Nitrogen compounds drug screening assays antitumor. Medical search. Frequent questions

Heterocyclic chemistry forms an integral part of synthetic chemistry and has been a source of a number of bioactive compounds. (ijpsonline.com)
Recent advancements have focused on isolating and screening bioactive compounds and their respective medicinal properties, and we also discuss chemical property space and clinical trials, where compounds with potential pharmacological effects, such as cytotoxicity, anticancer, and antiparasitic properties, are highlighted. (bvsalud.org)
Natural bioactive compounds derived from plant species show promising therapeutic properties to combat the emerging resistance in microbial pathogens, which can be exploited as next generation anti-infective drugs. (nature.com)
Further insight into the ecology of the source species is required, including knowledge of the biosynthetic origin of the bioactive compounds, so as to distinguish innately synthesized, dietary derived or symbiotic microbial sources for sustainable culture. (mdpi.com)
Bioactive compounds from E. arvense and their pharmacological activities are shown in Table 4. (researchgate.net)

The present study aims at the production optimization, purification, and characterization of a potent broad-spectrum antimicrobial compound (AMC) produced by Aspergillus fumigatus nHF-01 (GenBank Ac. (nature.com)
Antimicrobial activity was screened in vitro against Pseudomonas sp. (ijpsonline.com)
S.A. Khanum, S. Shashikanth, S. Umesha, R. Kavitha, Synthesis and antimicrobial study of novel heterocyclic compounds from hydroxybenzophenones. (dntb.gov.ua)

Biological assays to test the cytotoxicity of the compound 1b combined with electroporation were performed to determine its potential for future medical applications in cancer treatment. (hindawi.com)
It has been proven that combining electroporation with chemotherapy potentiates the cytotoxicity of drugs when the drugs' efficacy is limited by its uptake in the cell [ 9 - 13 ]. (hindawi.com)
The aim of this study was to prepare and characterize new ruthenium NAMI-type compounds, to test their in vitro cytotoxicity and study the influence of electroporation on the cytotoxic activity of the synthesized compounds. (hindawi.com)
The search for targeted drugs for cancer treatment includes consideration of natural products, which may provide new opportunities for antitumor cytotoxicity as single agents or in combination therapy. (cancer.gov)
The current investigation aimed to demonstrate how interpretation of results from several standard cytotoxicity and proliferation assays vary in dependence on contributions from the pentose phosphate pathway (PPP). (cdc.gov)
Non-tumorigenic Beas-2B cells were treated with graded concentrations of benzo[a]pyrene (B[a]P) for 24 and 48h prior to cytotoxicity and proliferation assessment with commonly used MTT, MTS, WST1, and Alamar Blue assays. (cdc.gov)

50 years of preclinical anticancer drug screening:empirical to target-driven approaches. (jscimedcentral.com)
Anticancer drugs: Keeping one step ahead. (jscimedcentral.com)
The contribution of synthetic organic chemistry to anticancer drug development. (jscimedcentral.com)
The development of platinum-drug resistance in cancer patients, the general toxicity and severe side effects of platinum drugs however required a different approach in the research of anticancer metal complexes [ 2 ]. (hindawi.com)
J. Akhtar, A.A. Khan, Z. Ali, R. Haider, M.S. Yar, Structure-activity relationship (SAR) study and design strategies of nitrogen-containing heterocyclic moieties for their anticancer activities. (dntb.gov.ua)
The extraordinary anticancer activity of tubulysin and pretubulysin against a validated target makes them exciting leads for the development of novel drugs for multidrug-resistant cancers. (biomedcentral.com)
Given these evidences and particulars, telomerase has gotten a lot of attention as a potential target for developing new anticancer drugs. (springeropen.com)
8 Plants containing lipids with anticancer properties Species Target disease or cell line Mode of action Page (if known) (if known) Nigella sativa Sho-saiko-to, Juzen-taiho-to (extract) Ehrilch ascites carcinoma Daltons lymphoma, sarcoma-180 (clinical) Cytotoxic in vitro 96 Immunomodulator, 68 antitumor Lipids (saponifiable) include fatty acids (aliphatic carboxylic acids), fatty acid esters, phospholipids and glycolipids. (qrforex.com)

