Synthesis of 3-nicotinamide-1, 2, 4-benzotriazine-1, 4-dioxide and the determination of its anti-tumor activity in vitro
- Author:
Rui DING
1
Author Information
1. Anhui Medical College
- Publication Type:Journal Article
- Keywords:
3-nicotinamide-1, 2, 4-benzotriazine-1, 4-dioxide;
Anti-tumor activity;
Tirapazamine
- From:
Chinese Pharmaceutical Journal
2012;47(8):639-641
- CountryChina
- Language:Chinese
-
Abstract:
To synthesize 3-nicotinamide-1, 2, 4-benzotriazine-1, 4-dioxide and to determine its anti-tumor activity in vitro. METHODS: Cyanogenamide and benzofuroxan were used as starting materials to prepare the intermediate (3-amino-1, 2, 4-benzotriazine-1, 4-dioxide, Tirapazamine). The objective substance was obtained from the reaction of the intermediate and nicotinic acyl chloride. The in vitro antitumor activities of the synthesized compounds were determined by MTT method using MCF-7 and HepG2 cells. RESULTS: The obtained compounds were identified by 1H-NMR, MS and IR. The purity of the objective substance determined by HPLC was 99.24%. CONCLUSION: The anti-tumor activity of 3-nicotinamide-1, 2, 4-benzotriazine-1, 4-dioxide is much better than tirapazamine. Copyright 2012 by the Chinese Pharmaceutical Association.