Design, synthesis and cytotoxic activity of novel spin-labeled rotenone derivatives.
Three series of novel spin-labeled rotenone derivatives were synthesized and evaluated for cytotoxicity against four tumor cell lines, A-549, DU-145, KB and KBvin. All of the derivatives showed promising in vitro cytotoxic activity against the tumor cell lines tested, with IC(50) values ranging from 0.075 to 0.738μg/mL. Remarkably, all of the compounds were more potent than paclitaxel against KBvin in vitro, and compounds 3a and 3d displayed the highest cytotoxicity against this cell line (IC(50) 0.075 and 0.092μg/mL, respectively). Based on the observed cytotoxicity, structure-activity relationships have been described.
School of Pharmacy, Lanzhou University, Lanzhou 730000, PR China; Chinese Medicine Research and Development Center, China Medical University and Hospital, Taichung, Taiwan.
Ying-Qian
YQ
Liu
Emika
E
Ohkoshi
Lin-Hai
LH
Li
Liu
L
Yang
Kuo-Hsiung
KH
Lee
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008968:Molecular Conformation; D012402:Rotenone / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013113:Spin Labels; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D013113:Spin Labels; D012402:Rotenone