The aforementioned compounds are the chosen representatives of two larger classes of compounds bearing nitrogen-bound aromatic heterocycles developed by the Alessio and Keppler research groups, respectively [ 4 , 7 , 8 ]. (hindawi.com)
Indoles and benzimidazoles are very popular nitrogen containing heterocycles. (ijpsonline.com)
M. Gaba, C. Mohan, Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions. (dntb.gov.ua)

The active compound curcumin is believed to have a wide range of biological effects including anti-inflammatory, antioxidant, antitumor, antibacterial, and antiviral activities, which have shown a lot of potential for use in clinical medicine. (blogspot.com)

The polysaccharide of SYQ (SYQ-PA) has been reported to have antioxidant and anti-inflammatory effects, but the effect and mechanism on antitumor is still unclear. (bvsalud.org)
New anti-inflammatory agents possessing dual cyclooxygenase/lipoxygenase (COX/LOX) inhibition were discovered by PASS prediction of biological activity for 573 virtually designed chemical compounds. (way2drug.com)
Eight tested compounds exhibited anti-inflammatory activity in the carrageenan-induced paw edema. (way2drug.com)
Epidemiological and clinical studies have suggested that cancer could be prevented or significantly reduced by treatment with anti-oxidant and anti-inflammatory drugs, therefore, curcumin, a principal component of turmeric (a curry spice) showing strong anti-oxidant and anti-inflammatory activities, might be a potential candidate for the prevention and/or treatment of cancer and other chronic diseases. (blogspot.com)
Patients can usually be treated with nonsteroidal anti-inflammatory drugs (NSAIDs) alone. (msdmanuals.com)

Various biologically active synthetic compounds have five membered nitrogen containing ring as the core pharmacophore [ 5 ]. (ijpsonline.com)
Many of these intrinsically biologically active compounds produced by marine invertebrates provide useful leads for pharmaceutical, nutraceutical, and other industrial ( e.g. , anti-fouling) development. (mdpi.com)
It can predict the biological activity profile of a compound based on the analysis of structure−activity relationships for more than 250 000 biologically active substances. (way2drug.com)

Tetrazolium reduction and resazurin assays are the mainstay of routine in vitro toxicity batteries. (cdc.gov)

Heterocyclic compounds are known to exhibit a variety of biological activities because of their resemblance to a number of naturally occurring metabolites. (ijpsonline.com)
Its utility lies in the capability of heterocyclic compounds to mimic the structure of peptides and to bind reversibly to proteins [ 1 - 4 ]. (ijpsonline.com)
O. Nagaraja, Y.D. Bodke, I. Pushpavathi, S. Ravi Kumar, Synthesis, characterization and biological investigations of potentially bioactive heterocyclic compounds containing 4-hydroxy coumarin. (dntb.gov.ua)

To a synthetic chemist, it provides an opportunity to synthesize a library of compounds based on a core scaffold and to screen the derivatives for various biological activities. (ijpsonline.com)
Pharmacophore-based activity profiling screen demonstrated some biological targets that MS44-53 may modulate their biological response, and thus can be considered as potential drugs to treat different kinds of diseases, such as carcinoma, diabetes type II, bacterial infection and cardiovascular diseases. (openmedicinalchemistryjournal.com)
Several computer programs were used for prediction of the biological activity of 29 compounds concerning CYP1A2, 2C9, and 3A4 inhibition. (way2drug.com)
However, Compounds Ia - Ie lose antitumor activity dramatically suggested that the conformation of the Tuv was crucial for the tubulysin analogues to maintain the biological activity. (biomedcentral.com)

We were interested in the possibility that orange juice might interact with drugs in a manner similar to grapefruit juice (GFJ) because both juices should contain similar classes of compounds. (aspetjournals.org)

To simplify the synthesis route and find new antitumor compounds is becoming a hotspot of research recent years. (biomedcentral.com)
Some advantages, like decreasing numbers of stereocenters, increasing lipophilicity, and simplifying the synthesis, were obvious to this series of compounds. (biomedcentral.com)
Methods used for the chemical synthesis of compounds. (uams.edu)

