In this work, 21 novel (1,4-disubstituted 1,2,3-triazole)-dihydropyrimidinone (1,2,3-trzl-DHPM) type hybrids were synthesized and characterized. These were divided into two types: hybrids A (5 in total) containing the dihydropyrimidinone heterocyclic ring decorated with a 1,4-disubstituted 1,2,3-triazole in the C-5 position [these compounds were accessed by a multicomponent copper(I)-catalyzed azide alkyne cycloaddition (CuAAC) (or click)–Biginelli reactions with satisfactory yields (39–57%)] and hybrids B (16 in total) containing two 1,2,3-triazole units in the C-5 and C-6 methyl position of the DHPM. Hybrids B were synthesized via functionalization of the C-6 methyl group of hybrids A, a multistep sequence of reactions was used that included bromination, azidation, and a CuAAC. Hybrids B were obtained in very good to excellent yields (up to 99%). Some hybrids A and B were evaluated for their antiproliferative activity against different cancer cell lines that included A549 and SW1573 (non-small-cell lung), HBL-100 and T-47D (breast), HeLa (cervix) and WiDr (colon). Three of these hybrids were potent cell proliferation inhibitors of non-small-cell lung cancer, cervix cancer, breast cancer, and colon cancer.

中文翻译：

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使用多组分 1,3-偶极环加成 (Click)-Biginelli 反应合成新型 1,2,3-三唑-二氢嘧啶酮杂化物：抗癌活性

在这项工作中，合成并表征了 21 种新型 (1,4-二取代 1,2,3-三唑)-二氢嘧啶酮 (1,2,3-trzl-DHPM) 型杂化物。它们分为两种类型：杂化物 A（总共 5 个）包含在 C-5 位置装饰有 1,4-二取代 1,2,3-三唑的二氢嘧啶酮杂环 [这些化合物通过多组分铜（ I)-催化叠氮炔环加成 (CuAAC)（或点击）-Biginelli 反应，产率令人满意（39-57%）] 和杂化物 B（共 16 个）在 C-5 中包含两个 1,2,3-三唑单元DHPM 的 C-6 甲基位置。杂化物 B 通过杂化物 A 的 C-6 甲基的官能化合成，使用多步反应序列，包括溴化、叠氮化和 CuAAC。以非常好到极好的产量（高达 99%）获得了杂种 B。评估了一些杂交种 A 和 B 对不同癌细胞系的抗增殖活性，包括 A549 和 SW1573（非小细胞肺）、HBL-100 和 T-47D（乳腺）、HeLa（宫颈）和 WiDr（结肠） . 其中三种杂交体是非小细胞肺癌、宫颈癌、乳腺癌和结肠癌的有效细胞增殖抑制剂。