Literature DB >> 16111887

New dual inhibitors of EGFR and HER2 protein tyrosine kinases.

Brian E Fink1, Gregory D Vite, Harold Mastalerz, John F Kadow, Soong-Hoon Kim, Kenneth J Leavitt, Karen Du, Donald Crews, Toomas Mitt, Tai W Wong, John T Hunt, Dolatrai M Vyas, John S Tokarski.   

Abstract

A novel series of dual EGFR and HER2 inhibitors based on the pyrrolo[2,1-f][1,2,4]triazine nucleus is described. A general route toward their synthesis, which enables functionalization at multiple sites, has been developed. Biological evaluation in enzymatic and cell-based assays has identified a series of C-6 carbamates with potent biochemical and cellular activities.

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Year:  2005        PMID: 16111887     DOI: 10.1016/j.bmcl.2005.07.027

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


  6 in total

1.  Structure-activity relationship of conformationally constrained peptidomimetics for antiproliferative activity in HER2-overexpressing breast cancer cell lines.

Authors:  Sashikanth Banappagari; Sharon Ronald; Seetharama D Satyanarayanajois
Journal:  Medchemcomm       Date:  2011-01-01       Impact factor: 3.597

2.  A conformationally constrained peptidomimetic binds to the extracellular region of HER2 protein.

Authors:  Sashikanth Banappagari; Sharon Ronald; Seetharama D Satyanarayanajois
Journal:  J Biomol Struct Dyn       Date:  2010-12

3.  Design, synthesis, and docking studies of peptidomimetics based on HER2-herceptin binding site with potential antiproliferative activity against breast cancer cell lines.

Authors:  Seetharama Satyanarayanajois; Stephanie Villalba; Liu Jianchao; Go Mei Lin
Journal:  Chem Biol Drug Des       Date:  2009-09       Impact factor: 2.817

4.  Synthesis, molecular structure and characterization of allylic derivatives of 6-amino-3-methyl-1,2,4-triazolo[3,4-f][1,2,4]-triazin-8(7H)-one.

Authors:  Long-Chih Hwang; Shin-Yi Jane; Hsing-Yi Lai; Chun-Hsien Tu; Gene-Hsiang Lee
Journal:  Molecules       Date:  2006-06-22       Impact factor: 4.411

5.  Identifying HER2 inhibitors from natural products database.

Authors:  Shun-Chieh Yang; Su-Sen Chang; Calvin Yu-Chian Chen
Journal:  PLoS One       Date:  2011-12-12       Impact factor: 3.240

6.  Synthetic strategies for pyrrolo[2,1-f][1,2,4]triazine: the parent moiety of antiviral drug remdesivir.

Authors:  Gaurav S Rai; Jayesh J Maru
Journal:  Chem Heterocycl Compd (N Y)       Date:  2021-01-04       Impact factor: 1.277

  6 in total

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