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Ester Muraglia

Explore the profile of Ester Muraglia including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 26
Citations 753
Followers 0
Related Specialties
Biochemistry
Chemistry
Molecular Biology
Top 10 Co-Authors
Michael Rowley
Philip Jones
Ralph Laufer
Federica Orvieto
Edith Monteagudo
Uwe Koch
Olaf Kinzel
Danila Branca
Vincenzo Summa
Maria Cecilia Palumbi
Published In
Bioorg Med Chem Lett
J Med Chem
J Virol
Acta Crystallogr D Biol Crystallogr
EMBO Rep
Affiliations
Soon will be listed here.
Recent Articles
1.
N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists
Muraglia E, Ontoria J, Branca D, Dessole G, Bresciani A, Fonsi M, et al.
Bioorg Med Chem Lett . 2011 Aug; 21(18):5283-8. PMID: 21802943
Smoothened (Smo) antagonists are emerging as new therapies for the treatment of neoplasias with aberrantly reactivated hedgehog (Hh) signaling pathway. A novel series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as smoothened antagonists was...
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 L, Muraglia E, et al.
Bioorg Med Chem Lett . 2009 Dec; 20(3):1094-9. PMID: 20031401
Herein we describe the discovery of a novel series of pyrrolo[1,2-a]pyrazin-1(2H)-one PARP inhibitors. Optimization led to compounds that display excellent PARP-1 enzyme potency and inhibit the proliferation of BRCA deficient...
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, Bufi L, Monteagudo E, et al.
Bioorg Med Chem Lett . 2009 Dec; 20(3):1100-5. PMID: 20022747
We describe an extensive SAR study in the 6-[4-fluoro-3-(substituted)benzyl]-4,5-dimethylpyridazin-3(2H)-one series which led to the identification of potent PARP-1 inhibitors, capable of inhibiting the proliferation of BRCA-1 deficient cancer cells in...
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 J, Altamura S, Di Marco A, Ferrigno F, Laufer R, Muraglia E, et al.
J Med Chem . 2009 Nov; 52(21):6782-9. PMID: 19888759
5-Aryl-2-(trifluoroacetyl)thiophenes were identified as a new series of class II HDAC inhibitors (HDACi). Further development of this new series led to compounds such as 6h, a potent inhibitor of HDAC4...
5.
(1)H, (13)C and (15)N backbone assignments for the ligand binding domain of the Pseudomonas aeruginosa virulence regulator LasR
Bottomley M, Muraglia E, Bazzo R
Biomol NMR Assign . 2009 Jul; 1(2):237-9. PMID: 19636874
LasR regulates toxin production in Pseudomonas aeruginosa and its inhibition can attenuate the virulence of this opportunistic human pathogen. To aid studies of interactions with inhibitors, we report the NMR...
6.
Dihydroxy-pyrimidine and N-methylpyrimidone HIV-integrase inhibitors: improving cell based activity by the quaternarization of a chiral center
Nizi E, Vittoria Orsale M, Crescenzi B, Pescatore G, Muraglia E, Alfieri A, et al.
Bioorg Med Chem Lett . 2009 Jul; 19(16):4617-21. PMID: 19616948
In the context of HIV-integrase, dihydroxypyrimidine and N-methyl pyrimidone inhibitors the cellular activity of this class of compounds has been optimized by the introduction of a simple methyl substituent in...
7.
Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors
Branca D, Cerretani M, Jones P, Koch U, Orvieto F, Palumbi M, et al.
Bioorg Med Chem Lett . 2009 Jun; 19(15):4042-5. PMID: 19553107
PARP inhibitors have been demonstrated to retard intracellular DNA repair and therefore sensitize tumor cells to cytotoxic agents or ionizing radiation. We report the identification of a novel class of...
8.
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 J, et al.
Bioorg Med Chem Lett . 2009 Jun; 19(15):4196-200. PMID: 19541484
A novel series of pyrazolo[1,5-a]quinazolin-5(4H)-one derivatives proved to be a potent class of PARP-1 inhibitors. An extensive SAR around the 3-position of pyrazole in the scaffold led to the discovery...
9.
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 M, et al.
Bioorg Med Chem Lett . 2009 Jun; 19(15):4191-5. PMID: 19540115
We report the synthesis and biological evaluation of N-[(1-aryl-1H-indazol-5-yl)methyl]amide derivatives as Smoothened antagonists and inhibitors of the Hedgehog pathway. Identification of the lead structure 1 by HTS, followed by SAR...
10.
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, et al.
Bioorg Med Chem Lett . 2008 Oct; 18(23):6078-82. PMID: 18952417
5-(Trifluoroacetyl)thiophene-2-carboxamides were found to be potent and selective class II HDAC inhibitors. This paper describes their further development and the investigation on the cause for the lack of cell-based activity....