Synthesis and structure-activity relationships of sinenxan A derivatives as multidrug resistance reversal agents.
Two types of sinenxan A derivatives with different side chains at C-5 were synthesized and evaluated for their in vitro multidrug resistant reversal activities. Several derivatives exhibited better activities than the positive control verapamil. The structure-activity relationships of these derivatives suggested that a carbonyl group at C-13 and the length of side chain at C-5 are important for the activity.
Huang
Meng
M
Department of Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, China.
Zhao
Xin
X
Zhang
Meng
M
Gu
Jun
J
Chen
Xiaoguang
X
Yin
Dali
D
D000085:Acetates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002121:Calcium Channel Blockers / Q000494:pharmacology; D004224:Diterpenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship; D020946:Taxus / Q000737:chemistry; D014407:Tumor Cells, Cultured; D014700:Verapamil / Q000494:pharmacology
D000085:Acetates; D002121:Calcium Channel Blockers; D004224:Diterpenes; C484850:sinenxan A; D014700:Verapamil