Ribonuclease A inhibition by carboxymethylsulfonyl-modified xylo- and arabinopyrimidines

Datta, Dhrubajyoti ; Dasgupta, Swagata ; Pathak, Tanmaya (2014) Ribonuclease A inhibition by carboxymethylsulfonyl-modified xylo- and arabinopyrimidines ChemMedChem, 9 (9). pp. 2138-2149. ISSN 1860-7179

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Official URL: http://onlinelibrary.wiley.com/doi/10.1002/cmdc.20...

Related URL: http://dx.doi.org/10.1002/cmdc.201402179

Abstract

A group of acidic nucleosides were synthesized to develop a new class of ribonuclease A (RNase A) inhibitors. Our recent study on carboxymethylsulfonyl-modified nucleosides revealed some interesting results in RNase A inhibition. This positive outcome triggered an investigation of the role played by secondary sugar hydroxy groups in inhibiting RNase A activity. Uridines and cytidines modified with -SO2CH2COOH groups at the 2'- and 3'-positions show good inhibitory properties with low inhibition constant (Ki) values in the range of 109–17 μM. The present work resulted in a set of inhibitors that undergo more effective interactions with the RNase A active site, as visualized by docking studies.

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ID Code:103751
Deposited On:22 Mar 2017 05:10
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