European Journal of Medicinal Chemistry p. 368 - 379 (2018)
Update date:2022-08-04
Topics:
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
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.
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