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KMID : 0043320080310010001
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Archives of Pharmacal Research
2008 Volume.31 No. 1 p.1 ~ p.5
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Chromone and Chromanone Derivatives as Strand Transfer Inhibitors of HIV-1 Integrase
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Park Jang-Hyun
Lee Seung-Uk
Kim Sang-Hoon
Shin Seo-Yeong
Lee Jae-Yeol
Shin Cha-Gyun
Yoo Kyung-Ho
Lee Yong-Sup
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Abstract
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HIV-1 integrase catalyzes terminal cleavage at the 3’ end of the proviral DNA, removing a pair of bases and causing strand transfer by joining the 3’ end to 5’-phosphates in the target DNA. Several aryl 1,3-diketo acids that can inhibit the strand transfer reaction of HIV-1 IN have been identified. Here we synthesized a new series of compounds with a chromone or chromanone ring as conformationally constrained scaffolds of 1,3-diketo acids, and then tested their ability to inhibit HIV-1 IN-mediated strand transfer. All compounds moderately inhibited HIV-1 IN activity, indicating that the conformational restriction of one keto group into a chromone or chromanone ring decreases inhibition of the HIV-1 IN strand transfer.
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KEYWORD
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HIV-1 integrase inhibitor, Strand transfer, Chromone, Chromanone, Conformationally constrained
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