Literature DB >> 21561771

Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.

Kazutomo Kinoshita1, Yoshiyuki Ono, Takashi Emura, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Shota Tanaka, Kenji Morikami, Toshiyuki Tsukaguchi, Hiroshi Sakamoto, Takuo Tsukuda, Nobuhiro Oikawa.   

Abstract

Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered a promising therapeutic target for human cancers. We identified novel tetracyclic derivatives as potent ALK inhibitors. Among them, compound 27 showed strong cytotoxicity against KARPAS-299 with an IC(50) value of 21 nM and significant antitumor efficacy in ALK fusion-positive blood and solid cancer xenograft models in mice without body weight loss.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21561771     DOI: 10.1016/j.bmcl.2011.04.020

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  ALK and ROS1 as a joint target for the treatment of lung cancer: a review.

Authors:  Raimon Puig de la Bellacasa; Niki Karachaliou; Roger Estrada-Tejedor; Jordi Teixidó; Carlota Costa; José I Borrell
Journal:  Transl Lung Cancer Res       Date:  2013-04

Review 2.  Latest perspectives of orally bioavailable 2,4-diarylaminopyrimidine analogues (DAAPalogues) as anaplastic lymphoma kinase inhibitors: discovery and clinical developments.

Authors:  Muhammad Latif; Zaman Ashraf; Sulman Basit; Abdul Ghaffar; Muhammad Sohail Zafar; Aamer Saeed; Sultan Ayoub Meo
Journal:  RSC Adv       Date:  2018-05-04       Impact factor: 4.036

  2 in total

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