Synthesis of Substituted Thieno[2,3‐<i>d</i>]pyrimidin‐4‐ones and Their Testing for Evaluation of Cytotoxic Activity on Mammalian Cell Models

Abstract

From 2‐amino‐3‐ethoxycarbonyl‐4,5‐dimethyl‐, ‐polymethylenethiophenes ( 1-4 ) were synthesized 2,3‐disubstituted thieno[2,3‐d]dihydropyrrolo‐, tetrahydropyrido‐, and tetrahydroazepino[1,2‐a]pyrimidin‐4‐ones ( 5-16 ) for pharmacological investigations. The 12 compounds ( 5-16 ) were individually evaluated for their antiproliferative activities on mammalian cancer cell models. All tested compounds showed weak affection on human cervix adenocarcinoma cells (HeLa) whereas some of the tested compounds exhibited more consistent inhibition of cell growth on murine myeloma cells (P3X). In both cases some compounds enhanced cell proliferation.