Reed, Nilgun Isik published the artcileExploring N-Arylsulfonyl-L-proline Scaffold as a Platform for Potent and Selective αvβ1 Integrin Inhibitors, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is arylsulfonylproline scaffold preparation alphavbeta1 integrin inhibitor structure activity antifibrotic; RGF mimetic preparation alphavbeta1 integrin inhibitor structure activity antifibrotic; Fibrosis; TGFβ; integrin antagonist; phenylsulfonylproline; αvβ1 integrin.
One small mol. inhibitor of αvβ1 integrin, RGD mimetic c8, shows antifibrotic effects in multiple in vivo mouse models. Here the authors synthesized c8 analogs and systematically investigate their structure-activity relationships (SAR) in αvβ1 integrin inhibition. N-Phenylsulfonyl-L-homoproline analogs of c8 maintained excellent potency against αvβ1 integrin while retaining good selectivity over other RGD integrins. In addition, 2-aminopyridine or cyclic guanidine analogs were shown to be equally potent to c8. A rigid Ph linker increased the potency compared to c8, but the selectivity over other RGD integrins diminished. These results can provide further insights on design of αvβ1 integrin inhibitors as antifibrotics.
ACS Medicinal Chemistry Letters published new progress about Antifibrotic agents. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Application of 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics