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
Citations

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

A375PAnticancerDiarylamideDiarylurea1,3,4-TriarylpyrazoleMELANOMA-CELL LINEANTIPROLIFERATIVE ACTIVITYDERIVATIVESDISCOVERY
제목
Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New Diarylureas and Diarylamides Possessing 1,3,4-Triarylpyrazole Scaffold
저자
Choi, Won-KyoungEl-Gamal, Mohammed I.Choi, Hong SeokHong, Jun HeeBaek, DaejinChoi, KihangOh, Chang-Hyun
DOI
10.5012/bkcs.2012.33.9.2991
발행일
2012-09-20
유형
Article
저널명
Bulletin of the Korean Chemical Society
33
9
페이지
2991 ~ 2998