Synthesis and evaluation of 4-anilinoquinazoline bioisosteres as potential anti-breast cancer agents

  • Eur J Med Chem. 2014 Oct 30:86:202-10. doi: 10.1016/j.ejmech.2014.08.056.
Afaf K El-Ansary  1 Aliaa M Kamal  2 Mokhtar AbdHafiz Al-Ghorafi  1
Affiliations
  • 1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 11561 Cairo, Egypt.
  • 2. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 11561 Cairo, Egypt. Electronic address: [email protected].
Abstract

Based on one of the four major categories of scaffold hopping theory namely hetrocycle replacements, a series of 5-arylthieno[2,3-d]pyrimidines had been prepared and evaluated as anti-breast Cancer agents. Optimization by combination of different pharmacophores with the thienopyrimidine scaffold led to discovery of biologically active compounds.

Keywords
Breast cancer; Cytotoxic activity; Scaffold hopping; Synthesis; Thienopyrimidines.