7-Substituted-[1,4]dioxano[2,3-g]quinazolines as inhibitors of epidermal growth factor receptor kinase

Arch Pharm (Weinheim). 2002 Dec;335(10):487-94. doi: 10.1002/ardp.200290003.

Abstract

With the aim of developing inhibitors of EGFR tyrosine kinase, the 7-methoxymethyl-[1,4]dioxano[2,3-g]quinazolines (3a-b) and 7-mono- or di-alkylaminomethyl-[1,4]dioxano[2,3-g]quinazolines (4a-i) were prepared and evaluated for the inhibition of EGFR tyrosine kinase and the growth inhibition of human tumor cell lines. Among them, compounds 4d and 4h showed potencies against both EGFR tyrosine and the A431 cell line similar to that of PD153035 with greater aqueous solubilities of their HCl salts.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / physiology
  • Humans
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology
  • Structure-Activity Relationship
  • Tumor Cells, Cultured / drug effects

Substances

  • Quinazolines
  • ErbB Receptors