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Issue 12, 2016
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New potent αvβ3 integrin ligands based on azabicycloalkane (γ,α)-dipeptide mimics

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Abstract

We have designed a new synthetic strategy for the preparation of a new class of cyclic RGD integrin ligands in which the azabicycloalkane scaffold can be envisaged as a (γ,α) dipeptide mimic. The synthesis and in vitro biological evaluation of these RGD derivatives, as well as the computational study of their conformational properties and binding modes to αVβ3 integrin are described. Compound 3 has shown to be a promising candidate as αVβ3 integrin antagonist able to interfere with both cell adhesion and movement on vitronectin with no evidence of cytotoxic effects.

Graphical abstract: New potent αvβ3 integrin ligands based on azabicycloalkane (γ,α)-dipeptide mimics

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Publication details

The article was received on 03 Feb 2016, accepted on 19 Feb 2016 and first published on 19 Feb 2016


Article type: Paper
DOI: 10.1039/C6OB00287K
Citation: Org. Biomol. Chem., 2016,14, 3221-3233
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    New potent αvβ3 integrin ligands based on azabicycloalkane (γ,α)-dipeptide mimics

    M. Pilkington-Miksa, E. M. V. Araldi, D. Arosio, L. Belvisi, M. Civera and L. Manzoni, Org. Biomol. Chem., 2016, 14, 3221
    DOI: 10.1039/C6OB00287K

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