879896-41-0Relevant academic research and scientific papers
1,2-Benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors
Wu, Lixin,Lu, Meiqi,Yan, Zhihui,Tang, Xiaobin,Sun, Bo,Liu, Wei,Zhou, Honggang,Yang, Cheng
, p. 2416 - 2426 (2014/05/06)
A novel series of 1,2-benzisothiazol-3-one derivatives was synthesized and their biological activities were evaluated for inhibiting caspase-3 and -7 activities, in which some of them showed low nanomolar potency against caspase-3 in vitro and significant protection against apoptosis in a camptothecin-induced Jurkat T cells system. Among the tested compounds, compound 5i exhibited the most potent caspase-3 inhibitory activity (IC50 = 1.15 nM). The molecular docking predicted the interactions and binding modes of the synthesized inhibitor in the caspase-3 active site.
Benzodiazepines as potent and selective bradykinin B1 antagonists
Wood, Michael R.,Kim, June J.,Han, Wei,Dorsey, Bruce D.,Homnick, Carl F.,DiPardo, Robert M.,Kuduk, Scott D.,MacNeil, Tanya,Murphy, Kathy L.,Lis, Edward V.,Ransom, Richard W.,Stump, Gary L.,Lynch, Joseph J.,O'Malley, Stacey S.,Miller, Patricia J.,Chen, Tsing-Bau,Harrell, Charles M.,Chang, Raymond S. L.,Sandhu, Punam,Ellis, Joan D.,Bondiskey, Peter J.,Pettibone, Douglas J.,Freidinger, Roger M.,Bock, Mark G.
, p. 1803 - 1806 (2007/10/03)
Antagonism of the bradykinin B1 receptor was demonstrated to be a potential treatment for chronic pain and inflammation. Novel benzodiazepines were designed that display subnanomolar affinity for the bradykinin B1 receptor (Ki = 0.59 nM) and high selectivity against the bradykinin B2 receptor (Ki > 10 nM). In vivo efficacy, comparable to morphine, was demonstrated for lead compounds in a rodent hyperalgesia model.
