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Kale , S.S. and Kedhe , G.S. and Meshram, S.N. and Santra, M.K. and Hamel , E. and Sanjayan, G. (2015) Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity. Bioorg Med Chem Lett., 25 (9). pp. 1982-1985.

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We describe the design, synthesis and SAR profiling of a series of novel combretastatin-nocodazole conjugates as potential anticancer agents. The thiophene ring in the nocodazole moiety was replaced by a substituted phenyl ring from the combretastatin moiety to design novel hybrid analogues. The hydroxyl group at the ortho position in compounds 2, 3 and 4 was used as the conformationally locking tool by anticipated six-membered hydrogen bonding. The bioactivity profiles of all compounds as tubulin polymerization inhibitors and as antiproliferative agents against the A-549 human lung cancer cell line were investigated Compounds 1 and 4 showed μM IC50 values in both assays.

Item Type: Article
Subjects: Infection and Immunity
Depositing User: Mr. Rameshwar Nema
Date Deposited: 27 May 2016 04:17
Last Modified: 27 May 2016 04:17
URI: http://nccs.sciencecentral.in/id/eprint/250

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