Sardaru, Monica-Cornelia; Craciun, Anda Mihaela; Al Matarneh, Cristina-Maria; Sandu, Isabela Andreea; Amarandi, Roxana Maria; Popovici, Lacramioara; Ciobanu, Catalina Ionica; Peptanariu, Dragos; Pinteala, Mariana; Mangalagiu, Ionel I.; Danac, Ramona published the artcile< Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors>, Product Details of C10H8N2, the main research area is indolizine derivative preparation colchicine tubulin polymerization inhibitor cancer; Indolizine; Phenstatin; anticancer; pyridyl; tubulin polymerisation inhibitors.
A potential microtubule destabilizing series of new indolizine derivatives was synthesized and tested for their anticancer activity against a panel of 60 human cancer cell lines. the compounds showed a broad spectrum of growth inhibitory activity against cancer cell lines representing leukemia, melanoma and cancer of lung, colon, central nervous system, ovary, kidney, breast, and prostate. Among them, compound was distinguishable by its excellent cytostatic activity, showing GI50 values in the range of 10-100 nM on 43 cell lines. The less potent compounds and in terms of GI50 values showed a high cytotoxic effect against tested colon cancer, CNS cancer, renal cancer and melanoma cell lines and only on few cell lines from other types of cancer. In vitro assaying revealed tubulin polymerization inhibition by all active compounds Mol. docking showed good complementarity of active compounds with the colchicine binding site of tubulin.
Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antitumor agents. 581-47-5 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Product Details of C10H8N2.