Literature DB >> 24900831

Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities.

Zhiqing Liu1, Jing Ai1, Xia Peng1, Zilan Song1, Kui Wu2, Jing Zhang1, Qizheng Yao2, Yi Chen1, Yinchun Ji1, Yanhong Yang1, Meiyu Geng1, Ao Zhang1.   

Abstract

By repurposing a typical dopamine D1/D5 receptor agonist motif, C1-substituted-N3-benzazepine or benzazecine, into the classical RTK inhibitor 2,4-diaminopyrimidine skeleton, a series of new 2,4-diarylaminopyrimidine analogues (DAAPalogues) were developed. Compounds 7 and 8a were identified possessing high potency against both c-Met and ALK kinases. Compound 8a displayed appreciable antitumor efficacy at the dose of 1 mg/kg in the ALK-driven BF3/EML4-ALK xenograft mice model.

Entities:  

Keywords:  2,4-diarylaminopyrimidine analogues; C1-Substituted-N3-benzazepine; c-Met/ALK dual inhibitor; structure repurposing

Year:  2014        PMID： 24900831      PMCID： PMC4027579          DOI： 10.1021/ml400373j

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  29 in total

Review 1.  New strategies for treatment of ALK-rearranged non-small cell lung cancers.

Authors:  Takaaki Sasaki; Pasi A Jänne
Journal:  Clin Cancer Res       Date:  2011-10-18       Impact factor: 12.531

2.  CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.

Authors:  Hiroshi Sakamoto; Toshiyuki Tsukaguchi; Sayuri Hiroshima; Tatsushi Kodama; Takamitsu Kobayashi; Takaaki A Fukami; Nobuhiro Oikawa; Takuo Tsukuda; Nobuya Ishii; Yuko Aoki
Journal:  Cancer Cell       Date:  2011-05-17       Impact factor: 31.743

3.  Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinase inhibitors.

Authors:  Christine M Lovly; Johannes M Heuckmann; Elisa de Stanchina; Heidi Chen; Roman K Thomas; Chris Liang; William Pao
Journal:  Cancer Res       Date:  2011-05-25       Impact factor: 12.701

4.  Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.

Authors:  Ailing Zhao; Xin Gao; Yuanxiang Wang; Jing Ai; Ying Wang; Yi Chen; Meiyu Geng; Ao Zhang
Journal:  Bioorg Med Chem       Date:  2011-05-24       Impact factor: 3.641

Review 5.  Inhibitors of the anaplastic lymphoma kinase.

Authors:  Luca Mologni
Journal:  Expert Opin Investig Drugs       Date:  2012-05-22       Impact factor: 6.206

6.  Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: synthesis and SAR study as tyrosine kinase c-Met inhibitors.

Authors:  Kui Wu; Jing Ai; Qiufeng Liu; TianTian Chen; Ailing Zhao; Xia Peng; Yuanxiang Wang; Yinchun Ji; Qizheng Yao; Yechun Xu; Meiyu Geng; Ao Zhang
Journal:  Bioorg Med Chem Lett       Date:  2012-08-27       Impact factor: 2.823

Review 7.  Drug development of MET inhibitors: targeting oncogene addiction and expedience.

Authors:  Paolo M Comoglio; Silvia Giordano; Livio Trusolino
Journal:  Nat Rev Drug Discov       Date:  2008-06       Impact factor: 84.694

8.  A mouse model for EML4-ALK-positive lung cancer.

Authors:  Manabu Soda; Shuji Takada; Kengo Takeuchi; Young Lim Choi; Munehiro Enomoto; Toshihide Ueno; Hidenori Haruta; Toru Hamada; Yoshihiro Yamashita; Yuichi Ishikawa; Yukihiko Sugiyama; Hiroyuki Mano
Journal:  Proc Natl Acad Sci U S A       Date:  2008-12-08       Impact factor: 11.205

9.  Global survey of phosphotyrosine signaling identifies oncogenic kinases in lung cancer.

Authors:  Klarisa Rikova; Ailan Guo; Qingfu Zeng; Anthony Possemato; Jian Yu; Herbert Haack; Julie Nardone; Kimberly Lee; Cynthia Reeves; Yu Li; Yerong Hu; Zhiping Tan; Matthew Stokes; Laura Sullivan; Jeffrey Mitchell; Randy Wetzel; Joan Macneill; Jian Min Ren; Jin Yuan; Corey E Bakalarski; Judit Villen; Jon M Kornhauser; Bradley Smith; Daiqiang Li; Xinmin Zhou; Steven P Gygi; Ting-Lei Gu; Roberto D Polakiewicz; John Rush; Michael J Comb
Journal:  Cell       Date:  2007-12-14       Impact factor: 41.582

10.  Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma.

Authors:  James G Christensen; Helen Y Zou; Maria E Arango; Qiuhua Li; Joseph H Lee; Scott R McDonnell; Shinji Yamazaki; Gordon R Alton; Barbara Mroczkowski; Gerrit Los
Journal:  Mol Cancer Ther       Date:  2007-12       Impact factor: 6.261
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  1 in total

1.  Data driven polypharmacological drug design for lung cancer: analyses for targeting ALK, MET, and EGFR.

Authors:  Dilip Narayanan; Osman A B S M Gani; Franz X E Gruber; Richard A Engh
Journal:  J Cheminform       Date:  2017-07-04       Impact factor: 5.514
  1 in total

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