A focused compound library of novel N-(7-indolyl)benzenesulfonamides for the discovery of potent cell cycle inhibitors.
A series of compounds containing an N-(7-indolyl)benzenesulfonamide pharmacophore was synthesized and evaluated as a potential antitumor agent. Cell cycle analysis with P388 murine leukemia cells revealed that there were two different classes of potent cell cycle inhibitors; one disrupted mitosis and the other caused G1 accumulation. Herein described is the SAR summary of the substituent patterns on this pharmacophore template.
Owa
T
T
Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan. t-owa@hhc.eisai.co.jp
Okauchi
T
T
Yoshimatsu
K
K
Sugi
N H
NH
Ozawa
Y
Y
Nagasu
T
T
Koyanagi
N
N
Okabe
T
T
Kitoh
K
K
Yoshino
H
H
D002453:Cell Cycle / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D013449:Sulfonamides / Q000737:chemistry* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D013449:Sulfonamides