| Literature DB >> 22225917 |
Kazutomo Kinoshita1, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Sousuke Hara, Jun Ohwada, Takuho Miyagi, Takamitsu Kobayashi, Kenji Takanashi, Toshiyuki Tsukaguchi, Hiroshi Sakamoto, Takuo Tsukuda, Nobuhiro Oikawa.
Abstract
Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered an attractive therapeutic target for human cancers, especially non-small cell lung cancer (NSCLC). Our previous study revealed that 8,9-side-chains of 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazole scaffold crucially affected kinase selectivity, cellular activity, and metabolic stability. In this work, we optimized the side-chains and identified highly selective, orally active and potent ALK inhibitor CH5424802 (18a) as the clinical candidate.Entities:
Mesh：
Substances：
Year: 2011 PMID： 22225917 DOI： 10.1016/j.bmc.2011.12.021
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641