Structure-activity relationship (SAR) of parthenin analogues with pro-apoptotic activity: Development of novel anti-cancer leads.
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.
Shah
Bhahwal Ali
BA
Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu Tawi 180 001, India. bashah@iiim.res.in
Kaur
Rajbir
R
Gupta
Pankaj
P
Kumar
Ajay
A
Sethi
Vijay Kumar
VK
Andotra
Samar Singh
SS
Singh
Jaswant
J
Saxena
Ajit Kumar
AK
Taneja
Subhash Chandra
SC
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D018922:HL-60 Cells; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D009369:Neoplasms / Q000188:drug therapy*; D010957:Plasmids / Q000378:metabolism; D012717:Sesquiterpenes / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D019098:Telomerase / Q000037:antagonists & inhibitors; D059005:Topoisomerase II Inhibitors
D000970:Antineoplastic Agents; D012717:Sesquiterpenes; D059005:Topoisomerase II Inhibitors; C022097:parthenin; D019098:Telomerase