It is reported that the compounds bearing O-H bonds behave as antioxidants but along with them, amines having N-H bond functions as the antioxidant, which have attracted much research attention because cyclic amines have always been the central structure in many currently used drugs [ 11 ]. (ijpsonline.com)
Indoles also present in naturally occurring compounds like dimethyltryptamine (hallucinogen), tryptophan (amino acid) and melatonin [ 16 ] (antioxidant as free radical scavenger). (ijpsonline.com)
1994a,b) and possible antitumor effect and antioxidant role of peroxynitrite will produce by reacting with methanol extract of Triumfetta rhomboidea superoxide (Wink et aI. (docslib.org)

assists in identifying natural products and synthetic compounds that may serve as bioprobes for chemical genetics, proteomics, target validation and potential lead compounds for clinical development. (cancer.gov)
Thorough studies have revealed pronounced differences between natural and synthetic compounds in terms of their structural and physicochemical properties, which renders the inference of targets for natural products from well-characterized drug-like compounds conceptually difficult. (way2drug.com)

The bioassay-guided separation of the extract provided ten active compounds, including three new N-methyladenine-containing diterpenoids, agelasines W-Y ( 1 - 3 ), a new bromopyrrole alkaloid, N(1)-methylisoageliferin ( 4 ), and six known ageliferin derivatives ( 5 - 10 ). (cancer.gov)

Since discovering the life-supporting drug, Penicillin, the first β -lactam antibiotic, by Sir Alexander Fleming in the 1920s, lots of progress have been developed in the antibacterial compounds production, process development and characterization of active molecules. (nature.com)

Potent cell growth inhibitory properties were shown by ligands MS47 and MS49 against human melanoma MDA-MB-435, colon cancer HCT-116 and COLO 205, and pancreatic cancer MIA PaCa-2 cell lines, as evidenced by MTT assay. (openmedicinalchemistryjournal.com)
While all of the isolated compounds showed Cbl-b inhibitory activities, ageliferins ( 4 - 10 ) were the most potent metabolites, with IC50 values that ranged from 18 to 35 μM. (cancer.gov)
Tubulysins family is a kind of natural compound with potent, antitumor activity. (biomedcentral.com)

Compound 5f is the most active compound with a modest cytotoxic activity against six human cancer cell lines: U-251 (glioma), PC-3 (prostate cancer), K-562 (leukemia), HCT-15 (colon cancer), MCF-7 (breast cancer) and SKLU-1 (lung cancer). (scirp.org)

The analysis reveals that carbon atom exactly at 3 bonds from aromatic carbon atom, nitrogen atom exactly at six bonds from planer nitrogen atom, aromatic carbon atom within 2 A 0 from the center of mass of molecule and occurrence of element hydrogen within 2 A 0 from donar atom are the key pharmacophoric features important for dual inhibition of TERT and human telomeric G-quadruplex DNA. (springeropen.com)

Drug repositioning and pharmacophore identification in the discovery of hookworm MIF inhibitors. (jscimedcentral.com)
The search for specific inhibitors is mainly performed in cell-based assays. (eurekaselect.com)
In this study, a dual-luciferase assay-based screening of 537 compounds for STAT-3 inhibitors of hepatocellular carcinoma (HCC) cells was conducted, leading to the identification of genipin. (biomedcentral.com)
The combination of QSAR, pharmacophore modeling and molecular docking may be useful for the future drug design of dual inhibitors to combat the devastating issue of resistance. (springeropen.com)

This study investigated whether BRD4 inhibition can alter the immunomodulatory and antitumor effects of radiation therapy (RT). (preprints.org)
Therefore, addition of BRD4 inhibition significantly enhanced the systemic antitumor responses of local RT. (preprints.org)

Importantly, the use of drugs (whether chemotherapy, hormonal therapy or targeted therapy) constitutes systemic therapy for cancer in that they are introduced into the blood stream and are therefore in principle able to address cancer at any anatomic location in the body. (worldsbest.rehab)

Natural products from plants and microbial sources, either as pure compounds or as standardized extracts, provide unlimited opportunities for new drugs discoveries due to unmatched chemical diversity 1 . (nature.com)
Therefore, extracts and biomolecules with promising activity are unscrupulously screened for efficacy in order to determine if these products have a potential for commercial development. (youbookinc.com)

