Structure-activity relationship (SAR) of parthenin analogues with pro-apoptotic activity: Development of novel anti-cancer leads

Bhahwal Ali Shah; Rajbir Kaur; Pankaj Gupta; Ajay Kumar; Vijay Kumar Sethi; Samar Singh Andotra; Jaswant Singh; Ajit Kumar Saxena; Subhash Chandra Taneja

doi:10.1016/j.bmcl.2009.05.089

Structure-activity relationship (SAR) of parthenin analogues with pro-apoptotic activity: Development of novel anti-cancer leads

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4394-8. doi: 10.1016/j.bmcl.2009.05.089. Epub 2009 May 28.

Authors

Bhahwal Ali Shah¹, Rajbir Kaur, Pankaj Gupta, Ajay Kumar, Vijay Kumar Sethi, Samar Singh Andotra, Jaswant Singh, Ajit Kumar Saxena, Subhash Chandra Taneja

Affiliation

¹ Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu Tawi 180 001, India. [email protected]

PMID: 19501509
DOI: 10.1016/j.bmcl.2009.05.089

Abstract

Analogues of parthenin were synthesized by substitutions at different reaction centres to establish a structure-activity relationship (SAR). Some of the molecules have displayed significant cytotoxicity in human cervical carcinoma (HeLa) and human myeloid leukemia (HL-60) cells. A few of the compounds also induced apoptosis in HL-60 cells measured in terms of sub-Go/G1 DNA fraction. Also one of the lead molecules has been shown to be the inhibitor of both telomerase and topoisomerase-II.

Publication types

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

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology
Apoptosis*
Chemistry, Pharmaceutical / methods*
Drug Design
HL-60 Cells
HeLa Cells
Humans
Inhibitory Concentration 50
Models, Chemical
Neoplasms / drug therapy*
Plasmids / metabolism
Sesquiterpenes / chemical synthesis*
Sesquiterpenes / pharmacology
Structure-Activity Relationship
Telomerase / antagonists & inhibitors
Topoisomerase II Inhibitors

Substances

Antineoplastic Agents
Sesquiterpenes
Topoisomerase II Inhibitors
parthenin
Telomerase