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

Authors
Choi, Won-KyoungEl-Gamal, Mohammed I.Choi, Hong SeokHong, Jun HeeBaek, DaejinChoi, KihangOh, Chang-Hyun
Issue Date
2012-09-20
Publisher
KOREAN CHEMICAL SOC
Citation
BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.33, no.9, pp.2991 - 2998
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.
Keywords
MELANOMA-CELL LINE; ANTIPROLIFERATIVE ACTIVITY; DERIVATIVES; DISCOVERY; MELANOMA-CELL LINE; ANTIPROLIFERATIVE ACTIVITY; DERIVATIVES; DISCOVERY; A375P; Anticancer; Diarylamide; Diarylurea; 1,3,4-Triarylpyrazole
ISSN
0253-2964
URI
https://pubs.kist.re.kr/handle/201004/128864
DOI
10.5012/bkcs.2012.33.9.2991
Appears in Collections:
KIST Article > 2012
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