Two ruthenium compounds, NAMI-A and KP1019 [ 4 - 6 ], are currently among the most successful candidates to enter the clinical practice. (hindawi.com)

Out of seven tested compounds, four showed the inhibitory activity. (way2drug.com)

One of the first approaches in the field of in silico pharmacology was PASS (Prediction of Activity Spectra for Substances), which applies a set of 2D descriptors to compounds that are then correlated with a set of bioactivities. (way2drug.com)

The role of the medicinal chemist in drug discovery--then and now. (jscimedcentral.com)
Researchers have been focused on developing drugs from natural sources particularly the medicinal plants for global mitigation of medical conditions while protecting the environment. (researchgate.net)
Plant kingdom represents a vast emporium of untapped medicinal potential and play a vital role for the development of new drugs. (youbookinc.com)
The medicinal value of drug plants is due to the presence of some chemical compounds in the plant tissue that produce a definite physiological action on human body. (youbookinc.com)

The data have shown that about 43% of the compounds investigated have cytotoxic effects, and around 8% have anti-trypanosome activity. (bvsalud.org)
Many different low molecular weight compounds have been studied for activity. (eurekaselect.com)
Compound IIb exhibited certain antitumor activity with the IC 50 value of 7.6 and 11.8 µM against MDA-MB-231 and MCF7 cells respectively. (biomedcentral.com)
The l -phenylalanine was chosen instead of the Tup in the tubulysin, because a previous structure-activity-relationship study showed that the Tup had little effect on the antitumor activity [ 10 , 11 ]. (biomedcentral.com)
In silico development of new molecules by using a logical structure-based drug design approach that identifies prominent hits and confirms activity for carefully selected hits. (springeropen.com)

6. The drug delivery device of claim 1, wherein the polyethyleneimine has a molecular weight between 20,000 and 50,000 Daltons. (patentsencyclopedia.com)
Compared with tubulysins, this series of compounds were relatively low molecular weight (around 550), and less stereocenters (Scheme 1 ). (biomedcentral.com)

Another reason that a phenyl group was used was because there were at most 4 positions could be utilized to introduce substituents to modify the pharmacokinetic profiles of the compounds. (biomedcentral.com)

The compounds with electron donating substituents were found to be better antioxidants with IIIa to be most effective. (ijpsonline.com)

The structures of the new compounds were elucidated from their spectroscopic and spectrometric data, including IR, HRESIMS, and NMR, and by comparison with spectroscopic data in the literature. (cancer.gov)
The structures of the resultant compounds are established using IR, 1 H and 13 C NMR spectroscopy, mass spectrometry and elemental analysis. (scirp.org)
All these compounds are new compounds, and the structures were characterized by 1 H NMR, 13 C NMR, and HRMS. (biomedcentral.com)
Peptides and nucleic acids can self-assemble to give supramolecular structures that find application in different fields, ranging from the delivery of drugs to the obtainment of materials endowed with optical properties. (cnr.it)

Billingsley ML. Druggable targets and targeted drugs: enhancing the development of new therapeutics. (jscimedcentral.com)
This mini review highlights the development of compounds that target cancer cells by taking advantage of redox or metabolic alteration in cancer cells. (degruyter.com)

Early societies learned through trial and error that many plants contained substances with significant curative properties and over the years the natural products became used in more refined ways leading ultimately to the use of pure single component "active ingredient" as drugs. (youbookinc.com)
Drug delivery devices that are orally administered, and that release active ingredients in the colon, are disclosed. (patentsencyclopedia.com)
1. Oral drug delivery devices for colonic release of active ingredients, comprising:a) an active agent capable of inactivating an antibiotic, andb) a drug delivery device comprising pectin beads, where the pectin is crosslinked with calcium ions, and reticulated with polyethyleneimine. (patentsencyclopedia.com)
2. The drug delivery device of claim 1, wherein the amount of polyethyleneimine is sufficient to allow a substantial portion of the pectin beads to pass through the gastrointestinal tract to the colon without releasing the active agent, and is also sufficient such that the pectin beads are sufficiently degraded in the colon to release an effective amount of the active agent. (patentsencyclopedia.com)
3. The drug delivery device of claim 1, wherein the active agent is an enzyme capable of inactivating beta-lactam antibiotics. (patentsencyclopedia.com)

