Wang, Guangcheng published the artcileDesign, synthesis, molecular modeling, and biological evaluation of pyrazole-naphthalene derivatives as potential anticancer agents on MCF-7 breast cancer cells by inhibiting tubulin polymerization, Category: isoquinoline, the main research area is pyrazole naphthalene preparation docking anticancer human tubulin polymerization inhibition; Anticancer; Naphthalene; Pyrazole; Tubulin polymerization inhibitor.
A new series of pyrazole-naphthalene derivatives I (R = 4-Me, 3-MeO, 4-EtO, etc.) have been synthesized and evaluated for their anticancer activity against human breast cancer cell lines (MCF-7). Most of newly synthesized compounds, except I (R = 3,4-(MeO)2, 4-F, 3-Cl) exhibited potent antiproliferative activity in the range of IC50 = 2.78 +/- 0.24μM – 9.13 +/- 0.47μM. Among them, compound I (R = 4-EtO) (IC50 = 2.78 +/- 0.24μM), bearing ethoxy at the 4-position of the Ph ring, was found to be the most active compound in this series of compounds, with five folds more active than the standard drug cisplatin (IC50 = 15.24 +/- 1.27μM). In addition, compound I (R = 4-EtO) and colchicine showed the same ability to inhibit tubulin polymerization with the IC50 values of 4.6μM and 6.7μM, resp. Cellular mechanism studies elucidated that compound I (R = 4-EtO) arrested the cell cycle at G2/M phase and induced apoptosis. Furthermore, mol. docking anal. revealed that compound I (R = 4-EtO) formed stable interactions in the colchicine-binding site of tubulin.
Bioorganic Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Category: isoquinoline.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem