Indole- and indolizine-glyoxylamides displaying cytotoxicity against multidrug resistant cancer cell lines.
We report herein the SAR studies of a series of indole- and indolizine-glyoxylamides that demonstrate substantial in vitro anti-proliferative activities against cancer cell lines, including multidrug resistance (MDR) phenotypes. The in vitro cytotoxic effects have been demonstrated across a wide array of tumor types of various origins (e.g., breast, colon, uterine).
James
David A
DA
Synta Pharmaceuticals, 45 Hartwell Ave, Lexington, MA 02421, USA. djames@syntapharma.com
Koya
Keizo
K
Li
Hao
H
Liang
Guiqing
G
Xia
Zhiqiang
Z
Ying
Weiwen
W
Wu
Yaming
Y
Sun
Lijun
L
D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000235:genetics / Q000378:metabolism; D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015153:Blotting, Western; D016923:Cell Death / Q000187:drug effects; D018432:Drug Resistance, Multiple; D005455:Fluorescent Antibody Technique; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D007212:Indolizines / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy*; D012333:RNA, Messenger / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
C513055:ABCB1 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000577:Amides; D000970:Antineoplastic Agents; D007211:Indoles; D007212:Indolizines; D012333:RNA, Messenger; C035094:indolizine; C030374:indole