Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Masaaki Sawa; Kiriko Kurokawa; Yoshimasa Inoue; Hirosato Kondo; Kohichiro Yoshino

doi:10.1016/S0960-894X(03)00292-0

Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Masaaki Sawa, Kiriko Kurokawa, Yoshimasa Inoue, Hirosato Kondo, Kohichiro Yoshino

Research output: Contribution to journal › Article › peer-review

19 Citations (Scopus)

Abstract

A novel series of phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE) was discovered by structural modification of tetrahydroisoquinoline derivative 1b, which was extremely weak inhibitor of TACE. (S)-Isomer at the phosphorus atom (7b) displayed potent inhibition for TACE, while selectivity sparing MMP-1, -3, and -9.

Original language	English
Pages (from-to)	2021-2024
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	13
Issue number	12
DOIs	https://doi.org/10.1016/S0960-894X(03)00292-0
Publication status	Published - Jun 16 2003
Externally published	Yes

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(03)00292-0

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author = "Masaaki Sawa and Kiriko Kurokawa and Yoshimasa Inoue and Hirosato Kondo and Kohichiro Yoshino",

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AU - Sawa, Masaaki

AU - Kurokawa, Kiriko

AU - Inoue, Yoshimasa

AU - Kondo, Hirosato

AU - Yoshino, Kohichiro

PY - 2003/6/16

Y1 - 2003/6/16

N2 - A novel series of phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE) was discovered by structural modification of tetrahydroisoquinoline derivative 1b, which was extremely weak inhibitor of TACE. (S)-Isomer at the phosphorus atom (7b) displayed potent inhibition for TACE, while selectivity sparing MMP-1, -3, and -9.

AB - A novel series of phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE) was discovered by structural modification of tetrahydroisoquinoline derivative 1b, which was extremely weak inhibitor of TACE. (S)-Isomer at the phosphorus atom (7b) displayed potent inhibition for TACE, while selectivity sparing MMP-1, -3, and -9.

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DO - 10.1016/S0960-894X(03)00292-0

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 12

ER -

Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Abstract

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