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Design and synthesis of indole derivatives of adenophostin A. A entry into subtype-selective IP3 receptor ligands |
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| Authors: | Tetsuya Mochizuki Akihiro Nezu Hiroshi Abe Mitsuhiro Arisawa |
| Institution: | a Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan b School of Dentistry, Health Sciences University of Hokkaido, Ishikari-Tobetsu 061-0293, Japan c RIKEN, Advanced Science Institute, 2-1, Hirosawa, Wako, Saitama 351-0198, Japan |
| Abstract: | Indole derivatives 3a and 3b of adenophostin A (2) in which the adenine of 2 was replaced with indole or 4-fluoroindole was designed as potential inositol trisphosphate receptor ligands. These target compounds were successfully synthesized from the key disaccharide unit 6. Biological evaluation showed that 3b selectively activates IP3R1, a subtype of IP3 receptors. |
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