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Bioisostere of valtrate, anti-HIV principle by inhibition for nuclear export of Rev.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tamura S,Shimizu N,Fujiwara K,Kaneko M,Kimura T,Murakami N

doi

10.1016/j.bmcl.2010.02.038

subject

Has Abstract

pub_date

2010-04-01 00:00:00

pages

2159-62

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00238-6

journal_volume

20

pub_type

杂志文章

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