Structure-Based Design of erbB-2 Selective Small Molecule Kinase Inhibitors

Abstract

Our studies in the first two years have led to the identification of a number of promising "lead" compounds. Among these initial lead compounds, B-17 has excellent activity in inhibition of erbB-2 auto-phosphorylation and inhibition of cell proliferation using MDA-453 human breast cancer cells with erbB-2 overexpression. Furthermore, this compound appears to also be quite selective of breast cancer cells and model cells with EGFR overexpression but not erbB-2 overexpression (see below). Accordingly, B-17 represents a quite promising lead compound for further modifications.

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Document Details

Document Type
Technical Report
Publication Date
Jul 01, 2003
Accession Number
ADA419538

Entities

People

  • Shaomeng Wang

Organizations

  • University of Michigan

Tags

DTIC Thesaurus Topics

  • Abstracts
  • Analogs
  • Biomedical Research
  • Body Weight
  • Breast Cancer
  • Cell Line
  • Cells
  • Electronic Mail
  • Inhibition
  • Inhibitors
  • Kinases
  • Lead Compounds
  • Michigan
  • Molecules
  • Neoplasms
  • Proteins
  • Small Molecules

Fields of Study

  • Chemistry

Readers

  • Breast cancer cell signaling and growth regulation.