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Synthesis and biological evaluation of benzimidazole-oxindole conjugates as microtubule-targeting agents.

Abstract：

:A series of benzimidazole-oxindole conjugates were synthesized and evaluated for their cytotoxic activity. The cytotoxicity assay results suggest that conjugates 5c and 5p exhibit promising cytotoxicity against human breast cancer cell line (MCF-7). The Cell cycle analysis revealed that these conjugates induced cell cycle arrest at G2/M phase in MCF-7 cells. The tubulin polymerization assay results suggested that these conjugates inhibit tubulin polymerization with IC50 values 1.12 and 1.59μM respectively. Immunofluorescence analysis also suggested that these conjugates effectively inhibited the microtubule assembly in MCF-7 cells. Further, molecular docking studies indicated that these conjugates 5c and 5p interact and binds efficiently with the tubulin protein. By and large, the results demonstrated that these benzimidazole-oxindole conjugates possess cytotoxic property by inhibiting the tubulin polymerization.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Kamal A,Nagaseshadri B,Nayak VL,Srinivasulu V,Sathish M,Kapure JS,Suresh Reddy C

doi

10.1016/j.bioorg.2015.09.003

subject

Has Abstract

pub_date

2015-12-01 00:00:00

pages

72-84

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(15)30018-3

journal_volume

63

pub_type

杂志文章

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