Studies on the chemical transformations of rotenoids. 6 Synthesis and antitumor-promoting activity of benzofuro[2,3-d]pyridazines fused with 1,2,4-triazole, 1,2,4-triazine and 1,2,4-triazepine
✍ Scribed by Shin-Ichi Nagai; Satoshi Takemoto; Taisei Ueda; Kanako Mizutani; Yasuhiro Uozumi; Harukuni Tokuda
- Publisher
- Journal of Heterocyclic Chemistry
- Year
- 2001
- Tongue
- English
- Weight
- 57 KB
- Volume
- 38
- Category
- Article
- ISSN
- 0022-152X
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✦ Synopsis
Abstract
[1]Benzofuro[2,3‐d]pyridazines fused with 1,2,4‐triazole (6 and 7), 1,2,4‐triazine (8–10) and 1,2,4‐tri‐azepine (12) were prepared by the ring closure of 4‐hydrazino‐[1]benzofuro[2,3‐d]pyridazine (5), derived from naturally occurring rotenone. Compounds (la and lb) exhibited significant inhibitory activity against 12‐O‐tetradecanoylphorbol 13‐acetate (TPA)‐induced Epstein‐Barr virus early antigen (EBA‐EA) activation in Raji cells. In contrast, the fused [1]benzofuro[2,3‐d]pyridazines except 6c and 8 were quite inactive.
📜 SIMILAR VOLUMES
## Abstract 5,8‐Methanoquinazolines fused with 1,2,4‐triazole 4–5, tetrazole 6, and 1,2,4‐triazine 8 were prepared starting from 2‐hydrazino‐5,8‐methanoquinazoline 3. Compound 3 and 6 showed the most potent central nervous system (CNS) stimulant activities.