Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties.

Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties. Research Abstract Details 

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Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties. Abstract Text:

The causative agent behind adult T-cell leukemia and tropical spastic paraparesis/HTLV-I-associated myelopathy is the human T-cell leukemia virus type 1 (HTLV-I). Tetrapeptidic HTLV-I protease inhibitors were designed on a previously reported potent inhibitor KNI-10516, with modifications at the P(3)-cap moieties. All the inhibitors showed high HIV-1 protease inhibitory activity (over 98% inhibition at 50nM) and most exhibited highly potent inhibition against HTLV-I protease (IC(50) values were less than 100nM).

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Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Bioorganic & medicinal chemistry

VOLUME: 16

Page Numbers: 5795-802

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 1464-3391

DAY: 27

MONTH: 03

YEAR: 2008

Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties. Information

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LANGUAGE: eng

NlmUniqueID: 9413298

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Grant and Affiliation Information for Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties.

AFFILIATION: Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science and 21st Century COE Program, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.

Country: England

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MEDLINETA: Bioorg Med Chem

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