Abstract

Synthesis and anticancer evaluation of some fused coumarino-[3, 4-d]�?�?pyrimidine derivatives

Author(s): M.H.Sherif, Amal M.Yossef

7,9-Disubstrtuted-2-amino-4-hydroxy-5H-[1]- benzopyrano-[4, 3-d]- pyrimidines (3a,b) were prepared via cyclocondensation of 6, 8-disubstituted-3-ethoxycarbonyl coumarin (2) with guanidine hydrochloride in presence of anhydrous potassium carbonate. Acetylation and alkylation of compounds with acetic anhydride and - bromomethyl aryl ketones yielded the corresponding N-acetyl derivatives (4a,b) and substituted benzopyrano- [4,3-d]-imidazolidino-[2,1-b]-pyrimidines (5a,b). Treatment of compound (3a) with ethylchloroacetate andmethyl acrylate afforded the corresponding benzopyrano-[4, 3-d]-imidazolidino- [2, 1-b]-pyrimidine (6) and benzopyrano- [4, 3-d]-pyrimidino-[2,1-b]-pyrimidine (7), respectively. Some of the newcompounds were evaluated for cytotoxicity activity against hepatocellular carcinoma cell line (HepG2).