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Design, Synthesis and Biological Activities of New Pyrazole Derivatives Possessing Both Coxib and Combretastatins Pharmacophores
Author(s) -
Thi Thuy Hang Nguyen,
Thi Yen Tran,
Nguyen Le Anh,
Vo Ngoc Binh,
Ngo Quoc Anh
Publication year - 2019
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201900108
Subject(s) - pharmacophore , chemistry , pyrazole , aryl , combinatorial chemistry , celecoxib , stereochemistry , molecule , combretastatin , organic chemistry , biochemistry , alkyl , microtubule , tubulin , biology , microbiology and biotechnology
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‐1 H ‐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.