Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors | Zendy

Xianming Deng | Zendy; Jinhua Wang | Zendy; Jianming Zhang | Zendy; Taebo Sim | Zendy; Nam Doo Kim | Zendy; Takaaki Sasaki | Zendy; William Luther | Zendy; Rani E. George | Zendy; Pasi A. Jänne | Zendy; Nathanael S. Gray | Zendy

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Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors

Author(s) -

Xianming Deng,

Jinhua Wang,

Jianming Zhang,

Taebo Sim,

Nam Doo Kim,

Takaaki Sasaki,

William Luther,

Rani E. George,

Pasi A. Jänne,

Nathanael S. Gray

Publication year - 2011

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml200002a

Subject(s) - anaplastic lymphoma kinase , lymphoma , triazole , cancer research , computational biology , medicine , chemistry , biology , organic chemistry , malignant pleural effusion , pleural effusion

A series of novel 3,5-diamino-1,2,4-triazole benzyl ureas was identified as having potent anaplastic lymphoma kinase (ALK) inhibition exemplified by 15a, 20a, and 23a, which exhibited antiproliferative IC(50) values of 70, 40, and 20 nM in Tel-ALK transformed Ba/F3 cells, respectively. Moreover, 15a and 23a potently inhibited the growth and survival of NPM-ALK positive anaplastic large cell lymphoma cell (SU-DHL-1) and neuroblastoma cell lines (KELLY, SH-SY5Y) containing the F1174L ALK mutation. These compounds provide novel leads for the development of small-molecule ALK inhibitors for cancer therapy.

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