当前位置: X-MOL 学术J. Heterocycl. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis of tricyclic pyrazolopyrimidine arylidene ester derivatives and their cytotoxic and molecular docking evaluations
Journal of Heterocyclic Chemistry ( IF 2.4 ) Pub Date : 2024-02-14 , DOI: 10.1002/jhet.4791
Tong Lu 1, 2 , Lifei Nie 1 , Dan Tang 1 , Khurshed Bozorov 1, 3 , Jiangyu Zhao 1, 2 , Haji Akber Aisa 1, 2, 4
Affiliation  

Our research team has synthesized 33 tricyclic pyrazolopyrimidine arylidene ester derivatives using the lead compound CAM551 as a starting point. This was achieved by a designed five-step synthesis strategy. The synthesized compounds' inhibitory activities against HT-116 human colorectal adenocarcinoma cell line and HGC27 human gastric cancer cells were assessed through traditional MTT assays. The designed and synthesized compounds demonstrated superior inhibition against both types of cancer cells. Additionally, compound 7b, which contains a long-chain substituent, exhibited improved inhibition against hepatocellular carcinoma cells and a greater safety profile. These findings indicate that compound 7b has the potential as an antitumor lead compound for future research.

中文翻译:

三环吡唑并嘧啶亚芳基酯衍生物的合成及其细胞毒性和分子对接评价

我们的研究团队以先导化合物CAM551为起点,合成了33种三环吡唑并嘧啶亚芳基酯衍生物。这是通过设计的五步合成策略实现的。通过传统MTT法评估合成化合物对HT-116人结直肠腺癌细胞系和HGC27人胃癌细胞的抑制活性。设计和合成的化合物对两种类型的癌细胞均表现出优异的抑制作用。此外,含有长链取代基的化合物7b表现出改善的对肝细胞癌细胞的抑制作用和更高的安全性。这些发现表明化合物7b有潜力作为未来研究的抗肿瘤先导化合物。
更新日期:2024-02-14
down
wechat
bug