The design and the preparation of a small library of 1,4-diphenyl-1,2,3-triazole derivatives is reported, with the aim to obtain a new class of Hedgehog pathway inhibitors. The smoothened (SMO) protein is part of the hedgehog signalling pathway that is inhibited by the lead compound Vismodegib. Based on molecular modeling suggestions, seven triazole derivatives of Vismodegib were synthesized and their biological effect on different endothelial, cancer and cancer stem cell lines is reported.
Click reaction as a useful tool to creatively combine pharmacophores : the case of Vismodegib / M.S. Christodoulou, M. Morib, R. Pantanoa, R. Alfonsic, P. Infanteb, M. Bottad, E, G. Damiaf, F. Riccif, P.A. Sotiropouloug, S. Liekensh, B. Bottai, D. Passarella. - In: CHEMPLUSCHEM. - ISSN 2192-6506. - 80:6(2015 Jun), pp. 938-943. [10.1002/cplu.201402435]
Click reaction as a useful tool to creatively combine pharmacophores : the case of Vismodegib
M.S. ChristodoulouPrimo
;D. Passarella
2015
Abstract
The design and the preparation of a small library of 1,4-diphenyl-1,2,3-triazole derivatives is reported, with the aim to obtain a new class of Hedgehog pathway inhibitors. The smoothened (SMO) protein is part of the hedgehog signalling pathway that is inhibited by the lead compound Vismodegib. Based on molecular modeling suggestions, seven triazole derivatives of Vismodegib were synthesized and their biological effect on different endothelial, cancer and cancer stem cell lines is reported.
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