Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

Shudong Wang; Nikolai Zhelev; Susan Duff; Peter M. Fischer

doi:10.1016/j.bmcl.2006.02.035

Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

Shudong Wang, Nikolai Zhelev, Susan Duff, Peter M. Fischer

Research output: Contribution to journal › Article › peer-review

15 Citations (Scopus)

Abstract

Synthesis of paclitaxel–penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel–2′-pAntp[43–58]-NH₂ 3b and paclitaxel–2′-pAntp[52–58]-NH₂ 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug–peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.

Original language	English
Pages (from-to)	2628-2631
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2006.02.035
Publication status	Published - May 2006
Externally published	Yes

Keywords

Paclitaxel
Penetratin
Cell delivery vector
Drug–peptide conjugate
Antitumour activity

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10.1016/j.bmcl.2006.02.035

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title = "Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin",

abstract = "Synthesis of paclitaxel–penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel–2′-pAntp[43–58]-NH2 3b and paclitaxel–2′-pAntp[52–58]-NH2 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug–peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.",

author = "Shudong Wang and Nikolai Zhelev and Susan Duff and Fischer, {Peter M.}",

year = "2006",

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doi = "10.1016/j.bmcl.2006.02.035",

language = "English",

volume = "16",

pages = "2628--2631",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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TY - JOUR

T1 - Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

AU - Wang, Shudong

AU - Zhelev, Nikolai

AU - Duff, Susan

AU - Fischer, Peter M.

PY - 2006/5

Y1 - 2006/5

N2 - Synthesis of paclitaxel–penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel–2′-pAntp[43–58]-NH2 3b and paclitaxel–2′-pAntp[52–58]-NH2 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug–peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.

AB - Synthesis of paclitaxel–penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel–2′-pAntp[43–58]-NH2 3b and paclitaxel–2′-pAntp[52–58]-NH2 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug–peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.

U2 - 10.1016/j.bmcl.2006.02.035

DO - 10.1016/j.bmcl.2006.02.035

M3 - Article

VL - 16

SP - 2628

EP - 2631

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 10

ER -

Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

Abstract

Keywords

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