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Ribonuclease A Inhibition by Carboxymethylsulfonyl‐Modified Xylo‐ and Arabinopyrimidines
Author(s) -
Datta Dhrubajyoti,
Dasgupta Swagata,
Pathak Tanmaya
Publication year - 2014
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201402179
Subject(s) - ribonuclease , chemistry , ribonuclease iii , computational biology , biochemistry , stereochemistry , combinatorial chemistry , biology , rna , gene , rna interference
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 SO 2 CH 2 COOH groups at the 2′‐ and 3′‐positions show good inhibitory properties with low inhibition constant ( K i ) values in the range of 109–17 μ M . 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.