304452-55-9Relevant articles and documents
Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo
Vesci, Loredana,Milazzo, Ferdinando Maria,Stasi, Maria Antonietta,Pace, Silvia,Manera, Francesco,Tallarico, Carlo,Cini, Elena,Petricci, Elena,Manetti, Fabrizio,De Santis, Rita,Giannini, Giuseppe
, p. 368 - 379 (2018/08/17)
Small series of acylguanidine and acylthiourea derivatives were synthesized in gram-scale and assayed for their ability to modulate the Hh signalling pathway. In vitro studies showed a low micromolar inhibitory activity toward tumor cell lines, while the oral administration revealed an excellent ADME profile in vivo. Compound 5 emerged as the most active and safe inhibitor of colon cancer cells both in vitro and in a xenograft mouse model. Based on these data, 5 could be prioritized to further development with the perspective of clinical studies.
Acyl Guanidine Derivatives Modulating The Hedgehog Protein Signaling Pathway
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Page/Page column 16, (2012/08/08)
The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.