Shikonin derivatives: synthesis and inhibition of human telomerase.
We synthesized DL-shikonin, shikonin, alkanin, and their cyclo-derivatives and acyl-derivatives. These compounds have low cytotoxicity, as well as inhibitory activity against the telomerase enzyme, except cyclo-derivatives.
Lu
Qun
Q
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Science, 200031, Shanghai, PR China.
Liu
Weijun
W
Ding
Jian
J
Cai
Junchao
J
Duan
Wenhu
W
D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D009285:Naphthoquinones / Q000138:chemical synthesis* / Q000494:pharmacology; D013053:Spectrophotometry; D013329:Structure-Activity Relationship; D019098:Telomerase / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D009285:Naphthoquinones; C016101:shikonin; D019098:Telomerase