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Design, synthesis, ...
Design, synthesis, and biological evaluation of combretastatin nitrogen-containing derivatives as inhibitors of tubulin assembly and vascular disrupting agents
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Monk, KA (author)
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Siles, R (author)
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Hadimani, MB (author)
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Mugabe, BE (author)
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Ackley, JF (author)
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Studerus, SW (author)
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- Edvardsen, Klaus (author)
- Lund University,Lunds universitet,Immunologi,Forskargrupper vid Lunds universitet,Immunology,Lund University Research Groups
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Trawick, ML (author)
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Garner, CM (author)
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Rhodes, MR (author)
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Pettit, GR (author)
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Pinney, KG (author)
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(creator_code:org_t)
- Elsevier BV, 2006
- 2006
- English.
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In: Bioorganic & Medicinal Chemistry. - : Elsevier BV. - 0968-0896. ; 14:9, s. 3231-3244
- Related links:
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http://dx.doi.org/10...
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https://lup.lub.lu.s...
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https://doi.org/10.1...
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Abstract
Subject headings
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- A series of analogs with nitro or serinamide substituents at the C-2'-, C-5'-, or C-C-position of the combretastatin A-4 (CA4) B-ring was synthesized and evaluated for cytotoxic effects against heart endothelioma cells, blood flow reduction to tumors in SCID mice, and as inhibitors of tubulin polymerization. The synthesis of these analogs typically featured a Wittig reaction between a suitably functionalized arylaldehyde and an arylphosphonium salt followed by separation of the resultant F and Z-isomers. several of these nitrogen-modified CA4 derivatives (both amino and nitro) demonstrate significant inhibition of tubulin assembly as well as cytotoxicity and in vivo blood flow reduction. 2'-Aminostilbenoid 7 and 2'-amino-3'-hydroxystilbenoid 29 proved to be the most active in this series. Both compounds, 7 and 29, have the potential for further pro-drug modification and development as vascular disrupting agents for treatment of solid tumor cancers and certain ophthalmological diseases.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Immunologi inom det medicinska området (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Immunology in the medical area (hsv//eng)
Keyword
- vascular disrupting agents
- pro-drug constructs
- anti-cancer
- inhibitors of tubulin assembly
- combretastatin
- tubilin
Publication and Content Type
- art (subject category)
- ref (subject category)
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- By the author/editor
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Monk, KA
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Siles, R
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Hadimani, MB
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Mugabe, BE
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Ackley, JF
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Studerus, SW
-
show more...
-
Edvardsen, Klaus
-
Trawick, ML
-
Garner, CM
-
Rhodes, MR
-
Pettit, GR
-
Pinney, KG
-
show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Immunology in th ...
- Articles in the publication
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Bioorganic & Med ...
- By the university
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Lund University