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  • Title: Novel hybrid nocodazole analogues as tubulin polymerization inhibitors and their antiproliferative activity.
    Author: Kale SS, Jedhe GS, Meshram SN, Santra MK, Hamel E, Sanjayan GJ.
    Journal: Bioorg Med Chem Lett; 2015 May 01; 25(9):1982-5. PubMed ID: 25817588.
    Abstract:
    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.
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