Synthesis and in Vitro Cholesteryl Ester Transfer Protein Inhibitory Activity of Novel Esters of 2, 10-dichloro-12H-dibenzo [d,g] 1,3- dioxocin-6-carboxylic Acid

Talluri, Sirishadevi and Kini, Suvarna G and Kumar, Ganesh (2014) Synthesis and in Vitro Cholesteryl Ester Transfer Protein Inhibitory Activity of Novel Esters of 2, 10-dichloro-12H-dibenzo [d,g] 1,3- dioxocin-6-carboxylic Acid. Medicinal Chemistry Research, 23 (10). :4491-4499. ISSN 1054-2523

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Abstract

Novel ester derivatives of 2, 10-dichloro-12Hdibenzo [d,g] 1,3 dioxocin-6-carboxylic acid were synthesized and evaluated for their in vitro human cholesteryl ester transfer protein (CETP) inhibition. Three out of twelve synthesized compounds showed good inhibition of CETP (more than 50 %). Compound 10 showed 81.32 % inhibition of CETP at the dose of 0.5 nM whereas compound 11 showed 75.78 % inhibition when tested at the same concentration. Compound 8 and 13 also showed modest activity with 57.44 and 38.02 % inhibition. All other synthesized compounds were devoid of significant inhibitory activity against CETP. We also performed molecular docking to predict the mode of binding of all compounds at the active site of CETP. Compound 10 showed the dock score of -9.16 whereas the dock score of compound 11 was found to be -9.09

Item Type: Article
Uncontrolled Keywords: Cholesteryl Ester Transfer Protein (CETP) ; 2, 10-Dichloro-12H-dibenzo [d,g] [1,3] dioxocin-6- carboxylic acid; In Vitro activity
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Depositing User: KMC Manipal
Date Deposited: 06 Dec 2014 10:29
Last Modified: 06 Dec 2014 10:29
URI: http://eprints.manipal.edu/id/eprint/141229

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