Synthesis and Enantiomeric Separation of a Novel Spiroketal derivative: A Potent Human Telomerase Inhibitor with High In Vitro Anticancer Activity(295 views visite) 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.
Keywords Parole chiave: Not available. Non disponibili.
Affiliations Affiliazioni: *** IBB - CNR ***
References Riferimenti: Not available. Non disponibili.
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
Vitiello M, Finamore E, Falanga A, Raieta K, Cantisani M, Galdiero F, Pedone C, Galdiero M, Galdiero S * Fusion in Coq(399 visite) Lecture Notes In Computer Science (ISSN: 0302-9743, 0302-974335404636319783540463634, 0302-974335402975459783540297543), 2001; 2178LNCS: 583-596. Impact Factor:0.415 DettagliEsporta in BibTeXEsporta in EndNote
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(433 visite) Hepatology (ISSN: 1827-1669electronic, 0026-4806linking), 1988 Sep; 83120693611123109(5): 1019-1026. Impact Factor:0.913 DettagliEsporta in BibTeXEsporta in EndNote
817 Records (769 escludendo Abstract e Conferenze). Impact factor totale: 2970.039 (2828.337 escludendo Abstract e Conferenze). Impact factor a 5 anni totale: 3052.099 (2898.893 escludendo Abstract e Conferenze).
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