Abstract A new series of 2,5-regioselective benzofuran-tetrazole hybrids ( XIIIa – XIIIp ) were synthesised from 2 H -chromene-3-carbonitriles ( IXa ), ( IXb ) in multi steps approach under mild reaction conditions in good yields and evaluated their anti-proliferative activity against HCT116 and Miapaca2 cell lines. Wherein compounds ( XIIIe ) (IC 50 : 3.19 μM) and ( XIIIm ) (IC 50 : 2.25 μM) were displayed highest anti-proliferative activity in both cell lines. Molecular docking and SAR studies revealed the in vitro results with target Proto-oncogene tyrosine kinase Src protein.

中文翻译：

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新型 2-取代-苄基-5-(2-甲基苯并呋喃-3-基)-2H-四唑的设计与合成：抗增殖活性

摘要 以 2 H-色烯-3-甲腈 (IXa), (IXb ) 为原料，在温和的反应条件下以多步法合成了一系列新的 2,5-区域选择性苯并呋喃-四唑杂化物 (XIIIa – XIIIp ) 并进行了评价。它们对 HCT116 和 Miapaca2 细胞系的抗增殖活性。其中化合物 ( XIIIe ) (IC 50 : 3.19 μM) 和 ( XIIIm ) (IC 50 : 2.25 μM) 在两种细胞系中均显示出最高的抗增殖活性。分子对接和 SAR 研究揭示了靶原癌基因酪氨酸激酶 Src 蛋白的体外结果。