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Chem Biodivers. 2019 Jun;16(6):e1900108. doi: 10.1002/cbdv.201900108. Epub 2019 May 20.

Design, Synthesis and Biological Activities of New Pyrazole Derivatives Possessing Both Coxib and Combretastatins Pharmacophores.

Author information

1
Institute of Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, CauGiay, 100000, Hanoi, Viet Nam.
2
Graduate University of Science and Technology, 18 Hoang Quoc Viet, CauGiay, 100000, Hanoi, Viet Nam.

Abstract

In our efforts to discover novel multi-target agents having better antitumor activities than celecoxib, 21 new aryl-substituted pyrazole derivatives possessing cis-diphenylethylene scaffold were mostly synthesized by a one-pot approach to ethyl 1,4,5-triaryl-1H-pyrazole-3-carboxylates via an improved Claisen condensation - Knorr reaction sequence. The cytotoxic effects of these compounds against three human cancer cell lines HT-29, Hep-G2, MCF-7 as well as their inhibition of NO production were studied. Results showed that incorporation of the important pharmacophoric groups of two original molecules celecoxib and combretastatin A-4 in a single molecule plays an important role in determining a better biological activities of the new coxib-hybrided compounds.

KEYWORDS:

COX-2; celecoxib; combretastatin; cytotoxicity; hybrid compounds; multi-target agents; synthesis design

PMID:
30977306
DOI:
10.1002/cbdv.201900108
[Indexed for MEDLINE]

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