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Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4

Hadimani, MB ; Hua, Jianyi LU ; Jonklaas, MD ; Kessler, RJ ; Sheng, Yezhou LU ; Olivares, A ; Tanpure, RP ; Weiser, A ; Zhang, JX and Edvardsen, Klaus LU , et al. (2003) In Bioorganic & Medicinal Chemistry Letters 13(9). p.1505-1508
Abstract
Combretastatin A-4 disodiumphosphate (CA4P), a prodrug formulation of the natural product combretastatin A-4 (CA4), is currently in clinical investigation for the treatment of cancer. In vivo, CA4P is rapidly enzymatically converted to CA4, a potent inhibitor of tubulin polymerization (IC50 = 1-2 muM), and rapidly causes bloodflow shutdown in tumor tissues. A variety of alkyl and aryl di- and triesters of CA4P have been synthesized and evaluated as potential CA4 prodrugs and/or stable CAV analogues. (C) 2003 Elsevier Science Ltd. All rights reserved.
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organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Bioorganic & Medicinal Chemistry Letters
volume
13
issue
9
pages
1505 - 1508
publisher
Elsevier
external identifiers
  • pmid:12699742
  • wos:000182418900001
  • scopus:12444259666
ISSN
0960-894X
DOI
10.1016/S0960-894X(03)00206-3
language
English
LU publication?
yes
id
6e36e319-77b6-4836-823b-63872820be54 (old id 312816)
date added to LUP
2016-04-01 12:10:04
date last changed
2022-02-03 18:28:37
@article{6e36e319-77b6-4836-823b-63872820be54,
  abstract     = {{Combretastatin A-4 disodiumphosphate (CA4P), a prodrug formulation of the natural product combretastatin A-4 (CA4), is currently in clinical investigation for the treatment of cancer. In vivo, CA4P is rapidly enzymatically converted to CA4, a potent inhibitor of tubulin polymerization (IC50 = 1-2 muM), and rapidly causes bloodflow shutdown in tumor tissues. A variety of alkyl and aryl di- and triesters of CA4P have been synthesized and evaluated as potential CA4 prodrugs and/or stable CAV analogues. (C) 2003 Elsevier Science Ltd. All rights reserved.}},
  author       = {{Hadimani, MB and Hua, Jianyi and Jonklaas, MD and Kessler, RJ and Sheng, Yezhou and Olivares, A and Tanpure, RP and Weiser, A and Zhang, JX and Edvardsen, Klaus and Kane, RR and Pinney, KG}},
  issn         = {{0960-894X}},
  language     = {{eng}},
  number       = {{9}},
  pages        = {{1505--1508}},
  publisher    = {{Elsevier}},
  series       = {{Bioorganic & Medicinal Chemistry Letters}},
  title        = {{Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4}},
  url          = {{http://dx.doi.org/10.1016/S0960-894X(03)00206-3}},
  doi          = {{10.1016/S0960-894X(03)00206-3}},
  volume       = {{13}},
  year         = {{2003}},
}