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Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors.

Authors
  • Zhang, Qing1
  • Zhao, Kuantao1
  • Zhang, Lixun1
  • Jiao, Xiaoyu1
  • Zhang, Yongjie1
  • Tang, Chunlei2
  • 1 School of Pharmaceutical Science, Jiangnan University, Wuxi, China. , (China)
  • 2 School of Pharmaceutical Science, Jiangnan University, Wuxi, China. Electronic address: [email protected] , (China)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Sep 05, 2020
Pages
127525–127525
Identifiers
DOI: 10.1016/j.bmcl.2020.127525
PMID: 32898697
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

As a class III receptor tyrosine kinase (RTK), FMS-like tyrosine kinase 3 (FLT3) is always overexpressed in many cases of acute leukemia. This paper studies the structure-based synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 15b, 16b, 24a, and 24c showed excellent biological activities in a low nanomolar range. In particular, compound 16b demonstrated significant inhibitory potency against FLT3-ITD (IC50 = 5.60 nM) and better antiproliferative activity than quizartinib against MV4-11 cell line (IC50 = 0.176 nM). It is indicated that compound 16b for the treatment of acute myeloid leukemia could be very promising. Copyright © 2020. Published by Elsevier Ltd.

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