220510-03-2Relevant articles and documents
Pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. Synthesis and SAR of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-pyrrolo[3, 4-c]quinoline-1,3-diones
Kravchenko, Dmitri V.,Kysil, Volodymyr M.,Tkachenko, Sergey E.,Maliarchouk, Sergey,Okun, Ilya M.,Ivachtchenko, Alexandre V.
, p. 1377 - 1383 (2005)
Synthesis, biological evaluation and structure-activity relationships for a series of 2-substituted 4-methyl-8-(morpholine-4-sulfonyl)-1,3-dioxo-2,3- dihydro-1H-pyrrolo[3,4-c]quinolines are described. These compounds represent a new chemotype of nonpeptid
Synthesis, modification and docking studies of 5-sulfonyl isatin derivatives as SARS-CoV 3C-like protease inhibitors
Liu, Wei,Zhu, He-Min,Niu, Guo-Jun,Shi, En-Zhi,Chen, Jie,Sun, Bo,Chen, Wei-Qiang,Zhou, Hong-Gang,Yang, Cheng
, p. 292 - 302 (2014/01/17)
The Severe Acute Respiratory Syndrome (SARS) is a serious life-threatening and strikingly mortal respiratory illness caused by SARS-CoV. SARS-CoV which contains a chymotrypsin-like main protease analogous to that of the main picornavirus protease, 3CLpro. 3CLpro plays a pivotal role in the viral replication cycle and is a potential target for SARS inhibitor development. A series of isatin derivatives as possible SARS-CoV 3CL pro inhibitors was designed, synthesized, and evaluated by in vitro protease assay using fluorogenic substrate peptide, in which several showed potent inhibition against the 3CLpro. Structure-activity relationship was analyzed, and possible binding interaction modes were proposed by molecular docking studies. Among all compounds, 8k1 showed most potent inhibitory activity against 3CLpro (IC50 = 1.04 μM). These results indicated that these inhibitors could be potentially developed into anti-SARS drugs.
SUBSTITUTED OXINDOL CB2 AGONISTS FOR PAIN TREATMENT
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Page/Page column 121, (2010/08/04)
Provided are 3-substituted oxindole derivatives which are agonists of the CB2 receptor, pharmaceutical compositions containing the same, and methods of treatment related to CB2-mediated disorders (e.g., pain, cancer etc.) using the 3-substituted oxindole derivatives and compositions described herein.
Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6
Chu, Wenhua,Rothfuss, Justin,Chu, Yunxiang,Zhou, Dong,Mach, Robert H.
supporting information; experimental part, p. 2188 - 2191 (2010/03/03)
A key step in the onset of Huntington's disease is the caspase-6 mediated cleavage of the protein huntingtin into toxic fragments. Therefore, the inhibition of caspase-6 has been identified as a target for therapeutic drug development for the treatment of
INHIBITION OF SHP2/PTPN11 PROTEIN TYROSINE PHOSPHATASE BY NSC-87877, NSC-117199 AND THEIR ANALOGS
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Page/Page column 33, (2010/11/28)
Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Signif
Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1, 3-diones as potent caspase-3 inhibitors
Kravchenko, Dmitri V.,Kuzovkova, Yulia A.,Kysil, Volodymyr M.,Tkachenko, Sergey E.,Maliarchouk, Sergey,Okun, Ilya M.,Balakin, Konstantin V.,Ivachtchenko, Alexandre V.
, p. 3680 - 3683 (2007/10/03)
Synthesis, biological evaluation, and SAR dependencies for a series of novel 1,3-dioxo-2,3-dihydro-1H-pyrrolo-[3,4-c]quinoline inhibitors of caspase-3 are described. The inhibitory activity of the synthesized compounds is highly dependent on the nature of
