Synthesis of some steroidal mitocans of nanomolar cytotoxicity acting by apoptosis.
Several steroids (abiraterone, prednisone, testosterone, cholesterol) and the BCL-2 inhibitor bexarotene were used as starting materials to synthesize iperazinyl-spacered rhodamine B conjugates. The conjugates were screened for their cytotoxicity in SRB assays against several human tumor cell lines and found to be active in a low μM to nM range. The conjugate derived from testosterone held an EC50 = 59 nM against MCF-7 tumor cells and acted mainly by necrosis. The prednisone conjugate, however, was less cytotoxic but acted mainly by apoptosis and held a moderate selectivity against MCF-7 tumor cells.
['Serbian|Immo|I|', 'Hoenke|Sophie|S|', 'Csuk|René|R|']
D000736:Androstenes D000970:Antineoplastic Agents D017209:Apoptosis D000077610:Bexarotene D045744:Cell Line, Tumor D049109:Cell Proliferation D002470:Cell Survival D002784:Cholesterol D004305:Dose-Response Relationship, Drug D004354:Drug Screening Assays, Antitumor D006801:Humans D008928:Mitochondria D015394:Molecular Structure D011241:Prednisone D012235:Rhodamines D013329:Structure-Activity Relationship D013739:Testosterone
Synthesis Steroids Cytotoxicity Apoptosis Prednisone Rhodamine B