Chemical reactivity of 4-((6-chloro-4-oxo-4H-chromen-3-yl)methylene)-2-phenyloxazol-5(4H)-one towards nitrogen and sulfur nucleophiles, as well as bidentate nucleophiles, has been studied under various conditions. The investigated nucleophilic reactions result in formation of heterocyclic systems, namely pyrazolyloxazolone, pyrazoldihydrotriazinone, chromonylimidazolone, chromonylimidazol, and chromonylbenzo[d]imidazole and chromonyloxathiazepine derivatives. All the synthesized products were screened for their anticancer activity against two cell lines, namely human colon (HCT-116) and mammary gland breast cancer (MCF-7) using the MTT assay. Some of the investigated compounds showed remarkable cytotoxic activities against HCT-116 (IC50 7.74‒82.49 µg/mL) and MCF-7 (IC50 4.98‒92.62 µg/mL) cells in comparison to the standard anticancer drug doxorubicin (IC50 5.23 and 4.17 µg/mL, respectively). Among the tested compounds, pyrazolbenzamide and pyrazoldihydrotriazinone derivatives were the most significant antiproliferative efficacy against the two cell lines. Our findings suggest that the designed compounds may be considered promising antiproliferative agents.

中文翻译：

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基于色酮-吡唑的抗癌剂的开发

4-((6-chloro-4-oxo-4H-chromen-3-yl)methylene)-2-phenyloxazol-5(4H)-one 对氮和硫亲核试剂以及双齿亲核试剂的化学反应性在各种条件下研究。所研究的亲核反应导致杂环系统的形成，即吡唑基恶唑酮、吡唑二氢三嗪酮、色酰咪唑酮、色酰咪唑、色酰苯并[d]咪唑和色酰氧硫氮杂衍生物。使用 MTT 测定筛选所有合成产物对两种细胞系的抗癌活性，即人结肠癌 (HCT-116) 和乳腺乳腺癌 (MCF-7)。一些研究的化合物对 HCT-116 (IC50 7.74-82.49 µg/mL) 和 MCF-7 (IC50 4.98-92) 显示出显着的细胞毒活性。62 µg/mL) 细胞与标准抗癌药物多柔比星（IC50 分别为 5.23 和 4.17 µg/mL）相比。在测试的化合物中，吡唑苯甲酰胺和吡唑二氢三嗪酮衍生物对两种细胞系具有最显着的抗增殖功效。我们的研究结果表明，设计的化合物可能被认为是有前途的抗增殖剂。