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新型吲哚吡唑、吲哚嗪和吲哚噻吩的合成及其抗癌活性研究。

Novel candidates synthesis of indenopyrazole, indenoazine and indenothiophene, with anticancer and studies.

机构信息

Chemistry Department, College of Sciences, University College of Taraba, Taif University, P. O. Box 11099, Taif, 21944, Saudi Arabia.

Department of Chemistry, Faculty of Science, Zagazig University, Zagazig, 44519, Egypt.

出版信息

Future Med Chem. 2024;16(14):1429-1447. doi: 10.1080/17568919.2024.2351350. Epub 2024 Jun 5.

Abstract

The indandione nucleus, is one of the most amazing nuclei in medicinal chemistry, is used to design new derivatives. Novel indandione derivatives are prepared with different electrophilic and nucleophilic reagents to yield , , , , , and . Compounds and are investigated against OVCAR-3 and HeLa, using LLC-MK2 and -Pt as references. and spectral studies were analyzed for the selected compounds. Compounds and at 100 ns were the most potent compounds, so molecular dynamics studies were performed. Compound was the most active toward the HeLa cervical cell line, and compound was the most active toward the Ovcar-3 cell line.

摘要

茚满二酮核是医学化学中最令人惊叹的核之一,被用于设计新的衍生物。用不同的亲电试剂和亲核试剂制备新型茚满二酮衍生物,得到 、 、 、 、 、 。选用 LLC-MK2 和 -Pt 作为对照物,对化合物 和 进行了 OVCAR-3 和 HeLa 的活性测试。对选定的化合物进行了 和光谱研究。在 100ns 时,化合物 和 是最有效的化合物,因此进行了分子动力学研究。化合物 对宫颈癌细胞系 HeLa 最为活跃,化合物 对 Ovcar-3 细胞系最为活跃。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7fc9/11352785/a372b073ee5a/IFMC_A_2351350_UF0001_C.jpg

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