Antitumor agents. Part 202: novel 2'-amino chalcones: design, synthesis and biological evaluation.
New 4',5',2,3,4-substituted 2'-amino chalcones were synthesized and evaluated for cytotoxicity against a panel of human tumor cell lines. Several compounds displayed significant cytotoxicity. The most promising lead molecule (10) also had high activity toward multi-drug resistant KB-VIN, and ovarian 1A9 cell lines. 2'-Amino chalcones demonstrated significantly increased antitumor activity compared with the corresponding chalcones, while, the epoxide derivatives generally showed greatly reduced activity.
Xia
Y
Y
Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.
Yang
Z Y
ZY
Xia
P
P
Bastow
K F
KF
Nakanishi
Y
Y
Lee
K H
KH
D000588:Amines / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D014407:Tumor Cells, Cultured
D000588:Amines; D000970:Antineoplastic Agents; D002599:Chalcone