Current chemotherapy regimens apply drug treatment in cycles, with the frequency and duration of treatments limited by toxicity. (worldsbest.rehab)
This transport creates concern for potential neurotoxicity of insoluble nanomaterials and a need for toxicity screening tests that detect nose-to-brain transport. (cdc.gov)

Another nitrogen containing heterocycle is benzimidazole, which has an imidazole ring fused to benzene. (ijpsonline.com)

In silico target prediction algorithms assess potential compound polypharmacology through the computational evaluation of the (functionally unrelated) targets modulated by a given compound, or its selectivity to species-specific targets, as they predict the probability of interaction of that compound with a panel of targets (Poroikov et al. (way2drug.com)

The Molecular Targets Program (MTP) provides the focus and infrastructure that enables CCR investigators to pursue molecularly targeted drug discovery research by promoting an interdisciplinary, collaborative, team-oriented approach to identifying and validating potential cancer-pertinent targets. (cancer.gov)

Kalkitoxin has five chiral centers, one of which is the ring carbon to which the terminal alkene is coordinated, with the remaining four occurring at tertiary carbon atoms along the aliphatic chain originating from the imine nitrogen. (wikipedia.org)

We discussed the role of different marine cyanobacteria groups in fixing nitrogen percentages on Earth and their outcomes in fish productivity by entering food webs and enhancing productivity in different agricultural and ecological fields. (bvsalud.org)

Structure (b) contains this carbonyl group, and an adjacent tertiary methylated nitrogen atom, constituting a tertiary amide group. (wikipedia.org)

Ooms F. Molecular modeling and computer aided drug design. (jscimedcentral.com)
Sharing of your experience, will support newcomers in their first steps to apply computer-aided drug discovery methods in practice, and will help us to improve our web-services. (way2drug.com)

Among the over 250 publications, there are many success stories about virtual screening, drug repurposing, revealing the hidden potential of natural products, chemical safety assessment, etc. (way2drug.com)
Also, there are increasing cases of antibiotics resistance among most causative agents of diseases in human beings, which calls for an alternative drug discovery using natural sources. (frontiersin.org)

Stereochemistry at C3 was determined by Marfey's analysis, wherein the compound was ozonized and subsequently hydrolyzed to obtain cysteic acid from the thiazoline ring and attached terminal alkene. (wikipedia.org)
Subsequently, the underlying mechanism analysis based on RNAseq and molecular assays indicated that SYQ-PA inhibited PPARÎ³ expression and regulated downstream NF-κB in macrophages. (bvsalud.org)
Subsequently, we identified 71 compounds with IC50 values that differed between the high-risk and low-risk groups. (biomedcentral.com)

Curcumin can be developed as a therapeutic drug through improvement in formulation properties or delivery systems, enabling its enhanced absorption and cellular uptake. (blogspot.com)

Compounds of interest include not only classical "drug-like" organic small molecules, but also peptides, proteins, and other bioactive chemical classes. (cancer.gov)
Based on PASS predictions for ~250000 molecules from the Open NCI database, we selected compounds with potential anti-angiogenesis action. (way2drug.com)

Several ligand-based methods apply data mining methods in order to identify unknown drug−target interactions. (way2drug.com)
Included under this heading are laboratory methods used to synthesize a variety of chemicals and drugs. (uams.edu)

However, the demands of modern medicine requires the evaluation of these plant bioactives using scientific methodologies and assays in order to gauge their potential in the management of the disease. (youbookinc.com)
They may have potential as agents for reversing multidrug resistance or for recovering the bioavailability of certain drugs. (aspetjournals.org)

Wolber G, Seidel T, Bendix F, Langer T. Molecule-pharmacophore superpositioning and pattern matching in computational drug design. (jscimedcentral.com)

In these compounds, peptide bonds were adopted as the linker to connect the Tuv and Tup parts, instead of the ethylene group in pretubulysin. (biomedcentral.com)

