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. 2012 Feb 1;20(3):1271-80.
doi: 10.1016/j.bmc.2011.12.021. Epub 2011 Dec 22.

Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802)

Kazutomo Kinoshita  1 , 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
Affiliations

Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802)

Kazutomo Kinoshita et al. Bioorg Med Chem. .

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.

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