A new series of diarylamides possessing quinoline nucleus: Synthesis, in vitro anticancer activities, and kinase inhibitory effect
- A new series of diarylamides possessing quinoline nucleus: Synthesis, in vitro anticancer activities, and kinase inhibitory effect
- 모하메드엘가말; 아쉬라푸딩; 모하메드 사미르; 마흐무드 가말엘딘; 오창현
- Antiproliferative activity; C-RAF kinase; Quinoline; Diarylamide; In silico
- Issue Date
- European journal of medicinal chemistry
- VOL 87, 484-492
- Synthesis of a new series of diarylamides possessing 6,7-dimethoxy(dihydroxy)quinoline scaffold is described. Their in vitro antiproliferative activities against NCI-58 human cancer cell lines of nine different cancer types were tested. Compounds 1a and 1d–g showed the highest mean %inhibition values over the 58 cell line panel at 10 μM, and they were further tested in 5-dose testing mode to determine their IC50 values. The five compounds were more potent than Imatinib against all the cell lines of nine different cancer types. Compound 1g showed the highest potencies. It showed inhibitory effect against C-RAF kinase (76.65% at 10 μM concentration).
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