849216-79-1Relevant articles and documents
Evaluation and docking of indole sulfonamide as a potent inhibitor of α-glucosidase enzyme in streptozotocin –induced diabetic albino wistar rats
Taha, Muhammad,Imran, Syahrul,Salahuddin, Mohammed,Iqbal, Naveed,Rahim, Fazal,Uddin, Nizam,Shehzad, Adeeb,Khalid Farooq, Rai,Alomari, Munther,Mohammed Khan, Khalid
, (2021/03/26)
We have synthesized new hybrid class of indole bearing sulfonamide scaffolds (1–17) as α-glucosidase inhibitors. All scaffolds were found to be active except scaffold 17 and exhibited IC50 values ranging from 1.60 to 51.20 μM in comparison with
Small-molecule inhibitors that target protein-protein interactions in the RAD51 family of recombinases
Scott, Duncan E.,Coyne, Anthony G.,Venkitaraman, Ashok,Blundell, Tom L.,Abell, Chris,Hyv?nen, Marko
supporting information, p. 296 - 303 (2015/02/05)
The development of small molecules that inhibit protein-protein interactions continues to be a challenge in chemical biology and drug discovery. Herein we report the development of indole-based fragments that bind in a shallow surface pocket of a humanised surrogate of RAD51. RAD51 is an ATP-dependent recombinase that plays a key role in the repair of doublestrand DNA breaks. It both self-associates, forming filament structures with DNA, and interacts with the BRCA2 protein through a common "FxxA" tetrapeptide motif. We elaborated previously identified fragment hits that target the FxxA motif site and developed small-molecule inhibitors that are approximately 500-fold more potent than the initial fragments. The lead compounds were shown to compete with the BRCA2-derived Ac-FHTA-NH2 peptide and the self-association peptide of RAD51, but they had no effect on ATP binding. This study is the first reported elaboration of small-molecular-weight fragments against this challenging target.
Indole-3-ethylsulfamoylphenylacrylamides: Potent histone deacetylase inhibitors with anti-inflammatory activity
Mehndiratta, Samir,Hsieh, Yi-Ling,Liu, Yi-Min,Wang, Amber Weiching,Lee, Hsueh-Yun,Liang, Lung-Yu,Kumar, Sunil,Teng, Che-Ming,Yang, Chia-Ron,Liou, Jing-Ping
, p. 468 - 479 (2015/02/19)
A series of 2-methyl-1H-indol-3-ethylsulfamoylphenylacrylamides based on LBH589-PXD101 core have been synthesized and evaluated for their histone deacetylase (HDAC) inhibitory and anti-inflammatory activity. In vitro, compounds 9-12 show 2.6-fold better H