New triarylpyrazoles as broad-spectrum anticancer agents: Design, synthesis, and biological evaluation
- New triarylpyrazoles as broad-spectrum anticancer agents: Design, synthesis, and biological evaluation
- 모하메드엘가말; 박이슬; 지대윤; 유경호; 오창현
- Anticancer; Cytotoxicity; Diarylurea; Diarylamide; 1,3,4-Triarylpyrazole
- Issue Date
- European journal of medicinal chemistry
- VOL 65, 315-322
- A new series of diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was designed and synthesized. Their in vitro antiproliferative activities against NCI-60 cell line panel were tested. Most of the compounds showed strong and broad-spectrum antiproliferative activities. Compound 18 exerted sub-micromolar IC50 values over all the subpanels of nine different cancer types. Its IC50 value over MDAMB-435 melanoma cell line was 27 nM. Compounds 10e13, 22, and 23 possessing urea spacer exerted lethal effect over the NCI-60 panel with mean %inhibitions more than 100% in single-dose testing.
Compounds 13 and 23 with urea linker and 30,50-bis(trifluoromethyl)phenyl terminal ring showed the highest mean %inhibition over the NCI-60 panel in single-dose testing, and showed high potencies and broad-spectrum anticancer activities in five-dose testing.
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