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Items: 26

1.

N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.

Muraglia E, Ontoria JM, Branca D, Dessole G, Bresciani A, Fonsi M, Giuliano C, Llauger Bufi L, Monteagudo E, Palumbi MC, Torrisi C, Rowley M, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5283-8. doi: 10.1016/j.bmcl.2011.07.030. Epub 2011 Jul 14.

PMID:
21802943
2.

Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).

Pescatore G, Branca D, Fiore F, Kinzel O, Bufi LL, Muraglia E, Orvieto F, Rowley M, Toniatti C, Torrisi C, Jones P.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1094-9. doi: 10.1016/j.bmcl.2009.12.026. Epub 2009 Dec 6.

PMID:
20031401
3.

Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.

Ferrigno F, Branca D, Kinzel O, Lillini S, Llauger Bufi L, Monteagudo E, Muraglia E, Rowley M, Schultz-Fademrecht C, Toniatti C, Torrisi C, Jones P.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1100-5. doi: 10.1016/j.bmcl.2009.11.087. Epub 2009 Nov 22.

PMID:
20022747
4.

Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.

Ontoria JM, Altamura S, Di Marco A, Ferrigno F, Laufer R, Muraglia E, Palumbi MC, Rowley M, Scarpelli R, Schultz-Fademrecht C, Serafini S, Steinkühler C, Jones P.

J Med Chem. 2009 Nov 12;52(21):6782-9. doi: 10.1021/jm900555u.

PMID:
19888759
5.

Dihydroxy-pyrimidine and N-methylpyrimidone HIV-integrase inhibitors: improving cell based activity by the quaternarization of a chiral center.

Nizi E, Orsale MV, Crescenzi B, Pescatore G, Muraglia E, Alfieri A, Gardelli C, Spieser SA, Summa V.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4617-21. doi: 10.1016/j.bmcl.2009.06.091. Epub 2009 Jun 27.

PMID:
19616948
6.

Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.

Branca D, Cerretani M, Jones P, Koch U, Orvieto F, Palumbi MC, Rowley M, Toniatti C, Muraglia E.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4042-5. doi: 10.1016/j.bmcl.2009.06.031. Epub 2009 Jun 13.

PMID:
19553107
7.

Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.

Orvieto F, Branca D, Giomini C, Jones P, Koch U, Ontoria JM, Palumbi MC, Rowley M, Toniatti C, Muraglia E.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4196-200. doi: 10.1016/j.bmcl.2009.05.113. Epub 2009 Jun 2.

PMID:
19541484
8.

Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.

Dessole G, Branca D, Ferrigno F, Kinzel O, Muraglia E, Palumbi MC, Rowley M, Serafini S, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4191-5. doi: 10.1016/j.bmcl.2009.05.112. Epub 2009 Jun 2.

PMID:
19540115
9.

Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.

Scarpelli R, Di Marco A, Ferrigno F, Laufer R, Marcucci I, Muraglia E, Ontoria JM, Rowley M, Serafini S, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6078-82. doi: 10.1016/j.bmcl.2008.10.041. Epub 2008 Oct 12.

PMID:
18952417
10.

2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors.

Muraglia E, Altamura S, Branca D, Cecchetti O, Ferrigno F, Orsale MV, Palumbi MC, Rowley M, Scarpelli R, Steinkühler C, Jones P.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6083-7. doi: 10.1016/j.bmcl.2008.09.076. Epub 2008 Sep 24.

PMID:
18930398
11.

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.

Summa V, Petrocchi A, Bonelli F, Crescenzi B, Donghi M, Ferrara M, Fiore F, Gardelli C, Gonzalez Paz O, Hazuda DJ, Jones P, Kinzel O, Laufer R, Monteagudo E, Muraglia E, Nizi E, Orvieto F, Pace P, Pescatore G, Scarpelli R, Stillmock K, Witmer MV, Rowley M.

J Med Chem. 2008 Sep 25;51(18):5843-55. doi: 10.1021/jm800245z.

PMID:
18763751
12.

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.

Muraglia E, Kinzel O, Gardelli C, Crescenzi B, Donghi M, Ferrara M, Nizi E, Orvieto F, Pescatore G, Laufer R, Gonzalez-Paz O, Di Marco A, Fiore F, Monteagudo E, Fonsi M, Felock PJ, Rowley M, Summa V.

J Med Chem. 2008 Feb 28;51(4):861-74. doi: 10.1021/jm701164t. Epub 2008 Jan 25.

PMID:
18217703
13.

(1)H, (13)C and (15)N backbone assignments for the ligand binding domain of the Pseudomonas aeruginosa virulence regulator LasR.

