1226896-08-7Relevant academic research and scientific papers
Bioisostere of valtrate, anti-HIV principle by inhibition for nuclear export of Rev
Tamura, Satoru,Shimizu, Nobuhiro,Fujiwara, Katsuaki,Kaneko, Masafumi,Kimura, Tominori,Murakami, Nobutoshi
, p. 2159 - 2162 (2010)
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.
