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Copper-free click-chemistry platform to functionalize cisplatin prodrugs.

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.

SUBMITTER: Pathak RK

PROVIDER: S-EPMC4345128 | biostudies-literature | 2014 Jun

REPOSITORIES: biostudies-literature

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Copper-free click-chemistry platform to functionalize cisplatin prodrugs.

Pathak Rakesh K RK McNitt Christopher D CD Popik Vladimir V VV Dhar Shanta S

Chemistry (Weinheim an der Bergstrasse, Germany) 20140423 23

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-promote ...[more]

PMID: 24756923

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