Recently I am researching about DEPENDENT KINASE INHIBITOR; MICROTUBULE POLYMERIZATION; CDK4-SPECIFIC INHIBITORS; BIOLOGICAL EVALUATION; SELECTIVE INHIBITORS; CRYSTAL-STRUCTURE; NONPLANAR ANALOG; CYCLIN D1-CDK4; IN-VITRO; PROTEIN, Saw an article supported by the UKIERI; UGCUniversity Grants Commission, India [184-20/2013(IC), 201516-MANF-2015-17-MAH-60712]; HEIF-UK; CYP-Design Ltd; SERBDepartment of Science & Technology (India)Science Engineering Research Board (SERB), India [PDF/2017/001556]. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Sonawane, V; Siddique, MUM; Jadav, SS; Sinha, BN; Jayaprakash, V; Chaudhuri, B. The CAS is 88-68-6. Through research, I have a further understanding and discovery of 2-Aminobenzamide. Name: 2-Aminobenzamide
Inhibition of cyclin dependent kinase 4 (Cdk4) prevents cancer cells from entering the early G(0)/G(1) phase of the cell division cycle whereas inhibiting tubulin polymerization blocks cancer cells’ ability to undergo mitosis (M) late in the cell cycle. We had reported earlier that two non-planar and relatively non-toxic fascaplysin derivatives, an indole and a tryptoline, inhibit Cdk4 with IC50 values of 6.2 and 10 mu M, respectively. Serendipitously, we had also found that they inhibited tubulin polymerization. The molecules were efficacious in mouse tumor models. We have now identified Cink4T in a 59-compound quinazolinone library, designed on the basis of ligand-based virtual screening, as a compound that inhibits Cdk4 and tubulin. Its IC50 value for Cdk4 inhibition is 0.47 mu M and >50 mu M for inhibition of Cdk1, Cdk2, Cdk6, Cdk9. Cink4T inhibits tubulin polymerization with an IC50 of 0.6 mu M. Molecular modelling studies on Cink4T with Cdk4 and tubulin crystal structures lend support to these observations. Cancer cell cycle analyses confirm that Cink4T blocks cells at both G(0)/G(1) and M phases as it should if it were to inhibit both Cdk4 and tubulin polymerization. Our results show, for the very first time, that virtual screening can be used to design novel inhibitors that can potently block two crucial phases of the cell division cycle. (C) 2019 Elsevier Masson SAS. All rights reserved.
Name: 2-Aminobenzamide. Welcome to talk about 88-68-6, If you have any questions, you can contact Sonawane, V; Siddique, MUM; Jadav, SS; Sinha, BN; Jayaprakash, V; Chaudhuri, B or send Email.
Reference:
Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem