Daria Zakopailo, Yevhen Blashchak, Mykola Тupychak, Nataliya Finiuk, Nazariy Pokhodylo
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引用次数: 0
摘要
以1h -1,2,3-三唑-4-羧酸为起始原料,在POCl₃的作用下,经酰化、闭环等多步合成(1h -1,2,3-三唑-4-基)-1,2,4-三唑嗪衍生物。对标题化合物进行了细胞毒性测试,包括A549人肺癌、HCT116结肠癌、Jurkat t -白血病和KB3-1人宫颈癌。这些化合物表现出不同程度的活性,其中一些显示出强大的细胞毒性作用,特别是对人类肺癌A549和人类白血病Jurkat t细胞。结果表明,环闭合显著影响化合物的生物活性,增强其细胞毒性。该研究表明,(1h -1,2,3-三唑-4-酰基)-1,2,4-三唑嗪衍生物作为癌症治疗的有希望的候选者,特别是那些具有特定取代基模式的衍生物,可以增强其抗增殖作用。
Design and synthesis of novel 1H-1,2,3-triazolecarbohydrazides and 1,2,4-triazoloazines based on them for anticancer drug discovery
The synthesis of (1H-1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives was achieved via a multi-step synthesis starting from 1H-1,2,3-triazole-4-carboxylic acids, followed by acylation and ring closure under the influence of POCl₃. The title compounds were tested for cytotoxicity against a range of cancer cell lines, including A549 human lung carcinoma, HCT116 colon carcinoma, Jurkat T-leukemia, and KB3-1 human cervical carcinoma. The compounds demonstrated varying degrees of activity, with several showing potent cytotoxic effects, particularly against human lung carcinoma A549 and human leukemia Jurkat T-cells. The results suggest that ring closure significantly influences the bioactivity of the compounds, enhancing their cytotoxic properties. The study indicates the potential of (1H-1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives as promising candidates for cancer therapy, especially those with specific substituent patterns that enhance their antiproliferative effects.
期刊介绍:
Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.