2. Academic Validation
  3. Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802)

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

  • Bioorg Med Chem. 2012 Feb 1;20(3):1271-80. doi: 10.1016/j.bmc.2011.12.021.
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

Affiliation

  • 1 Research Division, Chugai Pharmaceutical Co., Ltd, 200 Kajiwara, Kamakura, Kanagawa 247-8530, Japan. kinoshitakzt@chugai-pharm.co.jp
PMID: 22225917 DOI: 10.1016/j.bmc.2011.12.021
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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