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Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New Diarylureas and Diarylamides Possessing 1,3,4-Triarylpyrazole Scaffold
- Authors
- Choi, Won-Kyoung; El-Gamal, Mohammed I.; Choi, Hong Seok; Hong, Jun Hee; Baek, Daejin; Choi, Kihang; Oh, Chang-Hyun
- Issue Date
- 20-Sep-2012
- Publisher
- KOREAN CHEMICAL SOC
- Keywords
- A375P; Anticancer; Diarylamide; Diarylurea; 1,3,4-Triarylpyrazole
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.33, no.9, pp.2991 - 2998
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 33
- Number
- 9
- Start Page
- 2991
- End Page
- 2998
- ISSN
- 0253-2964
- 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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Related Researcher
- CHOI, Ki hang
- College of Science (Department of Chemistry)