Synthesis and cytotoxicity of dihydroartemisinin ethers containing cyanoarylmethyl group.
A new type of ether of dihydroartemisinin containing cyano and aryl groups was prepared and tested for cytotoxicity to A549, P388, L1210 and HT29 cells using the MTT assay. 12k and 12l were the most cytotoxic compounds. 13 lacking the peroxy group showed a 1000-fold less potency than 12l. Similarly, the inactive compound 14 indicated that the position of cyano groups was also important. Flow cytometry data showed that the compounds caused an accumulation of P388 cells in the G(1)-phase of the cell cycle.
Li
Ying
Y
Department of Synthetic Chemistry, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China. yli@mail.shnc.ac.cn
Wu
Jin Ming
JM
Shan
Feng
F
Wu
Guang Shao
GS
Ding
Jian
J
Xiao
Dong
D
Han
Jia Xian
JX
Atassi
Ghanem
G
Leonce
Stéphane
S
Caignard
Daniel Henri
DH
Renard
Pierre
P
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D019306:Artemisia / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D004987:Ethers / Q000138:chemical synthesis* / Q000494:pharmacology*; D005434:Flow Cytometry; D016193:G1 Phase / Q000187:drug effects; D019073:HT29 Cells; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy / Q000473:pathology; D007941:Leukemia P388 / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D009570:Nitriles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013778:Tetrazolium Salts; D013844:Thiazoles
D000972:Antineoplastic Agents, Phytogenic; D004987:Ethers; D009570:Nitriles; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue