Synthesis and Anticancer Activities of Diverse Furo[2,3-D]pyrimidine and Benzofuro[3,2-D]pyrimidine Derivatives

A series of diverse furo[2,3-d]pyrimidines (2a-2b, 4a-4d and 8a-8c) and benzofuro[3,2-d]pyrimidines (12a-12c) were synthesized and screened for their antitumor effects against HepG2, Bel-7402 and HeLa cell lines in vitro. Representatively, 4a, with an IC50 of 0.70 mu M, exhibited the best antitumor activity against the tested HepG2 cell lines. Molecular docking investigation further revealed the possible binding modes of compound 4a with receptor tyrosine kinase. Preliminary results indicated that the title compounds were helpful as leading structures for preparing a new antitumor drug.