• detailed the discovery of the bacterial TopII DNA gyrase and discussed its inhibition when introduced to coumarin and quinolone class inhibitors, sparking greater interest in topoisomerase-targeting antibiotic and antitumor agents. (wikipedia.org)
  • BN80927 belongs to a novel family of camptothecin analogs, the homocamptothecins, developed on the concept of topoisomerase I (Topo I) inhibition and characterized by a stable seven-membered β-hydroxylactone ring. (aacrjournals.org)
  • In addition, BN80927 inhibits Topo II-mediated DNA relaxation in vitro but without cleavable-complex stabilization, thus indicating catalytic inhibition. (aacrjournals.org)
  • Thus, when topoisomerase I inhibition occurs with agents such as SN-38 in cell lines, the cells compensate by increasing expression of topoisomerase II and vice versa. (cancernetwork.com)
  • 3] This antagonism might be related to topoisomerase I inhibition of DNA synthesis, which is required for the cytotoxic effect of topoisomerase II-induced cleavable complexes. (cancernetwork.com)
  • The drug moieties may affect cytotoxic and cytostatic mechanisms including tubulin binding, DNA binding, or topoisomerase inhibition. (justia.com)
  • He revealed the interfacial inhibition paradigm based on molecular mechanisms of topoisomerase inhibitors, and has championed its broad relevance for molecular pharmacology and drug discovery. (cancer.gov)
  • Description: UK 383367 is a novel procollagen C-protein (PCP) inhibitor being investigated for the treatment of post-surgical dermal scarring, which potently inhibits the activity of PCP with the value of 50% inhibition concentration IC50 of 44 nM. (biolisp.org)
  • In this study, treatment of EMT6 mouse mammary tumor cells with hypoxia or the chemical stress agents brefeldin A (BFA) or okadaic acid (OA) causes the development of resistance to the topoisomerase II inhibitor etoposide. (aspetjournals.org)
  • Topoisomerase inhibitor classes have been derived from a wide variety of disparate sources, with some being natural products first extracted from plants (camptothecin, etoposide) or bacterial samples (doxorubicin, indolocarbazole), while others possess purely synthetic, and often accidental, origins (quinolone, indenoisoquinoline). (wikipedia.org)
  • Currently, topoisomerase inhibitors hold a prominent place among antibiotics and anticancer drugs in active medical use, as inhibitors like doxorubicin (anthracycline, TopII inhibitor), etoposide (TopII inhibitor), ciprofloxaxin (fluoroquinolone, TopII inhibitor), and irinotecan (camptothecin derivative, TopI inhibitor) were all included in the 2019 WHO Model List for Essential Medicines. (wikipedia.org)
  • Patients who are exposed to topoisomerase II inhibitors (eg, etoposide, doxorubicin) tend to present with frank leukemia within 1 year of the time primary therapy was initiated (see the following image). (medscape.com)
  • Certain alkylating agents like melphalan, platinum compounds, and topoisomerase II inhibitors like etoposide reported to confer a five fold increase risks for therapy related myelodysplasia or AML. (standardofcare.com)
  • Studies searching for antibiotic and anticancer agents in the mid to late 20th century have illuminated the existence of numerous unique families of both TopI and TopII inhibitors, with the 1960s alone resulting in the discovery of the camptothecin, anthracycline and epipodophyllotoxin classes. (wikipedia.org)
  • Gepotidacin (GlaxoSmithKline) is another bacterial topoisomerase II inhibitor with good in vitro activity against a wide range of drug-resistant bacteria, including methicillin-resistant Staphylococcus aureus , extended-spectrum beta-lactamase-producing Enterobacteriaceae , and N gonorrhoeae . (medscape.com)
  • Therapy-related AML (t-AML) is a subtype of AML caused by prior treatment with certain antineoplastic drugs (eg, alkylating agents, hydroxyurea , and topoisomerase II inhibitors). (msdmanuals.com)
  • Irinotecan lipid complex is in a class of antineoplastic medications called topoisomerase I inhibitors. (medlineplus.gov)
  • gov/cellminercdb) were used to investigate the following: (i) the correlations of fluoroindenoisoquinolines activity with other drugs, and (ii) genomic determinants of response in the NCI-60. (usuhs.edu)
  • To understand the determinants of response to topoisomerase inhibitors, he is studying the repair pathway centered on tyrosyl-DNA-phosphodiesterases (TDP1 and TDP2) and poly(ADP-ribose)polymerases (PARP). (cancer.gov)
