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Molecules 2015, 20(4), 5924-5941; doi:10.3390/molecules20045924

Carboxylated Acyclonucleosides: Synthesis and RNase A Inhibition

Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur 721302, India
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Authors to whom correspondence should be addressed.
Academic Editor: Mahesh Lakshman
Received: 17 December 2014 / Revised: 20 March 2015 / Accepted: 20 March 2015 / Published: 3 April 2015
(This article belongs to the Special Issue Nucleoside Modifications)
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Abstract

Strategically designed carboxylated acyclonucleosides have been probed as a new class of RNase A inhibitors. Several experimental and theoretical studies have been performed to compile relevant qualitative and quantitative information regarding the nature and extent of inhibition. The inhibition constant (Ki) values were determined using a UV-based kinetics experiment. The changes in the secondary structure of the enzyme upon binding with the inhibitors were obtained from circular dichroism studies. The binding constants for enzyme-inhibitor interactions were determined with the help of fluorescence spectroscopy. Docking studies were performed to reveal the possible binding sites of the inhibitors within the enzyme. The cytosine analogues were found to possess better inhibitory properties in comparison to the corresponding uracil derivatives. An increment in the number of carboxylic acid groups (-COOH) in the inhibitor backbone was found to result in better inhibition. View Full-Text
Keywords: acyclonucleosides; RNase A; inhibition; kinetics; docking acyclonucleosides; RNase A; inhibition; kinetics; docking
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Chakraborty, K.; Dasgupta, S.; Pathak, T. Carboxylated Acyclonucleosides: Synthesis and RNase A Inhibition. Molecules 2015, 20, 5924-5941.

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