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. 2021 Sep 7;16(23):3496–3512. doi: 10.1002/cmdc.202100473

Table 6.

Summary of mutual prodrugs of 5‐FU for targeted drug delivery.

Compd.

Type of hybrid

Linker

Study

Outcomes

Ref.

22c, 24 ac

5‐FU/aspartic acid oligopeptides‐based

succinate

HAP binding study, drug release study, in vitro cytotoxicity assay, in vivo biodistribution in mice tissue

targeting the bone antiproliferative activity

[101a]

26 ac

5‐FU/F16

carboxylic, amidic, disulfide

in vitro cytotoxicity assay, detection of cellular uptake, colocalization assay, detection of apoptosis and cell cycle, in vitro measurement of intracellular oxidation level, stability study in PBS or DMEM medium

targeting mitochondria ↑ antiproliferative activity

[107]

27, 28

5‐FU/c(RGDyK)

amide, disulfide

in vitro cytotoxicity assay, chemostability study, 5‐FUA release assay

integrin targeted chemotherapy ↑ antiproliferative activity

[115]