  • Biological Activity: Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. (epigenetics-modulation-frontier.com)
  • 517-02, is an inhibitor of topoisomerase II (Topo II) and hepatitis C viral replication. (biolisp.org)
  • Topoisomerase inhibitors have been used as important experimental tools that have contributed to the discovery of some topoisomerases, as the quinolone nalidixic acid helped elucidate the bacterial TopII proteins it binds to. (wikipedia.org)
  • In this study we focused our attention on the behavior of four nuclear matrix proteins during the various stages of apoptosis in the HL-60 cell line exposed to the DNA topoisomerase I inhibitor, camptothecin. (nih.gov)
  • It was previously reported that proadifen (SKF-525A), a well-known cytochrome P450 monooxygenase inhibitor, not only has anti-proliferative potential in some cancer cell lines, but it is also able to inhibit BCRP and MRP1 transporter proteins ( 8 ). (spandidos-publications.com)
  • J Med Chem 2005) and extended it to macromolecular complexes involving proteins and protein-RNA complexes beyond topoisomerases (Pommier et al. (cancer.gov)
  • Some topoisomerase inhibitors prevent topoisomerases from performing DNA strand breaks while others, deemed topoisomerase poisons, associate with topoisomerase-DNA complexes and prevent the re-ligation step of the topoisomerase mechanism. (wikipedia.org)
  • These topoisomerase-DNA-inhibitor complexes are cytotoxic agents, as the un-repaired single- and double stranded DNA breaks they cause can lead to apoptosis and cell death. (wikipedia.org)
  • Preclinical data reported here show that BN80927 retains Topo I poisoning activity in cell-free assay (DNA relaxation) as well as in living cells, in which in vivo complexes of topoisomerase experiments and quantification of DNA-protein-complexes stabilization, have confirmed the higher potency of BN80927 as compared with the Topo I inhibitor SN38. (aacrjournals.org)
  • Dr. Pommier conceptualized the "interfacial inhibitors" mechanism based on his finding that DNA topoisomerase inhibitors act by trapping topoisomerase-DNA complexes (Capranico et al. (cancer.gov)
  • One of these targets is bacterial DNA, and we call these medications DNA inhibitors or nucleic acid inhibitors. (osmosis.org)
  • Now, quinolones are created to target bacterial topoisomerases, but it was soon discovered that by adding a fluorine molecule to the quinolones, they become more effective. (osmosis.org)
  • We performed a phase 2 study in children with recurrent or refractory leptomeningeal leukemia to determine the objective response rate after treatment with intrathecal (IT) topotecan. (nih.gov)
  • In a phase II trial reported in JAMA Oncology, Takahashi et al found that the addition of the ataxia telangiectasia and Rad3-related (ATR) kinase inhibitor berzosertib to topotecan did not improve progression-free survival in patients with relapsed small cell lung cancer (SCLC). (ascopost.com)
  • Contrary to other anticancer targets, topoisomerase I (TOP1) is targeted by only one chemical class of FDA-approved drugs: topotecan and irinotecan, the derivatives of the plant alkaloid, camptothecin. (usuhs.edu)
  • While the antibody to the nucleolar isoform of DNA topoisomerase II gave a fluorescent pattern that was well-maintained until the late phases of apoptosis, the other three nuclear antigens showed marked modifications in their distribution. (nih.gov)
  • Pretreatment with the proteasome inhibitor carbobenzyoxyl-leucinyl-leucinyl-leucinal inhibits stress-induced NF-κB activation and reverses BFA-induced drug resistance. (aspetjournals.org)
  • Reversible proteasome inhibitor. (medscape.com)
  • So there are many different types of topoisomerases but we'll be looking at topoisomerase II, also called DNA gyrase, and topoisomerase IV. (osmosis.org)
  • SN-38 binds to and stabilizes the topoisomerase I-DNA complex and prevents the relegation of DNA after it has been cleaved by topoisomerase I, inhibiting DNA replication. (medscape.com)
  • Based on reported resistance of Ng strains, the CDC currently prescribes a two antibiotic protocol using ceftriaxone (a β-lactam) and azithromycin (a macrolide). (elifesciences.org)
  • This gene encodes a DNA topoisomerase, an enzyme that controls and alters the topologic states of DNA during transcription. (cancerindex.org)
