TY - JOUR
T1 - Synthesis and evaluation of isatin analogs as caspase-3 inhibitors
T2 - Introduction of a hydrophilic group increases potency in a whole cell assay
AU - Chu, Wenhua
AU - Rothfuss, Justin
AU - Zhou, Dong
AU - MacH, Robert H.
N1 - Funding Information:
This research was funded by CA121952 and HL13851 awarded by the National Institutes of Health .
PY - 2011/4/15
Y1 - 2011/4/15
N2 - A series of isatin analogs containing a hydrophilic group, including a pyridine ring, ethylene glycol group, and a triazole ring, have been synthesized, and their inhibition potency for caspase-3 was measured both in vitro (i.e., recombinant enzyme) and in whole cells (HeLa cells). The analogs having a hydrophilic group, including 12, 13, 16, 38, and 40, have dramatically increased activity in vitro and in HeLa cells compared to the corresponding unsubstituted N-phenyl isatin analogs.
AB - A series of isatin analogs containing a hydrophilic group, including a pyridine ring, ethylene glycol group, and a triazole ring, have been synthesized, and their inhibition potency for caspase-3 was measured both in vitro (i.e., recombinant enzyme) and in whole cells (HeLa cells). The analogs having a hydrophilic group, including 12, 13, 16, 38, and 40, have dramatically increased activity in vitro and in HeLa cells compared to the corresponding unsubstituted N-phenyl isatin analogs.
KW - Apoptosis
KW - Caspase-3
KW - Cell death
UR - http://www.scopus.com/inward/record.url?scp=79953281429&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2011.03.015
DO - 10.1016/j.bmcl.2011.03.015
M3 - Article
C2 - 21441025
AN - SCOPUS:79953281429
SN - 0960-894X
VL - 21
SP - 2192
EP - 2197
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 8
ER -