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ID: ALA4270604
Journal: Eur J Med Chem
Title: Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo.
Authors: Vesci L, Milazzo FM, Stasi MA, Pace S, Manera F, Tallarico C, Cini E, Petricci E, Manetti F, De Santis R, Giannini G.
Abstract: 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.
CiteXplore: 30099257