  • COVID-19 directly enhances its affinity with the functional host-cell receptor angiotensin-converting enzyme 2 (ACE2) and thus targets only stem-like cell types whose ACE2-dependent baseline activities regulate a myriad of homeostatic cellular processes that maintain genome, proteome, ion, energy, and immune system stability in a tissue-specific fashion. (epicos.com)
  • First total synthesis of the (±)-2-methoxy-6-heptadecynoic acid and related 2-methoxylated analogs as effective inhibitors of the leishmania topoisomerase IB enzyme. (usp.br)
  • There are plenty of processes and enzymes involved that we can target and the quinolones and fluoroquinolones inhibit an enzyme called DNA topoisomerase. (osmosis.org)
  • The indenoisoquinolines LMP400, LMP744, and LMP776 are novel noncamptothecin TOP1 inhibitors in clinical trial, which overcome the limitations of camptothecins. (usuhs.edu)
  • He discovered the indenoisoquinolines as novel Top1 inhibitors, which are in clinical development, and the mitochondrial topoisomerase gene, TOP1mt. (cancer.gov)
  • Three of his indenoisoquinoline TOP1 inhibitors are in Phase 1/2 clinical development (Thomas & Pommier, Clin Cancer Res 2019): LMP400 (Indotecan), LMP776 (Indimitecan) and LMP744. (cancer.gov)
  • 2020). Based on their promising clinical activity and their superior medicinal properties over the camptothecins, the indenoisoquinolines represent the first non-camptothecin TOP1 inhibitors for the treatment of cancers. (cancer.gov)
  • Recently, Dr. Pommier demonstrated that misincorporated ribonucleotides (the most frequent DNA alteration) trap topoisomerases, which convert them to toxic and mutagenic nicks by TOP1 (Kim et al. (cancer.gov)
  • 2018). While studying the tyrosyl-DNA-phosphodiesterase (TDP1 and TDP2) repair pathways for the excision of topoisomerases from DNA, Dr. Pommier revealed that TDP1 repairs a broad range of 3'-blocking lesions in addition to TOP1 (Murai et al. (cancer.gov)
  • Knowledge of the first topoisomerase inhibitors, and their medical potential as anticancer drugs and antibiotics, predates the discovery of the first topoisomerase (Escherichia. (wikipedia.org)
  • This fact prompted the WHO in 2016 to issue updated global treatment recommendations advising clinicians to use two antibiotics: ceftriaxone and azithromycin. (medscape.com)
  • Topoisomerase inhibitors inhibit cell growth and proliferation. (medscape.com)
  • Camptothecin-derived TopI inhibitors function by forming a ternary complex with TopI-DNA and are able to stack between the base pairs that flank the cleavage site due to their planar structure. (wikipedia.org)
  • Topoisomerase inhibitors are chemical compounds that block the action of topoisomerases, which are broken into two broad subtypes: type I topoisomerases (TopI) and type II topoisomerases (TopII). (wikipedia.org)
  • Furthermore, they imply that coadministration of agents that inhibit NF-κB may enhance the efficacy of topoisomerase II inhibitors in clinical cancer chemotherapy. (aspetjournals.org)
  • On the basis of clinical behavior and morphologic features, two predominant and clinically significant types of therapy-related myeloid neoplasms (t-MNs) have been defined, distinguished principally on the basis of the nature of cytotoxic therapy: those arising after treatment with alkylating chemotherapy (eg, cyclophosphamide, chlorambucil, cisplatin) and/or ionizing radiation therapy and those arising after therapy with topoisomerase II inhibitors. (medscape.com)
  • Risk of AML 0.25-1.0% per year beginning 2 years after the start of chemotherapy and lasts 5-7 years after its cessation. (standardofcare.com)
  • Several chemotherapy agents that include alkylating agents, topoisomerase inhibitors, and tax anew are associated with the development of acute myelogenous leukemia and myelodysplastic syndrome. (standardofcare.com)
  • Part 1 of this two-part series will discuss prevention, screening, adjuvant treatment, neoadjuvant chemotherapy, and adjuvant chemotherapy trials for ovarian cancer. (cancernetwork.com)
  • Two predominant and clinically significant types of therapy-related myeloid neoplasms (t-MN) have been defined, those arising after treatment with alkylating chemotherapy and/or radiation therapy and those arising after therapy with topoisomerase II inhibitors. (medscape.com)
  • In particular, the present invention provides methods for enhancing the effectiveness of chemotherapy by inducing differential stress resistance in normal cells and cancer cells via short-term starvation, cell growth inhibitors, or reduced caloric or glucose intake. (justia.com)
