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Synthesis of substituted benzimidazolyl curcumin mimics and their anticancer activity.

Abstract：

:A novel curcumin mimic library (14a-14h and 15a-15h) possessing variously substituted benzimidazole groups was synthesized through the aldol reaction of (E)-4-(4-hydroxy-3-methoxyphenyl)but-3-en-2-one (7) or (E)-4-(3-hydroxy-4-methoxyphenyl)but-3-en-2-one (13) with diversely substituted benzimidazolyl-2-carbaldehyde (12a-12h). The MTT assay of the cancer cells MCF-7, SH-SY5Y, HEP-G2, and H460 showed that compound 14c with IC(50) of 1.0 and 1.9μM has a strong inhibitory effect on the growth of SH-SY5Y and Hep-G2 cells, respectively, and that compound 15h with IC(50) of 1.9μM has a strong inhibitory effect on the growth of MCF-7 cancer cells.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Woo HB,Eom YW,Park KS,Ham J,Ahn CM,Lee S

doi

10.1016/j.bmcl.2011.12.074

subject

Has Abstract

pub_date

2012-01-15 00:00:00

pages

933-6

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01755-0

journal_volume

22

pub_type

杂志文章

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