Bioisostere of valtrate,anti-HIV principle by inhibition for nuclear export of Rev |
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| Authors: | Satoru Tamura Nobuhiro Shimizu Katsuaki Fujiwara Masafumi Kaneko Tominori Kimura Nobutoshi Murakami |
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| Institution: | 1. Graduate School of Pharmaceutical Sciences, Osaka University, 1-6 Yamada-oka, Suita, Osaka 565-0871, Japan;2. PRESTO, Japan Science and Technology Agency (JST), 4-1-8 Honcho, Kawaguchi, Saitama 332-0012, Japan;3. College of Pharmaceutical Sciences, Ritsumeikan University, 1-1-1 Noji Higashi, Kusatsu, Shiga 525-8577, Japan;4. Kansai Medical University, 10-15 Fumizono-cho, Moriguchi, Osaka 570-8506, Japan |
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| Abstract: | Rational design by the MO calculation disclosed 5,6-dihydrovaltrate (2) as the bioisostere of valtrate (1), the Rev-export inhibitor with anti-HIV activity. The synthesis of 2 was accomplished by ingenious use of asymmetric Diels–Alder reaction and stereoselective epoxidation associated with the adjacent hydroxyl group. Because of similar biological potency to 1, the analog 2 should be recognized as a promising scaffold for new anti-HIV agents with an unprecedented mechanism of action, inhibition for nuclear export of Rev protein, in the conventional remedy. |
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