Alessandro Boezio

Somerville, Massachusetts, United States Contact Info
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Publications

  • Development of novel azabenzofuran TRPA1 antagonists as in vivo tools.

    Bioorganic & medicinal chemistry letters

    The transient receptor potential ankyrin 1 (TRPA1) channel is activated by noxious stimuli including chemical irritants and endogenous inflammatory mediators. Antagonists of this channel are currently being investigated for use as therapeutic agents for treating pain, airway disorders, and itch. A novel azabenzofuran series was developed that demonstrated in vitro inhibition of allyl isothiocyanate (AITC)-induced (45)Ca(2+) uptake with nanomolar potencies against both human and rat TRPA1. From…

    The transient receptor potential ankyrin 1 (TRPA1) channel is activated by noxious stimuli including chemical irritants and endogenous inflammatory mediators. Antagonists of this channel are currently being investigated for use as therapeutic agents for treating pain, airway disorders, and itch. A novel azabenzofuran series was developed that demonstrated in vitro inhibition of allyl isothiocyanate (AITC)-induced (45)Ca(2+) uptake with nanomolar potencies against both human and rat TRPA1. From this series, compound 10 demonstrated in vivo target coverage in an AITC-induced flinching model in rats while providing unbound plasma concentrations up to 16-fold higher than the TRPA1 rat IC50.

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  • Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors

    Bioorganic & Medicinal Chemistry Letters

    mTOR is a critical regulator of cellular signaling downstream of multiple growth factors. The mTOR/PI3K/AKT pathway is frequently mutated in human cancers and is thus an important oncology target.

    Herein we report the evolution of our program to discover ATP-competitive mTOR inhibitors that demonstrate improved pharmacokinetic properties and selectivity compared to our previous leads.

    Through targeted SAR and structure-guided design, new imidazopyridine and imidazopyridazine…

    mTOR is a critical regulator of cellular signaling downstream of multiple growth factors. The mTOR/PI3K/AKT pathway is frequently mutated in human cancers and is thus an important oncology target.

    Herein we report the evolution of our program to discover ATP-competitive mTOR inhibitors that demonstrate improved pharmacokinetic properties and selectivity compared to our previous leads.

    Through targeted SAR and structure-guided design, new imidazopyridine and imidazopyridazine scaffolds were identified that demonstrated superior inhibition of mTOR in cellular assays, selectivity over the closely related PIKK family and improved in vivo clearance over our previously reported benzimidazole series.

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  • New methods in asymmetric catalysis based on new hemi-labile bidentate ligands

    Pure and Applied Chemistry

    Chiral bidentate hemi-labile bis(phosphine) monoxide ligands were shown to be quite effective in various copper-catalyzed transformations. Among them, the nucleophilic addition to imines, the conjugate addition to α,β-unsaturated nitro derivatives, and the conjugate reduction of α,β-unsaturated sulfones generally gave good to excellent yields and high enantiomeric excesses.

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  • Mitsunobu Reaction Using Triphenylphosphine Linked to Non-Cross-Linked Polystyrene

    Journal of Organic Chemistry / American Chemical Society

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Patents

  • Fused heterocyclic derivatives and methods of use

    Issued USPTO 08524900

    Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

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  • Preparation of heteroaryl compounds as PIKK inhibitors for the treatment of cancer

    Issued US WO 2010132598

  • Preparation of indole and benzimidazole compounds as mTOR kinase inhibitors for the treatment of cancer

    Issued US WO 2010096314

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