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

作者：El Gamal Mohammed I^*; Khan Mohammad Ashrafuddin; Abdel Maksoud Mohammed S; El Din Mahmoud M Gamal; Oh Chang Hyun

来源：European Journal of Medicinal Chemistry, 2014, 87: 484-492.

DOI：10.1016/j.ejmech.2014.09.068

• Antiproliferative activity
• Diarylamide
• In silico
• C-RAF kinase
• Quinoline

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 oyer the 58 cell line panel at 10 mu M, 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 mu M concentration).

• 出版日期2014-11-24