Semisynthesis and pharmacological activities of thyroxine analogs: Development of new angiogenesis modulators

Bridoux, Alexandre; Cui, Huadong; Dyskin, Evgeny; Schmitzer, Andreea-Ruxandra; Yalcin, MURAT; Mousa, Shaker

doi:10.1016/j.bmcl.2010.04.011

Semisynthesis and pharmacological activities of thyroxine analogs: Development of new angiogenesis modulators

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Bridoux A., Cui H., Dyskin E., Schmitzer A., Yalcin M., Mousa S. A.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol.20, no.11, pp.3394-3398, 2010 (SCI-Expanded)

Publication Type: Article / Article
Volume: 20 Issue: 11
Publication Date: 2010
Doi Number: 10.1016/j.bmcl.2010.04.011
Journal Name: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
Page Numbers: pp.3394-3398
Keywords: Thyroxine, Esterification, Silylation, UV-vis, Angiogenesis, Nanopharmaceutical technology, EXTRACELLULAR SEGMENT, CRYSTAL-STRUCTURE, THYROID-HORMONE, FORCE-FIELD, PROTEINS
Bursa Uludag University Affiliated: Yes

Abstract

Novel thyroxine analogs with hindered phenol, amino and carboxylic acid groups have been synthesized and the effects of the synthesized compounds on angiogenesis using the chick chorioallantoic membrane and mouse matrigel models have been tested. Pharmacological profiles revealed that thyroxine tolerates numerous modifications on the amino group and remains active. These results provide the rationale for the selection of a novel thyroxine nanoparticle precursor. (C) 2010 Elsevier Ltd. All rights reserved.