Herein, a rapid and highly efficient method for the synthesis of a new series of pyrimidine derivatives was demonstrated. The strategy was emanated from the reaction of hydrazinyl pyrimidine derivative (1) with different electrophilic species such as ethyl acetoacetate, ethyl 4,4,4‐trifluoro acetoacetate, and phenyl isothiocyanate following cyclocondensation mechanism to afford the corresponding derivatives (2‐6). Furthermore, condensation of hydrazine derivative (1) with different carbonyl compounds via conventional heating and microwave irradiation conditions was employed as a source of Schiff base derivatives bearing pyrimidine moiety (7‐12). The structural features of all newly synthesized compounds were characterized by elemental and spectroscopic evidences. Some of the synthesized compounds were evaluated for in vitro cytotoxicity. The preliminary screening results showed that most of the tested compounds have moderate cytotoxic activity against HepG2 and HCT‐116 cell lines. Finally, a molecular docking study was conducted to reveal the probable interaction with the thymidylate synthase enzyme.

中文翻译：

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新型嘧啶衍生物作为潜在抗癌剂的环保合成

在本文中，证明了一种快速高效的合成新系列嘧啶衍生物的方法。该策略是由肼基嘧啶衍生物（1）与不同的亲电物种如乙酰乙酸乙酯，4,4,4-三氟乙酰乙酸乙酯，异硫氰酸苯酯通过环缩合机理反应生成相应的衍生物（2-6）而产生的。此外，通过常规加热和微波辐射条件，将肼衍生物（1）与不同的羰基化合物缩合，用作带有嘧啶部分的席夫碱衍生物的来源（7-12）。所有新合成化合物的结构特征均通过元素和光谱学证据表征。评价了一些合成的化合物的体外细胞毒性。初步筛选结果表明，大多数测试化合物对HepG2和HCT-116细胞系具有中等的细胞毒活性。最后，进行了分子对接研究以揭示与胸苷酸合酶的可能相互作用。