Bottomley MJ, Muraglia E, Bazzo R.

Biomol NMR Assign. 2007 Dec;1(2):237-9. doi: 10.1007/s12104-007-9066-4. Epub 2007 Nov 30.

PMID:
19636874
14.

Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.

Gardelli C, Nizi E, Muraglia E, Crescenzi B, Ferrara M, Orvieto F, Pace P, Pescatore G, Poma M, Ferreira Mdel R, Scarpelli R, Homnick CF, Ikemoto N, Alfieri A, Verdirame M, Bonelli F, Paz OG, Taliani M, Monteagudo E, Pesci S, Laufer R, Felock P, Stillmock KA, Hazuda D, Rowley M, Summa V.

J Med Chem. 2007 Oct 4;50(20):4953-75. Epub 2007 Sep 8.

PMID:
17824681
15.

Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.

Pace P, Di Francesco ME, Gardelli C, Harper S, Muraglia E, Nizi E, Orvieto F, Petrocchi A, Poma M, Rowley M, Scarpelli R, Laufer R, Gonzalez Paz O, Monteagudo E, Bonelli F, Hazuda D, Stillmock KA, Summa V.

J Med Chem. 2007 May 3;50(9):2225-39. Epub 2007 Apr 12.

PMID:
17428043
16.
17.

4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.

Summa V, Petrocchi A, Matassa VG, Gardelli C, Muraglia E, Rowley M, Paz OG, Laufer R, Monteagudo E, Pace P.

J Med Chem. 2006 Nov 16;49(23):6646-9.

PMID:
17154493
18.

A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.

Kinzel O, Fattori D, Muraglia E, Gallinari P, Nardi MC, Paolini C, Roscilli G, Toniatti C, Gonzalez Paz O, Laufer R, Lahm A, Tramontano A, Cortese R, De Francesco R, Ciliberto G, Koch U.

J Med Chem. 2006 Sep 7;49(18):5404-7.

PMID:
16942012
19.

Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.

Muraglia E, Kinzel OD, Laufer R, Miller MD, Moyer G, Munshi V, Orvieto F, Palumbi MC, Pescatore G, Rowley M, Williams PD, Summa V.

Bioorg Med Chem Lett. 2006 May 15;16(10):2748-52. Epub 2006 Feb 28.

PMID:
16503141
20.

A functionally orthogonal estrogen receptor-based transcription switch specifically induced by a nonsteroid synthetic ligand.

Gallinari P, Lahm A, Koch U, Paolini C, Nardi MC, Roscilli G, Kinzel O, Fattori D, Muraglia E, Toniatti C, Cortese R, De Francesco R, Ciliberto G.

Chem Biol. 2005 Aug;12(8):883-93.

21.
22.

A novel, inducible, eukaryotic gene expression system based on the quorum-sensing transcription factor TraR.

Neddermann P, Gargioli C, Muraglia E, Sambucini S, Bonelli F, De Francesco R, Cortese R.

EMBO Rep. 2003 Feb;4(2):159-65. Erratum in: EMBO Rep. 2003 Apr;4(4):439.

23.

In vitro selection and characterization of hepatitis C virus serine protease variants resistant to an active-site peptide inhibitor.

Trozzi C, Bartholomew L, Ceccacci A, Biasiol G, Pacini L, Altamura S, Narjes F, Muraglia E, Paonessa G, Koch U, De Francesco R, Steinkuhler C, Migliaccio G.

J Virol. 2003 Mar;77(6):3669-79.

24.

The crystal structure of the quorum sensing protein TraR bound to its autoinducer and target DNA.

Vannini A, Volpari C, Gargioli C, Muraglia E, Cortese R, De Francesco R, Neddermann P, Marco SD.

EMBO J. 2002 Sep 2;21(17):4393-401.

25.

Crystallization and preliminary X-ray diffraction studies of the transcriptional regulator TraR bound to its cofactor and to a specific DNA sequence.

Vannini A, Volpari C, Gargioli C, Muraglia E, De Francesco R, Neddermann P, Di Marco S.

Acta Crystallogr D Biol Crystallogr. 2002 Aug;58(Pt 8):1362-4. Epub 2002 Jul 20.

PMID:
12136156
26.

Evolution, synthesis and SAR of tripeptide alpha-ketoacid inhibitors of the hepatitis C virus NS3/NS4A serine protease.

Colarusso S, Gerlach B, Koch U, Muraglia E, Conte I, Stansfield I, Matassa VG, Narjes F.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):705-8.

PMID:
11844706

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