  • Another method of the invention comprises administering a cell growth inhibitor to the subject and administering to the subject a chemotherapy agent. (justia.com)
  • It showed good efficacy in a phase 2 study, with 100% efficacy for genital, oral, and rectal sites of infection in men and women. (medscape.com)
  • Results from a phase 2 trial showed high efficacy in urogenital infections (98% to 100% microbiological cure rate, depending on dose). (medscape.com)
  • Description: Potent and selective inhibitor of MMP-3 (IC50 = 5.9 nM). (biolisp.org)
  • By selecting organisms resistant to the novel inhibitors and sequencing their genomes, we identified a new therapeutic target, the class Ia ribonucleotide reductase (RNR). (elifesciences.org)
  • The structures reveal their novel mode of action as competitive ligands for the binding site of an incoming DNA substrate, and point the way to generating novel and potent inhibitors of TDP2. (rcsb.org)
  • Description: UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier [1]. (biolisp.org)
  • Tyrosyl-DNA phosphodiesterase 2 (TDP2) is a 5'-tyrosyl DNA phosphodiesterase important for the repair of DNA adducts generated by non-productive (abortive) activity of topoisomerase II (TOP2). (rcsb.org)
  • Topoisomerase IV plays a role later on, after the chromosome has been replicated, where it causes a double strand break in the DNA so the new DNA strand can be disentangled from the original. (osmosis.org)
  • As we previously described, proadifen, a P450 monooxygenase inhibitor, might also be able to inhibit some ABC transporters, including breast cancer resistance protein (BCRP). (spandidos-publications.com)
  • This invention relates to methods of inducing differential stress resistance in a subject with cancer by starving the subject for a short term, administering a cell growth inhibitor to the subject, or reducing the caloric or glucose intake by the subject. (justia.com)
  • In thisopen-label phase I study, irinotecan was administered IV at a fixeddose of 250 mg/m2 on day 1 in combination with capecitabine at a fixeddose of 1,500 mg/m2 for days 2 to 7 and epirubicin starting at a dose of40 mg/m2 and escalating by 10 mg/m2 in cohorts of three patients forthose with metastatic adenocarcinomas. (cancernetwork.com)
  • Treatment with TopI inhibitors stabilizes the intermediate cleavable complex, preventing DNA re-ligation, and inducing lethal DNA strand breaks. (wikipedia.org)
  • In cancer cells, however, these checkpoints are typically inactivated, making them selectively sensitive to TopI inhibitors. (wikipedia.org)
  • 2, 3 ), which are becoming the standards of treatment for ovarian and colon cancers, respectively, in addition to a large number of compounds undergoing clinical or preclinical evaluation. (aacrjournals.org)
  • The combination of the ATR inhibitor ceralasertib and the immune checkpoint inhibitor durvalumab has demonstrated notable survival rates and clinical benefits among patients who have advanced non-small cell lung cancer (NSCLC) with RAS mutations, according to data presented at the International. (ascopost.com)
  • Both types of topoisomerases cause double strand breaks in DNA, but at different points during mitosis . (osmosis.org)
  • Consequently, TDP2 is an interesting target for the development of small molecule inhibitors that could restore sensitivity to topoisomerase-directed therapies. (rcsb.org)
  • Nucleic Acids Res 2007) and he is a world leader for the discovery of TDP1 and TDP2 inhibitors (Marchand et al. (cancer.gov)
  • Panobinostat is a histone deacetylase (HDAc) inhibitor. (medscape.com)
  • Zoliflodacin (Entasis Therapeutics), a first-in-class spiropyrimidinetrione topoisomerase II inhibitor with activity against several pathogens, including N gonorrhoeae and C trachomatis . (medscape.com)
  • PI3K inhibitors) for moderately-to-severely symptomatic patients to eliminate COVID-19's advantage over the host immunity at the self-amplifying stage, resulting in COVID-19 eradication (see our 3rd discovery here). (epicos.com)
  • Alkylating agents and topoisomerase II inhibitors induce therapy related leukemia. (standardofcare.com)
  • Alkylating agents or radiation related and topoisomerase II inhibitor related acute myelogenous leukemia are often related to deletions of monosomies of chromosomes 5 and 7 amd a relatively long latency of 4-6 years. (standardofcare.com)
