Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4
(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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https://lup.lub.lu.se/record/312816
- author
- organization
- publishing date
- 2003
- 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}}, }