Synthesis and anticancer activity evaluation of resveratrol-chalcone conjugates

Deepak Kumar; K. Kranthi Raj; Sanjay V. Malhotra; Diwan S. Rawat

doi:10.1039/c3md00329a

Synthesis and anticancer activity evaluation of resveratrol-chalcone conjugates

Deepak Kumar, K. Kranthi Raj, Sanjay V. Malhotra, Diwan S. Rawat

Research output: Contribution to journal › Article › peer-review

22 Scopus citations

Abstract

A series of novel resveratrol-chalcone conjugates have been synthesized. Four compounds were evaluated for their anticancer activity against 60 human cancer cell lines. Among all the derivatives, compound 70 was found to be the most active and showed high selectivity towards certain ovarian cancer, non-small cell lung cancer and breast cancer cell lines with GI₅₀ values in the range of 1.28-34.1 μM. Docking studies were performed to determine the probable binding mode of these compounds in the colchicine-tubulin binding site. A strong H-bonding interaction (1.852 Å) was observed with Cys-241 amino acid present in the binding pocket. Thus we believe that compound 70 may possibly be used as a lead for the development of new anticancer agents.

Original language	English (US)
Pages (from-to)	528-535
Number of pages	8
Journal	MedChemComm
Volume	5
Issue number	4
DOIs	https://doi.org/10.1039/c3md00329a
State	Published - Apr 2014
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Organic Chemistry

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title = "Synthesis and anticancer activity evaluation of resveratrol-chalcone conjugates",

abstract = "A series of novel resveratrol-chalcone conjugates have been synthesized. Four compounds were evaluated for their anticancer activity against 60 human cancer cell lines. Among all the derivatives, compound 70 was found to be the most active and showed high selectivity towards certain ovarian cancer, non-small cell lung cancer and breast cancer cell lines with GI50 values in the range of 1.28-34.1 μM. Docking studies were performed to determine the probable binding mode of these compounds in the colchicine-tubulin binding site. A strong H-bonding interaction (1.852 {\AA}) was observed with Cys-241 amino acid present in the binding pocket. Thus we believe that compound 70 may possibly be used as a lead for the development of new anticancer agents.",

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AU - Kumar, Deepak

AU - Raj, K. Kranthi

AU - Malhotra, Sanjay V.

AU - Rawat, Diwan S.

PY - 2014/4

Y1 - 2014/4

N2 - A series of novel resveratrol-chalcone conjugates have been synthesized. Four compounds were evaluated for their anticancer activity against 60 human cancer cell lines. Among all the derivatives, compound 70 was found to be the most active and showed high selectivity towards certain ovarian cancer, non-small cell lung cancer and breast cancer cell lines with GI50 values in the range of 1.28-34.1 μM. Docking studies were performed to determine the probable binding mode of these compounds in the colchicine-tubulin binding site. A strong H-bonding interaction (1.852 Å) was observed with Cys-241 amino acid present in the binding pocket. Thus we believe that compound 70 may possibly be used as a lead for the development of new anticancer agents.

AB - A series of novel resveratrol-chalcone conjugates have been synthesized. Four compounds were evaluated for their anticancer activity against 60 human cancer cell lines. Among all the derivatives, compound 70 was found to be the most active and showed high selectivity towards certain ovarian cancer, non-small cell lung cancer and breast cancer cell lines with GI50 values in the range of 1.28-34.1 μM. Docking studies were performed to determine the probable binding mode of these compounds in the colchicine-tubulin binding site. A strong H-bonding interaction (1.852 Å) was observed with Cys-241 amino acid present in the binding pocket. Thus we believe that compound 70 may possibly be used as a lead for the development of new anticancer agents.

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Synthesis and anticancer activity evaluation of resveratrol-chalcone conjugates

Abstract

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