A series of pyrimidine hydroxamic acids with a sulfide substituent at the second position and a sulfonamide substituent at the fourth position have been synthesized and evaluated for their activity against human myeloma cell line RPMI 8226. Several compounds exhibited significant anti-cancer potency. It was found that representative compound 6a selectively killed cancerous but not normal cells. Moreover, compound 6a was effective in causing apoptosis in RPMI 8226 cells and exhibited promising HDAC-inhibitory activities.
Keywords: anti-cancer activity; apoptosis; histone acetylation; multiple myeloma; pyrimidine hydroxamic acid; sulfide substituent.
© 2015 John Wiley & Sons A/S.