Synthesis and antiproliferative in-vitro activity of natural flavans and related compounds.
The total synthesis of natural flavan racemates (+/-) 1, (+/-) 2 and natural flavones 3, 4 had thus been achieved. A straightforward synthetic procedure of flavans via the Pd-C catalyzed hydrogenation/hydrogenolysis of corresponding flavones was developed. Furthermore, the antiproliferative activities of racemic flavans (+/-) 1, (+/-) 2, flavones 3, 4, and five synthetic intermediates toward human SGC-7901, BEL-7402, HeLa, and HL-60 cell lines in vitro were evaluated by MTT assay, and the racemic flavans (+/-) 1 were found to have significant antiproliferative activity against all four cell lines.
Zhang
Liang
L
Department of Medicinal Chemistry, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, PR China.
Zhang
Wei-Ge
WG
Ma
En-Long
EL
Wu
Lan
L
Bao
Kai
K
Wang
Xiao-Long
XL
Wang
Yu-Ling
YL
Song
Hong-Rui
HR
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D047309:Flavones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013778:Tetrazolium Salts; D013844:Thiazoles
D000970:Antineoplastic Agents; D047309:Flavones; D013778:Tetrazolium Salts; D013844:Thiazoles; C022616:thiazolyl blue