Synthesis of novel N-(2-hydroxyphenyl)arylsulfonamides as selective HDAC inhibitory and cytotoxic agents
Synthesis of novel N-(2-hydroxyphenyl)arylsulfonamides as selective HDAC inhibitory and cytotoxic agents / Jungsu Kim, Pusoon Chun, Hyung Ryong Moon
p. 1487-1493 ; 28 cm
수록자료: Bulletin of the Korean Chemical Society. Korean Chemical Society. Vol.34 No.5(2013 May). p. 1487-1493 34:5<1487 ISSN 0253-2964 저자: Jungsu Kim, Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University 저자: Pusoon Chun, College of Pharmacy, Inje University E-MAIL: email@example.com 저자: Hyung Ryong Moon, Laboratory of Medicinal Chemistry, College of Pharmacy, Pusan National University E-MAIL: firstname.lastname@example.org
Based on the finding that the 2-aminobenzamido group of MS-275 plays a crucial role in inhibiting HDACs through chelation of zinc existing at the active site of HDAC enzymes, novel N-(2-hydroxyphenyl)arylsulfonamide derivatives were synthesized for their potential ability to inhibit HDACs and evaluated for anticancer activity against human breast cancer cell line (MCF-7). Although the synthesized arylsulfonamides have failed to significantly inhibit total HDACs activity, phenyl carbamate-linked arylsulfonamide 10 and benzyl thiocarbamate-linked arylsulfonamide 15 exhibited good anticancer activities, which were only 4.3- and 3.6-fold lower anticancer activities, respectively, than MS-275 that is undergoing phase II clinical trials. These results suggest that these compounds may act as a selective HDAC inhibitor and probably N-(2-hydroxyphenyl) sulfamoyl group may play an important role in interacting with HDAC enzymes through chelation of zinc ion.