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Synthesis of 1-/2-substituted-[1,2,3]triazolo[4,5-g]phthalazine-4,9-diones and evaluation of their cytotoxicity and topoisomerase II inhibition

Title
Synthesis of 1-/2-substituted-[1,2,3]triazolo[4,5-g]phthalazine-4,9-diones and evaluation of their cytotoxicity and topoisomerase II inhibition
Authors
Kim J.S.Rhee H.-K.Park H.J.Lee S.K.Lee C.-O.Park Choo H.-Y.
Ewha Authors
박혜영이상국
SCOPUS Author ID
박혜영scopus
Issue Date
2008
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
Bioorganic and Medicinal Chemistry vol. 16, no. 8, pp. 4545 - 4550
Indexed
SCI; SCIE; SCOPUS WOS scopus
Document Type
Article
Abstract
Studies on antitumor heterocyclic quinones containing nitrogens revealed that the number and position of nitrogens on the heterocyclic ring have significance on cytotoxicity of quinones. In our continuous effort to find more cytotoxic quinone compounds, we designed triazolophthalazine analogues in order to introduce more nitrogens on the heterocyclic quinones. 1-/2-Substituted-[1,2,3]triazolo[4,5-g]phthalazine-4,9-diones were synthesized by 1,3-dipolar addition of phthalazine-5,8-dione and 4-methoxybenzyl azide by modification of previously reported method. The cytotoxicity of the synthesized compounds was evaluated by a SRB (sulforhodamine B) assay against nine types of human cancer cell lines and inhibition against topoisomerase II (Topo II) of them was assessed by a decatenation assay. Most of the synthesized compounds showed considerably higher cytotoxicity than that of doxorubicin. Also, topoisomerase II inhibitory activity of the tested compounds was higher than that of etoposide and IC50 values of the compounds were 19.4-64.5 μM. © 2008 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2008.02.049
Appears in Collections:
약학대학 > 약학과 > Journal papers
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