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4 results on '"Hernandez-Torres G"'

3. Total Stereoselective Synthesis of (+)-Goniothalesdiol

Author

Carreno, M. C., Hernandez-Torres, G., Urbano, A., and Colobert, F.

Abstract

The stereoselective synthesis of (+)-goniothalesdiol (1) was accomplished in nine steps starting from commercially available (−)-(2S,3S)-dimethyl d-tartrate (3). The key features were a completely diastereoselective reduction of a β-ketosulfoxide to generate the stereogenic center at C-5 in 7 and formation of the 2,5-cis-substituted tetrahydrofuran ring in 10 from a stereoselective Et3SiH/TMSOTf-promoted reductive cyclization/deoxygenation.

Published
2005

4. Design and Discovery of a Potent and Selective Inhibitor of Integrin αvβ1.

Author

Sabat M, Carney DW, Hernandez-Torres G, Gibson TS, Balakrishna D, Zou H, Xu R, Chen CH, de Jong R, Dougan DR, Qin L, Bigi-Botterill SV, Chambers A, Miura J, Johnson LK, Ermolieff J, Johns D, Selimkhanov J, Kwok L, DeMent K, Proffitt C, Vu P, Lindsey EA, Ivetac T, Jennings A, Wang H, Manam P, Santos C, Fullenwider C, Manohar R, and Flick AC

Subjects
Animals, Rats, Humans, Structure-Activity Relationship, Liver Cirrhosis drug therapy, Models, Molecular, Drug Discovery, Rats, Sprague-Dawley, Male, Crystallography, X-Ray, Benzimidazoles pharmacology, Benzimidazoles chemistry, Benzimidazoles chemical synthesis, Drug Design, Receptors, Vitronectin antagonists & inhibitors, Receptors, Vitronectin metabolism
Abstract

Selective inhibition of the RGD (Arg-Gly-Asp) integrin αvβ1 has been recently identified as an attractive therapeutic approach for the treatment of liver fibrosis given its function, target expression, and safety profile. Our identification of a non-RGD small molecule lead followed by focused, systematic changes to the core structure utilizing a crystal structure, in silico modeling, and a tractable synthetic approach resulted in the identification of a potent small molecule exhibiting a remarkable affinity for αvβ1 relative to several other integrin isoforms measured. Azabenzimidazolone 25 demonstrated antifibrotic efficacy in an in vivo rat liver fibrosis model and represents a tool compound capable of further exploring the biological consequences of selective αvβ1 inhibition.

Published
2024
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