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Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents.

Abstract：

:A series of novel cinnamic acyl sulfonamide derivatives (9a-16e) have been designed and synthesized and their biological activities were also evaluated as potential tubulin polymerization inhibitors. Among all the compounds, 10c showed the most potent growth inhibitory activity against B16-F10 cancer cell line in vitro, with an IC(50) value of 0.8μg/mL. Docking simulation was performed to insert compound 10c into the crystal structure of tubulin at colchicine binding site to determine the probable binding model. Based on the preliminary results, compound 10c with potent inhibitory activity in tumor growth may be a potential anticancer agent.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Luo Y,Qiu KM,Lu X,Liu K,Fu J,Zhu HL

doi

10.1016/j.bmc.2011.06.088

subject

Has Abstract

pub_date

2011-08-15 00:00:00

pages

4730-8

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(11)00538-4

journal_volume

19

pub_type

杂志文章

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