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Journal article

Synthesis and biological properties of bioreductively targeted nitrothienyl prodrugs of combretastatin A-4.

Abstract:

Nitrothienylprop-2-yl ether formation on the 3'-phenolic position of combretastatin A-4 (1) abolishes the cytotoxicity and tubulin polymerization-inhibitory effects of the drug. 5-Nitrothiophene derivatives of 1 were synthesized following model kinetic studies with analogous coumarin derivatives, and of these, compound 13 represents a promising new lead in bioreductively targeted cytotoxic anticancer therapies. In this compound, optimized gem-dimethyl alpha-carbon substitution enhances both t...

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Publication status:
Published

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Authors


Thomson, P More by this author
Naylor, MA More by this author
Everett, SA More by this author
Stratford, MR More by this author
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Journal:
Molecular cancer therapeutics
Volume:
5
Issue:
11
Pages:
2886-2894
Publication date:
2006-11-05
DOI:
EISSN:
1538-8514
ISSN:
1535-7163
URN:
uuid:1b77d0c1-e8cd-476c-9d86-87ff15105ec8
Source identifiers:
131886
Local pid:
pubs:131886

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