1611467-07-2Relevant academic research and scientific papers
Optimization of diaryl amine derivatives as kinesin spindle protein inhibitors
Takeuchi, Tomoki,Oishi, Shinya,Kaneda, Masato,Misu, Ryosuke,Ohno, Hiroaki,Sawada, Jun-Ichi,Asai, Akira,Nakamura, Shinya,Nakanishi, Isao,Fujii, Nobutaka
supporting information, p. 3171 - 3179 (2014/06/09)
Structure-activity relationship studies of diaryl amine-type KSP inhibitors were carried out. Diaryl amine derivatives with a pyridine ring or urea group were less active when compared with the parent carboline and carbazole derivatives. Optimization studies of a lactam-fused diphenylamine-type KSP inhibitor revealed that the aniline NH group and 3-CF3 phenyl group were indispensable for potent KSP inhibition. Modification with a seven-membered lactam-fused phenyl group and a 4-(trifluoromethyl)pyridin-2-yl group improved aqueous solubility while maintaining potent KSP inhibitory activity. From these studies, we identified novel diaryl amine-type KSP inhibitors with a favorable balance of potency and solubility.
