A new series of diarylamides possessing quinoline nucleus: Synthesis, in vitro anticancer activities, and kinase inhibitory effect

Title
A new series of diarylamides possessing quinoline nucleus: Synthesis, in vitro anticancer activities, and kinase inhibitory effect
Authors
모하메드엘가말아쉬라푸딩모하메드 사미르마흐무드 가말엘딘오창현
Keywords
Antiproliferative activity; C-RAF kinase; Quinoline; Diarylamide; In silico
Issue Date
2014-11
Publisher
European journal of medicinal chemistry
Citation
VOL 87, 484-492
Abstract
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).
URI
http://pubs.kist.re.kr/handle/201004/48670
ISSN
02235234
Appears in Collections:
KIST Publication > Article
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