Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs

Research output: Contribution to journal › Journal article › Research › peer-review

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Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs. / Pedersen, Palle J.; Christensen, Mikkel S.; Ruysschaert, Tristan; Linderoth, Lars; Andresen, Thomas L.; Melander, Fredrik; Mouritsen, Ole G.; Madsen, Robert; Clausen, Mads H.

In: Journal of Medicinal Chemistry, Vol. 52, No. 10, 2009, p. 3408-3415.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Pedersen, PJ, Christensen, MS, Ruysschaert, T, Linderoth, L, Andresen, TL, Melander, F, Mouritsen, OG, Madsen, R & Clausen, MH 2009, 'Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs', Journal of Medicinal Chemistry, vol. 52, no. 10, pp. 3408-3415. https://doi.org/10.1021/jm900091h

APA

Pedersen, P. J., Christensen, M. S., Ruysschaert, T., Linderoth, L., Andresen, T. L., Melander, F., Mouritsen, O. G., Madsen, R., & Clausen, M. H. (2009). Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs. Journal of Medicinal Chemistry, 52(10), 3408-3415. https://doi.org/10.1021/jm900091h

Vancouver

Pedersen PJ, Christensen MS, Ruysschaert T, Linderoth L, Andresen TL, Melander F et al. Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs. Journal of Medicinal Chemistry. 2009;52(10):3408-3415. https://doi.org/10.1021/jm900091h

Author

Pedersen, Palle J. ; Christensen, Mikkel S. ; Ruysschaert, Tristan ; Linderoth, Lars ; Andresen, Thomas L. ; Melander, Fredrik ; Mouritsen, Ole G. ; Madsen, Robert ; Clausen, Mads H. / Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs. In: Journal of Medicinal Chemistry. 2009 ; Vol. 52, No. 10. pp. 3408-3415.

Bibtex

@article{66d43618d12e46c2a08e26a3310cdbf1,
title = "Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs",
abstract = "The synthesis and biophysical characterization of four prodrug ether phospholipid conjugates are described. The lipids are prepared from the anticancer drug chlorambucil and have C16 and C18 ether chains with phosphatidylcholine or phosphatidylglycerol headgroups. All four prodrugs have the ability to form unilamellar liposomes (86-125 nm) and are hydrolyzed by phospholipase A2, resulting in chlorambucil release. Liposomal formulations of prodrug lipids displayed cytotoxicity toward HT-29, MT-3, and ES-2 cancer cell lines in the presence of phospholipase A2, with IC50 values in the 8-36 μM range.",
author = "Pedersen, {Palle J.} and Christensen, {Mikkel S.} and Tristan Ruysschaert and Lars Linderoth and Andresen, {Thomas L.} and Fredrik Melander and Mouritsen, {Ole G.} and Robert Madsen and Clausen, {Mads H.}",
year = "2009",
doi = "10.1021/jm900091h",
language = "English",
volume = "52",
pages = "3408--3415",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "10",

}

RIS

TY - JOUR

T1 - Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs

AU - Pedersen, Palle J.

AU - Christensen, Mikkel S.

AU - Ruysschaert, Tristan

AU - Linderoth, Lars

AU - Andresen, Thomas L.

AU - Melander, Fredrik

AU - Mouritsen, Ole G.

AU - Madsen, Robert

AU - Clausen, Mads H.

PY - 2009

Y1 - 2009

N2 - The synthesis and biophysical characterization of four prodrug ether phospholipid conjugates are described. The lipids are prepared from the anticancer drug chlorambucil and have C16 and C18 ether chains with phosphatidylcholine or phosphatidylglycerol headgroups. All four prodrugs have the ability to form unilamellar liposomes (86-125 nm) and are hydrolyzed by phospholipase A2, resulting in chlorambucil release. Liposomal formulations of prodrug lipids displayed cytotoxicity toward HT-29, MT-3, and ES-2 cancer cell lines in the presence of phospholipase A2, with IC50 values in the 8-36 μM range.

AB - The synthesis and biophysical characterization of four prodrug ether phospholipid conjugates are described. The lipids are prepared from the anticancer drug chlorambucil and have C16 and C18 ether chains with phosphatidylcholine or phosphatidylglycerol headgroups. All four prodrugs have the ability to form unilamellar liposomes (86-125 nm) and are hydrolyzed by phospholipase A2, resulting in chlorambucil release. Liposomal formulations of prodrug lipids displayed cytotoxicity toward HT-29, MT-3, and ES-2 cancer cell lines in the presence of phospholipase A2, with IC50 values in the 8-36 μM range.

U2 - 10.1021/jm900091h

DO - 10.1021/jm900091h

M3 - Journal article

C2 - 19402667

AN - SCOPUS:66249132302

VL - 52

SP - 3408

EP - 3415

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 10

ER -

ID: 230977061