Novel quinolinylaminoisoquinoline bioisosteres of sorafenib as selective RAF1 kinase inhibitors: design, synthesis, and antiproliferative activity against melanoma cell …
HJ Cho, MI El-Gamal, CH Oh, SH Lee, T Sim…
文献索引：Cho, Hye Jung; El-Gamal, Mohammed Ibrahim; Oh, Chang-Hyun; Lee, So Ha; Sim, Taebo; Kim, Garam; Choi, Hong Seok; Choi, Jung Hoon; Yoo, Kyung Ho Chemical and Pharmaceutical Bulletin, 2013 , vol. 61, # 7 p. 747 - 756
Design and synthesis of a new series of quinolinylaminoisoquinoline derivatives as conformationally restricted bioisosteres of Sorafenib are described. Their in vitro antiproliferative activity against A375P melanoma cell line was tested. Compounds 1b, 1d, 1g, and 1j showed the highest potency against A375P cell line with IC 50 values in sub- micromolar scale. In addition, compound 1d exerted high selectivity towards RAF1 serine/ ...
