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  • Title: Copper-free click-chemistry platform to functionalize cisplatin prodrugs.
    Author: Pathak RK, McNitt CD, Popik VV, Dhar S.
    Journal: Chemistry; 2014 Jun 02; 20(23):6861-5. PubMed ID: 24756923.
    Abstract:
    The ability to rationally design and construct a platform technology to develop new platinum(IV) [Pt(IV)] prodrugs with functionalities for installation of targeting moieties, delivery systems, fluorescent reporters from a single precursor with the ability to release biologically active cisplatin by using well-defined chemistry is critical for discovering new platinum-based therapeutics. With limited numbers of possibilities considering the sensitivity of Pt(IV) centers, we used a strain-promoted azide-alkyne cycloaddition approach to provide a platform, in which new functionalities can easily be installed on cisplatin prodrugs from a single Pt(IV) precursor. The ability of this platform to be incorporated in nanodelivery vehicle and conjugation to fluorescent reporters were also investigated.
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