Synthesis and Anti-Angiogenic Activity of Cortistatin Analogs

Yuuki SATO; Hiroshi KAMIYAMA; Takeo USUI; Tamio SAITO; Hiroyuki OSADA; Shigefumi KUWAHARA; Hiromasa KIYOTA

doi:10.1271/bbb.80562

Organic Chemistry Regular Papers

Synthesis and Anti-Angiogenic Activity of Cortistatin Analogs

Yuuki SATO, Hiroshi KAMIYAMA, Takeo USUI, Tamio SAITO, Hiroyuki OSADA, Shigefumi KUWAHARA, Hiromasa KIYOTA

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Keywords: Cortisium simplex, cortistatin A, synthesis, HUVEC, angiogenesis

JOURNAL FREE ACCESS

2008 Volume 72 Issue 11 Pages 2992-2997

DOI https://doi.org/10.1271/bbb.80562

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Abstract

Analogs of cortistatins, a series of anti-angiogenic compounds isolated from the Indonesian marine sponge Cortisium simplex, were synthesized from estrone by using the Suzuki-Miyaura coupling reaction as the key step. The estrone-isoquinoline hybridized compound showed selective inhibitory activity against the proliferation and VEGF-induced migration of HUVEC.

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