Design, Synthesis, and Antiangiogenic Effects of a Series of Potent Novel Fumagillin Analogues

Hong Woo Lee; Chin Sung Cho; Sung Kwon Kang; Yong Sang Yoo; Jae Soo Shin; Soon Kil Ahn

doi:10.1248/cpb.55.1024

Regular Articles

Design, Synthesis, and Antiangiogenic Effects of a Series of Potent Novel Fumagillin Analogues

Hong Woo Lee, Chin Sung Cho, Sung Kwon Kang, Yong Sang Yoo, Jae Soo Shin, Soon Kil Ahn

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Keywords: Aspergillus fumigatus, semisynthesis, hydroxyethoxycinnamoyl fumagillol derivative, antiangiogenic activity, TNP-470

JOURNAL FREE ACCESS

2007 Volume 55 Issue 7 Pages 1024-1029

DOI https://doi.org/10.1248/cpb.55.1024

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Abstract

A series of fumagillin analogues containing the C6-substituted cinnamoyl moiety were designed, synthesized, and evaluated for antiangiogenic activity. Among them, 4-hydroxyethoxy-cinnamoyl fumagillol (4a) and 4-hydroxyethoxy-3,5-dimethoxycinnamoyl fumagillol (4d) exhibited more potent anti-proliferation activity in CPAE and HUVEC cells with low cytotoxicity in vitro. These compounds are presently under further pharmacological evaluation studies.

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