Publications by authors named "Marco Molteni"

5 Publications

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Snorting the clivus away: an extreme case of cocaine-induced midline destructive lesion.

BMJ Case Rep 2016 Oct 20;2016. Epub 2016 Oct 20.

Otolaryngology Unit, ASST Santi Paolo e Carlo, Department of Health Sciences, Università degli Studi di Milano, Milan, Italy.

Cocaine is a drug with relevant socioeconomic and clinical implications, which is usually recreationally used for its stimulant effects. It is widely known that the habit of snorting cocaine is associated with a peculiar type of drug-induced chronic rhinitis, which leads to inflammation of the sinonasal mucosa, slowly progressing to a destruction of nasal, palatal and pharyngeal tissues. These characteristic lesions due to cocaine abuse are commonly called cocaine-induced midline destructive lesions (CIMDL). Diagnosis is not always straightforward, since various conditions, mainly vasculitis, might mimic this acquired condition. The extent of pharyngeal involvement varies, although often a prolonged abuse can trigger a progressive destruction of oral and nasal tissues, with development of infections and recurrent inflammation. Our article focuses on cocaine as a world health problem with important ear, nose and throat implications and discusses the difficulties in diagnosing and treating CIMDL, through a case report.
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http://dx.doi.org/10.1136/bcr-2016-216393DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5073690PMC
October 2016

Chiral resolution and pharmacological characterization of the enantiomers of the Hsp90 inhibitor 2-amino-7-[4-fluoro-2-(3-pyridyl)phenyl]-4-methyl-7,8-dihydro-6H-quinazolin-5-one oxime.

ChemMedChem 2014 Jul 17;9(7):1574-85. Epub 2014 Apr 17.

Genextra Group, Congenia s.r.l., Via Adamello 16, 20139 Milan (Italy); Current address: Drug Discovery Program, Department of Experimental Oncology, IEO-European Institute of Oncology, Via Adamello 16, 20139 Milan (Italy).

Heat-shock protein 90 (Hsp90) is a molecular chaperone involved in the stabilization of key oncogenic signaling proteins, and therefore, inhibition of Hsp90 represents a new strategy in cancer therapy. 2-Amino-7-[4-fluoro-2-(3-pyridyl)phenyl]-4-methyl-7,8-dihydro-6H-quinazolin-5-one oxime is a racemic Hsp90 inhibitor that targets the N-terminal adenosine triphosphatase site. We developed a method to resolve the enantiomers and evaluated their inhibitory activity on Hsp90 and the consequent antitumor effects. The (S) stereoisomer emerged as a potent Hsp90 inhibitor in biochemical and cellular assays. In addition, this enantiomer exhibited high oral bioavailability in mice and excellent antitumor activity in two different human cancer xenograft models.
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http://dx.doi.org/10.1002/cmdc.201400037DOI Listing
July 2014

Psi[CH(CF(3))NH]Gly-peptides: synthesis and conformation analysis.

Org Biomol Chem 2009 Jun 7;7(11):2286-96. Epub 2009 Apr 7.

Dipartimento di Chimica, Materiali, e Ingegneria Chimica Giulio Natta, Politecnico di Milano, via Mancinelli 7, 20131, Milano, Italy.

Psi[CH(CF(3))NH]Gly peptides, a conceptually new class of peptidomimetics having a stereogenic trifluoroethylamine group as a natural peptide-bond surrogate, have been synthesized by stereoselective addition of alpha-amino acid esters to trans-3,3,3-trifluoro-1-nitropropene. Long range nuclear Overhauser effects, detected via ROESY experiments, provided evidence that model Psi[CH(CF(3))NH]Gly-tetrapeptides incorporating a trifluoroethylamine mimic of the dipeptide loop Pro-Gly can be represented by an ensemble of unfolded and folded conformations. The latter are driven by the formation of a hydrogen bond between a carbonyl group and the aminic proton of the trifluoroethylamine unit. MD calculations indicate a population of conformers which adopt folded beta turn structures for all the L-peptides; on the other hand, a D-stereochemistry at the Pro residue induces a natural folding towards a beta hairpin conformation driven by the formation of a second hydrogen bond, regardless of the stereochemistry of the stereogenic peptide bond surrogate.
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http://dx.doi.org/10.1039/b901718fDOI Listing
June 2009

Stereocontrolled synthesis of psi[CH(CF3)NH]gly-peptides.

Org Lett 2003 Oct;5(21):3887-90

C.N.R.-Istituto di Chimica del Riconoscimento Molecolare, sezione A. Quilico, and Dipartimento di Chimica, Materiali ed Ingegneria Chimica G. Natta, Politecnico di Milano, via Mancinelli 7, I-20131, Milan, Italy.

[reaction: see text] A novel class of peptidomimetics having a stereogenic [CH(CF(3))NH] replacement for a [CONH] peptide bond has been synthesized. The new compounds have been obtained in a stereocontrolled fashion using a kinetically controlled aza-Michael addition of chiral alpha-amino acid esters to trans-3,3,3-trifluoro-1-nitropropene. The stereoselectivity is strongly influenced by the solvent, the base, its stoichiometry, and the R side-chain. Diastereomeric ratios higher than 11:1 were achieved using H-Val-OtBu.HCl in toluene with 1.1 equiv of DIPEA.
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http://dx.doi.org/10.1021/ol0354730DOI Listing
October 2003