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新型[(吲哚基)吡唑基]-1,3,4-恶二唑硫代糖苷和无环核苷类似物的合成及其抗癌活性

Synthesis and anticancer activity of new [(Indolyl)pyrazolyl]-1,3,4-oxadiazole thioglycosides and acyclic nucleoside analogs.

作者信息

El-Sayed Wael A, El-Sofany Walaa I, Hussein Hoda A R, Fathy Nahed M

机构信息

a Photochemistry Department , National Research Centre , Dokki , Giza , Egypt.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2017 Jul 3;36(7):474-495. doi: 10.1080/15257770.2017.1327665. Epub 2017 Jun 14.

Abstract

New [(Indolyl)pyrazolyl]-1,3,4-oxadiazole compounds and their derived thioglycosides as well as the corresponding sugar hydrazones were synthesized. The acyclo C-nucleoside analogs of the oxadiazoline base system were also prepared by reaction of acid hydrazides with aldehydo sugars followed by one pot process encompassing acetylation and cyclization of the synthesized hydrazones. The anticancer activity of the newly synthesized compounds was studied against colorectal carcinoma (HCT116), breast adenocarcinoma (MCF7) and prostate cancer (PC3) human tumor cell lines and a number of compounds showed moderate to high activities.

摘要

合成了新型[(吲哚基)吡唑基]-1,3,4-恶二唑化合物及其衍生的硫代糖苷以及相应的糖腙。通过酰肼与醛糖反应,随后经过一锅法进行合成腙的乙酰化和环化反应,还制备了恶二唑啉碱体系的无环C-核苷类似物。研究了新合成化合物对人结肠直肠癌(HCT116)、乳腺腺癌(MCF7)和前列腺癌(PC3)肿瘤细胞系的抗癌活性,许多化合物表现出中度至高活性。

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