  • Most t-AMLs occur 3 to 10 years after initial therapy, with a longer latency for alkylating agents and hydroxyurea (mean latency 5 to 7 years) than for topoisomerase II inhibitors (mean latency 6 months to 3 years). (msdmanuals.com)
  • The treatment of patients with epidermal growth factor receptor (EGFR)-mutated lung cancer that progresses on EGFR-targeted tyrosine kinase inhibitors has been challenging. (ascopost.com)
  • Topoisomerase plays important roles in cellular reproduction and DNA organization, as they mediate the cleavage of single and double stranded DNA to relax supercoils, untangle catenanes, and condense chromosomes in eukaryotic cells. (wikipedia.org)
  • Topoisomerase II plays a role in condensing the chromosomes by making a double strand break in the DNA so that it can be more tightly wound, causing a supercoil. (osmosis.org)
  • Pancreatic cancer is an aggressive malignancy with less than 5% of the patients alive at 5 years and 92% of the patients dead at 2 years[ 1 , 2 ]. (wjgnet.com)
  • Twenty-two patients enrolled in the study, of whom 20 were eligible and assessable for toxicity and 16 were assessable for response. (nih.gov)
  • Of 16 patients, 6 (38%) had a complete response, 8 (50%) had stable disease, and 2 (13%) had progressive disease. (nih.gov)
  • Headache was the most common grade ≤2 neurologic event and two patients developed grade ≤2 arachnoiditis. (nih.gov)
  • With the addition of granulocytecolony-stimulating factor (G-CSF [Neupogen]) to the regimen,patients received epirubicin at clinically relevant doses after dose-escalation.Results of the topoisomerase activity will be reported with thefinal results of this phase I study. (cancernetwork.com)
  • This combination regimen in patients with upper gastrointestinalmalignancies and breast cancer will be investigated as partof phase II studies, once the dose-limiting toxicity is determined. (cancernetwork.com)
  • COVID-19's course of infection bifurcates between (i) a self-limiting stage for mildly-to-moderately symptomatic patients when the unbiased survival strategy of COVID-19 is disadvantageous against the host immunity, and (ii) a self-amplifying stage for severely-to-critically ill patients when the unbiased survival strategy of COVID-19 is advantageous over the host immunity. (epicos.com)
  • The TROP-2-directed antibody-drug conjugate datopotamab deruxtecan may significantly improve progression-free survival in patients with metastatic non-small cell lung cancer (NSCLC), especially in patients with non-squamous cell tumors, according to new findings simultaneously published by Ahn et. (ascopost.com)
  • In a Dutch single-institution phase II trial (PEMMELA) reported in The Lancet Oncology, Douma et al found that the combination of pembrolizumab and lenvatinib showed activity as second- and third-line treatments of patients with pleural mesothelioma. (ascopost.com)
  • Early-phase trials demonstrate the potential for TROP-2-directed antibody-drug conjugates to enhance the response to immune checkpoint inhibitors in patients with advanced non-small cell lung cancer (NSCLC) without actionable genomic alterations, several investigators reported at the International. (ascopost.com)
  • Tina Cascone, MD, PhD, of The University of Texas MD Anderson Cancer Center, discusses new phase III findings from the CheckMate 77T trial of patients with previously untreated resectable stage II-IIIB non-small cell lung cancer (NSCLC). (ascopost.com)
  • On October 11, the U.S. Food and Drug Administration (FDA) approved the BRAF inhibitor encorafenib (Braftovi) with the MEK inhibitor binimetinib (Mektovi) for adult patients with metastatic non-small cell lung cancer (NSCLC) and a BRAF V600E mutation, as detected by an FDA-approved test. (ascopost.com)
  • These OA features lead to decreased joint function and mobility, pain, and impaired quality of life for patients [ 2 ]. (aging-us.com)
  • Patients with low-risk MDS (eg, refractory anemia with normal cytogenetics findings) generally do not develop AML, whereas patients with high-risk MDS (eg, refractory anemia with excess blasts-type 2) frequently do. (medscape.com)
  • Two antimetabolites cause myeolosuppression that can be staved off with the administration of other agents. (freezingblue.com)
  • Two purine analog antimetabolites are very similar. (freezingblue.com)
