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

Choi, Won-Kyoung; El-Gamal, Mohammed I.; Choi, Hong Seok; Hong, Jun Hee; Baek, Daejin; Choi, Kihang; Oh, Chang-Hyun

doi:10.5012/bkcs.2012.33.9.2991

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

Choi, Won-Kyoung;
El-Gamal, Mohammed I.;
Choi, Hong Seok;
Hong, Jun Hee;
Baek, Daejin;
... Choi, Kihang;
외 1명

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WEB OF SCIENCE

13

Citations

SCOPUS

14

초록

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.

키워드

A375P; Anticancer; Diarylamide; Diarylurea; 1,3,4-Triarylpyrazole; MELANOMA-CELL LINE; ANTIPROLIFERATIVE ACTIVITY; DERIVATIVES; DISCOVERY

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

저자: Choi, Won-Kyoung; El-Gamal, Mohammed I.; Choi, Hong Seok; Hong, Jun Hee; Baek, Daejin; Choi, Kihang; Oh, Chang-Hyun

DOI: 10.5012/bkcs.2012.33.9.2991

발행일: 2012-09-20

유형: Article

저널명: Bulletin of the Korean Chemical Society

권: 33

호: 9

페이지: 2991 ~ 2998

언어: ENG

출판사: KOREAN CHEMICAL SOC

발행국가: 대한민국

분량: 8 페이지

ISSN: E 1229-5949
P 0253-2964