Synthesis and biological evaluation of indolyl chalcones as antitumor agents

Dalip Kumar; N Maruthi Kumar; Kanako Akamatsu; Eriko Kusaka; Hiroshi Harada; Takeo Ito

doi:10.1016/j.bmcl.2010.05.016

Synthesis and biological evaluation of indolyl chalcones as antitumor agents

Bioorg Med Chem Lett. 2010 Jul 1;20(13):3916-9. doi: 10.1016/j.bmcl.2010.05.016. Epub 2010 May 13.

Authors

Dalip Kumar¹, N Maruthi Kumar, Kanako Akamatsu, Eriko Kusaka, Hiroshi Harada, Takeo Ito

Affiliation

¹ Birla Institute of Technology and Science, Pilani, India. dalipk@bits-pilani.ac.in

PMID: 20627724
DOI: 10.1016/j.bmcl.2010.05.016

Abstract

A series of indolyl chalcones were synthesized and evaluated in vitro for their anticancer activity against three human cancer cell lines. Compounds 3b-d, 3h, 3j, 3l, 3m, 4g, and 4j showed significant cytotoxicity, particularly, indolyl chalcones 3l and 3m were identified as the most potent and selective anticancer agents with IC(50) values 0.03 and 0.09 microM, against PaCa-2 cell line, respectively.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Chalcones / chemical synthesis*
Chalcones / chemistry
Chalcones / pharmacology*
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Stereoisomerism
Structure-Activity Relationship

Substances

Antineoplastic Agents
Chalcones