New analogues of the anticancer E7070: synthesis and pharmacology.
Cell cycle control in the G1 phase has attracted considerable attention in recent cancer research, because many of the important proteins involved in G1 progression or G1/S transition have been found to play a crucial role in proliferation, differentiation, transformation, and programmed cell death (apoptosis). E7070 is a novel antitumor sulfonamide, with a unique mode of action that affects G1 progression of the cell cycle. A series of compounds containing an N-[1-(3,4,5-trimethoxybenzyl)-1H-indol-5-yl]benzene sulfonamide, analogues of E7070, was synthesized and evaluated as potential antitumor agents. Cell cycle analysis with PC3 human prostate cancer cells revealed a cellular accumulation in the G1 phase.
Laconde
G
G
Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, 3 rue du Professeur Laguesse, B.P. 83, 59006 Lille, France.
Pommery
N
N
Depreux
P
P
Berthelot
P
P
Hénichart
J P
JP
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D016193:G1 Phase / Q000187:drug effects*; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D011471:Prostatic Neoplasms / Q000473:pathology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; C439829:N-(3-chloro-7-indolyl)-1,4-benzenedisulphonamide; D013449:Sulfonamides