2. Academic Validation
  3. Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors

Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors

  • Bioorg Med Chem Lett. 2009 Nov 15;19(22):6437-40. doi: 10.1016/j.bmcl.2009.09.038.
Peng Cho Tang 1,  Jun Feng,  Li Huang,  Zhe Xu,  Ling Cheng,  Xu Zhang,  Lei Zhang,  Bing Hu
Affiliations

Affiliation

  • 1 Shanghai Hengrui Pharmaceuticals Co., Ltd., 279 Wenjing Road, Shanghai 200245, China. tangpc@shhrp.com
PMID: 19815412 DOI: 10.1016/j.bmcl.2009.09.038
Abstract

A series of novel pyrrolopyridazine derivatives have been discovered to be HER-2 inhibitors. These compounds selectively inhibited HER-2 kinase activity at low nanomolar concentrations. Compound 7d was identified as a potent HER-2 inhibitor with an IC(50) of 4 nM.

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