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

•This work highlights the synthesis of a series of novel thieno[2,3-d]pyrimidines as anticancer agents.•Screening the target compounds against the human breast tumor cell line (MCF-7) was carried out.•Two out of the goal compounds shown displayed twice the potency of lapatinib.

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.

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