Synthesis and Enantiomeric Separation of a Novel Spiroketal derivative: A Potent Human Telomerase Inhibitor with High In Vitro Anticancer Activity(430 views) Fuggetta MP, De Mico A, Cottarelli A, Morelli F, Zonfrillo M, Ulgheri F, Peluso P, Mannu A, Deligia F, Marchetti M, Roviello GN, Romero AR, Dömling A, Spanu P
Journal Of Medicinal Chemistry, 2016 Mar; 59: 9140-9149.
Synthesis and Enantiomeric Separation of a Novel Spiroketal derivative: A Potent Human Telomerase Inhibitor with High In Vitro Anticancer Activity
The synthesis, the enantiomeric separation and the characterization of new simple spiroketal derivatives has been performed. The synthesised compounds have shown a very high anticancer activity. Cell proliferation assay showed that they induce a remarkable inhibition of cell proliferation in all cell lines treated, depending on culture time and concentration. The compounds have also shown a potent nanomolar human Telomerase inhibition activity and apoptosis induction. CD melting experiments demonstrate that spiroketal does not affect the G-quadruplex (G4) thermal stability. Docking studies showed that telomerase inhibition could be determined by a spiroketal interaction with the telomerase enzyme.
Synthesis and Enantiomeric Separation of a Novel Spiroketal derivative: A Potent Human Telomerase Inhibitor with High In Vitro Anticancer Activity
Testino G, Leone S, Fagoonee S, Del Bas JM, Rodriguez B, Puiggros F, Marine S, Rodriguez MA, Morina D, Armengol L, Caimari A, Arola L, Cimini FA, Barchetta I, Carotti S, Bertoccini L, Baroni MG, Vespasiani-gentilucci U, Cavallo MG, Morini S, Nelson JE, Roth CL, Wilson LA, Yates KP, Aouizerat B, Morgan-stevenson V, Whalen E, Hoofnagle A, Mason M, Gersuk V, Yeh MM, Kowdley KV, Lee SM, Jun DW, Cho YK, Jang KS, Kucukazman M, Ata N, Dal K, Yeniova AO, Kefeli A, Basyigit S, Aktas B, Akin KO, Agladioglu K, Ure OS, Topal F, Nazligul Y, Beyan E, Ertugrul DT, Catena C, Cosma C, Camozzi V, Plebani M, Ermani M, Sechi LA, Fallo F, Goto Y, Ray MB, Mendenhall CL, French SW, Gartside PS Serum vitamin A deficiency and increased intrahepatic expression of cytokeratin antigen in alcoholic liver disease(707 views) Hepatology (ISSN: 1827-1669electronic, 0026-4806linking), 1988 Sep; 83120693611123109(5): 1019-1026. Impact Factor:0.913 ViewExport to BibTeXExport to EndNote