Structure activity relationship and optimization of N-(3-(2-aminothiazol-4-yl)aryl)benzenesulfonamides as anti-cancer compounds against sensitive and resistant cells.

摘要: We recently described a new family of bioactive molecules with interesting anti-cancer activities: the N-(4-(3-aminophenyl)thiazol-2-yl)acetamides. The lead compound series (1) displays significant anti-proliferative and cytotoxic activities against panel cancer cell lines, either sensitive or resistant to standard treatments. This molecule also shows good pharmacological profile high in vivo potency towards mice xenografts, without signs toxicity on animals. In present article, we disclose structure-activity relationships this compound, which have provided clear information about replacement acetamide function substitution pattern benzenesulfonamide ring. An improved high-yielding synthetic procedure these compounds has been developed. Our drug design resulted enhancement 1, our optimized being 19. These findings are great interest further improve scaffold for development future clinical candidates.