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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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publication status
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Bioorganic & Medicinal Chemistry Letters
volume
13
issue
9
pages
1505 - 1508
publisher
Elsevier
external identifiers
  • pmid:12699742
  • wos:000182418900001
  • scopus:12444259666
ISSN
1090-2120
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
2007-09-03 13:30:05
date last changed
2018-05-29 12:06:51
@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         = {1090-2120},
  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},
  volume       = {13},
  year         = {2003},
}