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

Novel ester derivatives of 2, 10-dichloro-12 H -dibenzo [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 %). Compou...

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Bibliographic Details
Published in:Medicinal chemistry research 2014-10, Vol.23 (10), p.4491-4499
Main Authors: Talluri, Sirishadevi, Kini, Suvarna G., Kandale, Ajit, Kumar, Ganesh, Ohlyan, Renu
Format: Article
Language:English
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
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Summary:Novel ester derivatives of 2, 10-dichloro-12 H -dibenzo [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.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-014-1021-1