Design, synthesis, and biological evaluation of bifunctional thyrointegrin inhibitors: new anti-angiogenesis analogs

A Bridoux, RA Khan, C Chen, G Chevé…

Index: Bridoux, Alexandre; Khan, Riaz A.; Chen, Celei; Cheve, Gwenael; Cui, Huadong; Dyskin, Evgeny; Yasri, Aziz; Mousa, Shaker A. Journal of Enzyme Inhibition and Medicinal Chemistry, 2011 , vol. 26, # 6 p. 871 - 882

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Abstract

Context: Inhibition of pathological angiogenesis. Objective: Obtaining new transactivator, bifunctional, thyroid antagonist, non-toxic anti-angiogenic compounds. Materials and methods: In silico drug design, synthesis in bulk and biological evaluation in chick chorioallantoic membrane (CAM) model. Results: Significant inhibition (range 65–73%) at 0.25–2.0 µg/ml doses. Discussion and conclusion: The synthesis of compounds (9),(10), ...