tumor cells via amino acid transport system L, but is neither incorporated into proteins nor readily degraded, resulting in high intracellular concentrations of this imaging agent. (cancer.gov)
  • With cell uptake much higher in tumor cells compared to normal cells, the F18 moiety of fluorodeoxygalactose F-18 can be visualized upon PET imaging and this agent can be used as a tracer for the evaluation of galactose tumor uptake and metabolism. (cancer.gov)
  • In 3D fluorescence spectra, Camptothecin presented 3 fluorescence peaks with excitation wavelengths lambdaex of 215, 255 and 365 nm, separately. (protocol-online.org)
  • Fluorescence spectra of these analogues change in presence of liposomes: the fluorescence intensity increases and besides green band the blue band appears. (spie.org)
  • Accordingly, we have examined ATP-dependent transport of those CPT analogues by using plasma membrane vesicles prepared from ABCG2-overexpressing cells. (eurekaselect.com)