  • The interesting activities of a subset of 4-hydoxy-2-pyridones provided the impetus for synthesis of additional chemotypes with this core ( Figure 1 ) and their evaluation for effectiveness against additional pathogenic strains including Ng and N. meningitidis (Nm ). (elifesciences.org)
  • We undertook the synthesis of structures that were condensates of heterocyclic methyl carbimidates with 2-chlorobenzenesulfonamide and 4-chloropyridine-3-sulfonamide. (springer.com)
  • It was identified that the nuclear division cycle 80, cyclin B2 and topoisomerase 2‑α may serve important roles in adrenocortical tumor development. (cancerindex.org)
  • Chromosomal changes in AML related to topoisomerase II inhibitors are rearrangement abnormalities without gain or loss of chromosomal material. (standardofcare.com)
  • It acts throughout the entire cell cycle and by direct intercalating into DNA triggers DNA breakage by topoisomerase II, causing subsequent cytocydal activity. (medscape.com)
  • Effects of Nephrolithiasis on Serum DNase (Deoxyribonuclease I and II) Activity and E3 SUMO-Protein Ligase NSE2 (NSMCE2) in Malaysian Individuals. (nih.gov)
  • Results of the topoisomerase activity will be reported with the final results of this phase I study. (cancernetwork.com)
  • Seven compounds inhibited the growth of some cancer cell lines, whereas one of the 2-quinoline derivatives displayed favorable activity against all tested cancer cells with GI 50 values of 0.92-13 μM. (springer.com)
  • T opoisomerase enzymes I and II play a critical role in preserving DNA topology by producing transient single- and double-strand DNA breaks that relieve supercoiling during replication, recombination, chromosomal decondensation, and RNA transcription. (cancernetwork.com)
  • 3,5] The additive/synergistic effect of sequential topoisomerase I and II inhibitor administration has been examined in vivo in several phase I and II human trials that explored their sequential administration. (cancernetwork.com)
  • In the phase II HERTHENA-Lung01 trial, the topoisomerase-1 HER3-targeting antibody-drug conjugate patritumab deruxtecan. (ascopost.com)
  • Since the emergence of COVID-19, several SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2) variants have emerged and spread widely. (bvsalud.org)
  • Description: Recombinant SARS-CoV-2 Spike protein, S1 subunit encompassing amino acids 16-685. (biolisp.org)
  • Acute myeloid leukemia from a patient who presented 10 months after therapy with topoisomerase II inhibitor. (medscape.com)
  • Bortezomib is the first drug approved in the group of anticancer agents known as proteasome inhibitors. (medscape.com)
  • Associated with topoisomerase II agents usually not associated with myelodysplastic syndrome and frequently associated with 11q23 cytogenetic abnormality. (standardofcare.com)
  • Six of 23 species of Apocynaceae, Simaroubaceae and Magnoliaceae showed potential as anticancer agents, as DNA damag ing agent or Topoisomerase inhibitor. (stuartxchange.org)
  • COVID-19 indirectly enhances the activation of the distal promoters of the ACE2 gene in the host cells, resulting in (i) the suppression of ACE2 expression in the host cells, (ii) the hijack of the intracellular machineries of the host cells to enable viral replication and egress, and (iii) the disruption of the homeostatic functions of the host cells. (epicos.com)
  • COVID-19 leverages the disrupted homeostatic functions of the host cells to create a favorable microenvironment that (i) activates the innate immune response to further reduce ACE2 expression to boost viral replication and egress, and (ii) suppresses the adaptive immune response to further reduce host cell death to sustain viral replication and egress. (epicos.com)
  • X-ray crystallography of two derivatives was performed. (springer.com)
  • Isolated carbimidates are easy to obtain in pure form and can be also used for 2-pyrazine, 6-chloropyrazine, and 6-methoxypyrazine derivatives. (springer.com)
  • Biological evaluation, docking studies, and in silico ADME prediction of some pyrimidine and pyridine derivatives as potential EGFR WT and EGFR T790M inhibitors. (bvsalud.org)
  • [ 2 ] Under the WHO classification system, tumors are further classified as benign, intermediate or malignant. (medscape.com)
  • Displays selectivity over a range of MMPs (IC50 values are 73, 840, 1790, 1900 and 51000 for MMP-13, MMP-9, MMP-2, MMP-14 and MMP-1 respectively). (biolisp.org)