Synthesis and Antitumor Activities of N-hydroxy-5-(3-substituted ureido)-1H-indole-2-carboxamide Derivatives
- VernacularTitle: N-羟基-5-(3-取代脲)-1H-吲哚-2-酰胺衍生物的合成及其抗肿瘤活性研究
- Author:
Rui-Lin GUO
1
Author Information
- Publication Type:Journal Article
- Keywords: Carboxamide derivatives; Indole; Inhibitory activity; Synthesis
- From: Chinese Pharmaceutical Journal 2020;55(15):1234-1242
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To design and synthesize N-hydroxy-5-(3-substituted urea)-1H-indole-2-amide derivatives and investigate their anti-tumor activity in vitro. METHODS: A series of new N-hydroxy-5-(3-substituted ureido)-1H-indole-2-carboxamide derivatives (7a-7n)were designed and prepared from p-nitrophenylhydrazine and ethyl pyruvate. Their antitumor activities against Hela (breast cancer) lines, cervical cancer cell (MCF7) and human hepatoma cell lines (HepG2) were evaluated by methyl thiazolyl (MTT) method. RESULTS: Target compounds indicated certain antitumor activities, especially compound 7h showed the strongest cytotoxicity to Hela cells with a half inhibition concentration (IC50) of 7.31 μmol•L-1. CONCLUSION: The series of compounds show preferable antitumor activities, which are worthy of further study.
