Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors.

ABSTRACT: A potential microtubule destabilising series of new indolizine derivatives was synthesised and tested for their anticancer activity against a panel of 60 human cancer cell lines. Compounds 11a, 11b, 15a, and 15j showed a broad spectrum of growth inhibitory activity against cancer cell lines representing leukaemia, melanoma and cancer of lung, colon, central nervous system, ovary, kidney, breast, and prostate. Among them, compound 11a 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 15a and 15j in terms of GI₅₀ values showed a high cytotoxic effect against tested colon cancer, CNS cancer, renal cancer and melanoma cell line

SUBMITTER: Sardaru MC 

PROVIDER: S-EPMC7470029 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature