Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New Diarylureas and Diarylamides Possessing 1,3,4-Triarylpyrazole Scaffold 


Vol. 33,  No. 9, pp. 2991-2998, Sep.  2012
10.5012/bkcs.2012.33.9.2991


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  Abstract

A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.

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  Cite this article

[IEEE Style]

W. Choi, M. I. El-Gamal, H. S. Choi, J. H. Hong, D. Baek, K. Choi, C. Oh, "Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New Diarylureas and Diarylamides Possessing 1,3,4-Triarylpyrazole Scaffold," Bulletin of the Korean Chemical Society, vol. 33, no. 9, pp. 2991-2998, 2012. DOI: 10.5012/bkcs.2012.33.9.2991.

[ACM Style]

Won-Kyoung Choi, Mohammed I. El-Gamal, Hong Seok Choi, Jun Hee Hong, Daejin Baek, Kihang Choi, and Chang-Hyun Oh. 2012. Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New Diarylureas and Diarylamides Possessing 1,3,4-Triarylpyrazole Scaffold. Bulletin of the Korean Chemical Society, 33, 9, (2012), 2991-2998. DOI: 10.5012/bkcs.2012.33.9.2991.

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ISSN(Print) 0253-2964
ISSN(Online) 1229-5949