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Synthesis, characterizations, biological activities and docking studies of novel dihydroxy derivatives of natural phenolic monoterpenoids containing azomethine linkage

Rajput, Jamatsing D and Bagul, Suresh D and Hosamani, Amar A and Patil, Manohar M and Bendre, Ratnamala S (2017) Synthesis, characterizations, biological activities and docking studies of novel dihydroxy derivatives of natural phenolic monoterpenoids containing azomethine linkage. In: RESEARCH ON CHEMICAL INTERMEDIATES, 43 (10). pp. 5377-5393.

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Official URL: http://doi.org/10.1007/s11164-017-2933-4

Abstract

In the present work, we report the synthesis of six new azomethine linkage containing dihydroxy derivatives of carvacrol, thymol, and eugenol. All the synthesized derivatives have been characterized by spectroscopic techniques and their structures were confirmed by X-ray single crystallography. Synthesized derivatives were screened for anti-oxidant activity using DPPH radical scavenging assay, and anticancer activity by using SRB assay against pancreatic cancer with MIAPaCa-2 and colon cancer with HCT-15 cell lines. The molecular docking studies of all the synthesized derivatives were performed on cyclooxygenases (COX-2) protein enzyme. In the anti-oxidant test, the values of EC50 indicated that all the compounds show excellent anti-oxidant potency, and similarly the GI(50) values in anticancer tests indicated that most of the compounds possess good anticancer efficacy. The overall docking score suggested that all the synthesized compounds exhibit good binding affinity towards cyclooxygenases (COX-2) protein enzyme. GRAPHICS] .

Item Type: Journal Article
Publication: RESEARCH ON CHEMICAL INTERMEDIATES
Department/Centre: Division of Chemical Sciences > Solid State & Structural Chemistry Unit
Date Deposited: 07 Oct 2017 06:08
Last Modified: 07 Oct 2017 06:08
URI: http://eprints.iisc.ac.in/id/eprint/57967

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