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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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14초록
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
- 발행일
- 2012-09-20
- 유형
- Article
- 권
- 33
- 호
- 9
- 페이지
- 2991 ~ 2998