Design, synthesis, and antiproliferative activity of novel 1,2,4-triazole-chalcone compounds

IF 1.3 3区 化学 Q3 CHEMISTRY, ORGANIC Heterocyclic Communications Pub Date : 2023-01-01 DOI:10.1515/hc-2022-0165
Jinjing Li, Pingping Fan, Yuxiao Liu, Yan Zhao, Chengyang Shi, Shujing Zhou, Hongbin Qiu
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Abstract

Abstract A series of novel 1,2,4-triazole-chalcone compounds 10a–10s were designed by molecular hybridization strategy and synthesized. The molecular structures of the novel chalcones were characterized by 1 H-NMR, 13 C-NMR, and HRMS. The anti-proliferative activities of the novel chalcones against four cancer cell lines in vitro were examined by MTT, four tumor cell lines including human colon cancer cell SW620, human non-small cell lung cancer cell A549, human cervical cancer cell HeLa, and human breast cancer cell MCF-7. Compound 10o showed certain selectivity to SW620 cell line, and its IC 50 value was 21.55 μM. 10q had good anti-proliferative activity against A549 cells with an IC 50 value of 25.58 μM.
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新型1,2,4-三唑-查尔酮化合物的设计、合成及其抗增殖活性
摘要采用分子杂交策略设计并合成了一系列新的1,2,4-三唑-查尔酮化合物10a-10s。通过1h - nmr、13c - nmr和HRMS表征了新查尔酮的分子结构。MTT法检测了新型查尔酮对4种肿瘤细胞系(人结肠癌细胞SW620、人非小细胞肺癌细胞A549、人宫颈癌细胞HeLa、人乳腺癌细胞MCF-7)的体外抗增殖活性。化合物100对SW620细胞株有一定的选择性,其ic50值为21.55 μM。10q对A549细胞具有良好的抗增殖活性,ic50值为25.58 μM。
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来源期刊
Heterocyclic Communications
Heterocyclic Communications 化学-有机化学
CiteScore
3.80
自引率
4.30%
发文量
13
审稿时长
1.4 months
期刊介绍: Heterocyclic Communications (HC) is a bimonthly, peer-reviewed journal publishing preliminary communications, research articles, and reviews on significant developments in all phases of heterocyclic chemistry, including general synthesis, natural products, computational analysis, considerable biological activity and inorganic ring systems. Clear presentation of experimental and computational data is strongly emphasized. Heterocyclic chemistry is a rapidly growing field. By some estimates original research papers in heterocyclic chemistry have increased to more than 60% of the current organic chemistry literature published. This explosive growth is even greater when considering heterocyclic research published in materials science, physical, biophysical, analytical, bioorganic, pharmaceutical, medicinal and natural products journals. There is a need, therefore, for a journal dedicated explicitly to heterocyclic chemistry and the properties of heterocyclic compounds.
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