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: Aliaa.kamal@pharma.cu.edu.eg.

PMID: 25151582 DOI: 10.1016/j.ejmech.2014.08.056

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.

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