El-Gamal Mohammed I, Khan Mohammad Ashrafuddin, Abdel-Maksoud Mohammed S, Gamal El-Din Mahmoud M, Oh Chang-Hyun
Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt.
Center for Biomaterials, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea; Department of Biomolecular Science, University of Science and Technology, 113 Gwahangno, Yuseong-gu, Daejeon 305-333, Republic of Korea.
Eur J Med Chem. 2014 Nov 24;87:484-92. doi: 10.1016/j.ejmech.2014.09.068. Epub 2014 Sep 23.
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).
描述了一系列具有6,7-二甲氧基(二羟基)喹啉骨架的新型二芳基酰胺的合成。测试了它们对9种不同癌症类型的NCI-58人癌细胞系的体外抗增殖活性。化合物1a和1d-g在10μM时在58种细胞系组中显示出最高的平均抑制率,并且它们以5剂量测试模式进一步测试以确定其IC50值。这五种化合物对9种不同癌症类型的所有细胞系比伊马替尼更有效。化合物1g显示出最高的效力。它对C-RAF激酶显示出抑制作用(在10μM浓度下为76.65%)。