Abstract

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 μM, 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.

中文翻译：

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多种呋喃[2,3-d]嘧啶和苯并呋喃[3,2-d]嘧啶衍生物的合成及抗癌活性

摘要

合成了一系列不同的呋喃[2,3 - d ]嘧啶（2a-2b、4a-4d和8a-8c）和苯并呋喃[3,2 - d ]嘧啶（12a-12c）并筛选了它们的抗肿瘤作用体外HepG2、Bel-7402 和 HeLa 细胞系。具有代表性的是，IC _{50为 0.70 μM 的}4a对测试的 HepG2 细胞系表现出最佳的抗肿瘤活性。分子对接研究进一步揭示了化合物4a可能的结合模式与受体酪氨酸激酶。初步结果表明，标题化合物作为主要结构有助于制备新的抗肿瘤药物。