TY - JOUR
T1 - Isatin sulfonamide analogs containing a Michael addition acceptor
T2 - A new class of caspase 3/7 inhibitors
AU - Chu, Wenhua
AU - Rothfuss, Justin
AU - D'Avignon, André
AU - Zeng, Chenbo
AU - Zhou, Dong
AU - Hotchkiss, Richard S.
AU - Mach, Robert H.
PY - 2007/7/26
Y1 - 2007/7/26
N2 - A series of isatin sulfonamide analogs having a Michael acceptor were prepared and their potencies for inhibiting caspase-1, -3, -6, -7, and -8 were evaluated. These compounds have nanomolar potency for inhibiting the executioner caspases, caspase-3 and caspase-7, and have a low potency for inhibiting caspase-1, caspase-6, and caspase-8. The inhibition mechanism was investigated through NMR studies of the reaction between 11d and benzylmercaptan as a model for Cys-285 in the active site of caspase-3.
AB - A series of isatin sulfonamide analogs having a Michael acceptor were prepared and their potencies for inhibiting caspase-1, -3, -6, -7, and -8 were evaluated. These compounds have nanomolar potency for inhibiting the executioner caspases, caspase-3 and caspase-7, and have a low potency for inhibiting caspase-1, caspase-6, and caspase-8. The inhibition mechanism was investigated through NMR studies of the reaction between 11d and benzylmercaptan as a model for Cys-285 in the active site of caspase-3.
UR - http://www.scopus.com/inward/record.url?scp=34547593361&partnerID=8YFLogxK
U2 - 10.1021/jm070506t
DO - 10.1021/jm070506t
M3 - Article
C2 - 17585855
AN - SCOPUS:34547593361
SN - 0022-2623
VL - 50
SP - 3751
EP - 3755
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 15
ER -