Issue 16, 2006
From the journal:

Dalton Transactions

New polyethyleneglycol-functionalized texaphyrins: synthesis and in vitro biological studies†‡

Wen-Hao Wei,a   Zhong Wang,b   Toshihisa Mizuno,§a   Cecilia Cortez,b   Lei Fu,b   Mint Sirisawad,b   Louie Naumovski,b   Darren Magda*b  and  Jonathan L. Sessler*a  

* Corresponding authors

a Department of Chemistry and Biochemistry, Institute for Cellular and Molecular Biology, 1 University Station-A5300, The University of Texas at Austin, Austin, TX 78712-0165
E-mail: Sessler@mail.utexas.edu

b Pharmacyclics, Inc., 995 East Arques Avenue Sunnyvale, CA 94085
E-mail: dmagda@pcyc.com

Abstract

The synthesis of four new analogues of motexafin gadolinium (MGd), a gadolinium(III) texaphyrin complex in clinical trials for its anticancer properties, is described. These new derivatives contain either 1,2-diaminobenzene or 2,3-diaminonaphthalene subunits as the source of the imine nitrogens and bear multiple 2-[2-(2-methoxyethoxy)ethoxy]ethoxy (PEG) groups, on either meso aryl or beta-pyrrolic substituents, to increase their water solubility. All four analogues were found to be more active in vitro than the parent system MGd as judged from cell proliferation assays using the PC3 and A549 cell lines.

Graphical abstract: New polyethyleneglycol-functionalized texaphyrins: synthesis and in vitro biological studies

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Article information

DOI
https://doi.org/10.1039/B515636J
Article type
Paper
Submitted
04 Nov 2005
Accepted
17 Jan 2006
First published
24 Jan 2006

Dalton Trans., 2006, 1934-1942

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New polyethyleneglycol-functionalized texaphyrins: synthesis and in vitro biological studies

W. Wei, Z. Wang, T. Mizuno, C. Cortez, L. Fu, M. Sirisawad, L. Naumovski, D. Magda and J. L. Sessler, Dalton Trans., 2006, 1934 DOI: 10.1039/B515636J

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