The chemical shifts of ring carbons adjacent to the sulfur and nitrogen heteroatoms were compared to 13C NMR data from model compounds. (wikipedia.org)
This overview provides you a guide how people use our tools, to achieve better results in their projects aimed at drug design & discovery or chemical safety assessment. (way2drug.com)
The most important chemical components of turmeric are a group of compounds called curcuminoids, which include curcumin (diferuloylmethane), demethoxycurcumin, and bisdemethoxycurcumin. (blogspot.com)

Flow cytometry assay was employed to analysis the change of tumor microenvironment and the macrophages typing. (bvsalud.org)

After two classical peptide coupling reactions and one hydrolysis reaction, compound Ia - Ie were obtained in moderate yields. (biomedcentral.com)

The effects of the two essential oils, independently and as a mixture, on five tumor cell lines, MCF‑7, HS‑1, HepG2, HeLa and A549, were investigated using the MTT assay. (spandidos-publications.com)

Mechanism-based target identification and drug discovery in cancer research. (jscimedcentral.com)
Li X, Taratula O, Taratula O, Schumann C, Minko T. LHRH-Targeted Drug Delivery Systems for Cancer Therapy. (jscimedcentral.com)
Chemotherapy (often abbreviated to chemo and sometimes CTX or CTx ) is a type of cancer treatment that uses one or more anti-cancer drugs (chemotherapeutic agents or alkylating agents) as part of a standardized chemotherapy regimen. (worldsbest.rehab)
and many others - see Advanced Drug Delivery Systems of Curcumin for Cancer Chemoprevention for a good overview. (blogspot.com)

Indoles of commercial importance include drugs such as indomethacin (antiinflammatory, an antipyretic and an analgesic) and indoxole (an antiinflammatory and antipyretic drug). (ijpsonline.com)

Because of the effect on immune cells (especially lymphocytes), chemotherapy drugs often find use in a host of diseases that result from harmful overactivity of the immune system against self (so-called autoimmunity). (worldsbest.rehab)

Organic chemistry in drug discovery. (jscimedcentral.com)

A topical collection in Marine Drugs (ISSN 1660-3397). (mdpi.com)

The long-term effectiveness of most antibiotic treatments is restricted by both pathogen drug resistance and non-target effects on the host's commensal microbial community. (nature.com)
Many of the side effects of chemotherapy can be traced to damage to normal cells that divide rapidly and are thus sensitive to anti-mitotic drugs: cells in the bone marrow, digestive tract and hair follicles. (worldsbest.rehab)
9. A method for treating or preventing adverse effects of an antibiotic to the intestinal flora, comprising administering the drug delivery device of claim 1 to a patient, either before, during, or after administration of the antibiotic. (patentsencyclopedia.com)

The antitumor activities were screened by the MTT method using MDA-MB-231and MCF7 cells. (biomedcentral.com)
Compounds IIa - IIe had moderate antitumor activities suggested that the thiazole ring in the Tuv could be replaced by the phenyl ring. (biomedcentral.com)

Western blotting assay, chromatin immunoprecipitation (ChIP) assay, molecular docking study, tube formation assay, three-dimensional top culture assay, histological examination, and immunofluorescence were utilized to evaluate the regulatory signaling pathway. (biomedcentral.com)

Chemicals and Drugs6

Phenomena and Processes1

Bioactive compounds5

Antimicrobial3

Cytotoxicity6

Anticancer8

Heterocycles3

Antiviral1

Anti-inflammatory5

Biologically active3

Vitro1

Heterocyclic3

Biological4

Classes of compounds1

Synthesis3

Antioxidant3

Synthetic2

Derivatives1

Antibacterial1

Potent3

Cytotoxic activity1

Aromatic1

Inhibitors4

Inhibition2

Systemic1

Extracts2

Clinical1

Inhibitory1

Bioactivities1

Medicinal4

Activity5

Molecular weight2

Pharmacokinetic1

Substituents1

Structures4

Development2

Active5

Toxicity2

Benzimidazole1

Species1

Targets1

Aliphatic1

Outcomes1

Atom1

Computer aided drug2

Natural2

Subsequently3

Therapeutic1

Molecules2

Methods2

Potential2

Pharmacophore1

Bonds1

Chemical3

Flow1

Reactions1

Tumor1

Cancer4

Include1

Effect1

Organic1

ISSN1

Effects3

Activities2

Study1