Literature DB >> 20192275

The synthesis of a c(RGDyK) targeted SN38 prodrug with an indolequinone structure for bioreductive drug release.

Baohua Huang1, Ankur Desai, Shengzhuang Tang, Thommey P Thomas, James R Baker.   

Abstract

Preparation of a novel c(RGDyK) targeted SN38 prodrug incorporating an indolequinone structure for bioreductively triggered drug release is described. This design yields a prodrug that targets surface molecules on tumor cells (alpha(v)beta(3) integrins) and releases drug under bioreductive conditions. There are three moieties in the prodrug design, namely a therapeutic drug SN38, an indolequinone structure serving as a drug releasing trigger, and an alpha(v)beta(3) integrin targeting peptide c(RGDyK). Preliminary studies showed that SN38 is released in the presence of a bioreductive enzyme (DT-diaphorase).

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Year:  2010        PMID: 20192275      PMCID: PMC2851157          DOI: 10.1021/ol1002626

Source DB:  PubMed          Journal:  Org Lett        ISSN: 1523-7052            Impact factor:   6.005


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