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

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.

• Authors: Bhahwal Ali Shah, Rajbir Kaur, Pankaj Gupta, Ajay Kumar, Vijay Kumar Sethi, Samar Singh Andotra, Jaswant Singh, Ajit Kumar Saxena, Subhash Chandra Taneja
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 19 Issue 15 Pg. 4394-8 (Aug 01 2009) ISSN: 1464-3405 [Electronic] England
• PMID: 19501509 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Sesquiterpenes
• Topoisomerase II Inhibitors
• parthenin
• Telomerase

Topics

• Antineoplastic Agents (chemical synthesis, 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, pharmacology)
• Structure-Activity Relationship
• Telomerase (antagonists & inhibitors)
• Topoisomerase II Inhibitors