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新型 2-(芳基亚氨基)-3-甲基-1-苯并吲哚衍生物的合成及细胞毒性活性研究。

Synthesis and Cytotoxic Activity Study of Novel 2-(Aryldiazenyl)-3-methyl-1-benzo[]indole Derivatives.

机构信息

Faculty of Pharmacy, Middle East University, Amman 11831, Jordan.

Chemistry Department, College of Science, Sultan Qaboos University, Muscat 123, Oman.

出版信息

Molecules. 2021 Jul 12;26(14):4240. doi: 10.3390/molecules26144240.

Abstract

A novel series of 2-(aryldiazenyl)-3-methyl-1-benzo[]indole derivatives (-) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (-) were characterized using H NMR, C NMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 µM concentration, two of them () and () were subjected to five dose screens and showed a significant cytotoxicity and selectivity.

摘要

通过相应芳基腙的环化反应,使用多聚磷酸(PPA)作为环化试剂,合成了一系列新型的 2-(芳基亚氨基)-3-甲基-1-苯并[]吲哚衍生物(-)。所有化合物(-)均通过 1H NMR、13C NMR、MS、元素分析和熔点技术进行了表征。通过国家癌症研究所,用合成的化合物对多种人癌细胞系进行了细胞毒性活性筛选。虽然所有筛选的化合物在 10 μM 浓度下都显示出细胞毒性,但其中两种()和()进行了 5 个剂量筛选,显示出显著的细胞毒性和选择性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e6/8306180/b5ef38225025/molecules-26-04240-sch001.jpg

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