Synthesis and biological evaluation of DNA targeting flexible side-chain substituted beta-carboline derivatives.
A series of 3-substituted-beta-carboline derivatives was synthesized from L-tryptophan. The intercalating binding mode of these compounds with DNA, the effects of the flexible alkylamine side chain on the intercalating ability and their antitumor activity were studied, which agreed well with the molecular modeling results.
National Research Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing, People's Republic of China.
S
S
Xiao
W
W
Lin
C
C
Wang
M
M
Yang
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D004247:DNA / Q000378:metabolism*; D006801:Humans; D007364:Intercalating Agents / Q000138:chemical synthesis*; D008958:Models, Molecular; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D002243:Carbolines; D007364:Intercalating Agents; D004247:DNA