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Synthesis and cytotoxicity evaluation of 6,11-dihydro-pyridazo- and 6,11-dihydro-pyrido[2,3-b]phenazine-6,11-diones

Title
Synthesis and cytotoxicity evaluation of 6,11-dihydro-pyridazo- and 6,11-dihydro-pyrido[2,3-b]phenazine-6,11-diones
Authors
Lee H.-J.Kim J.S.Park S.-Y.Suh M.-E.Kim H.J.Seo E.-K.Lee C.-O.
Ewha Authors
서명은김화정서은경김진성
SCOPUS Author ID
서명은scopus; 김화정scopus; 서은경scopus
Issue Date
2004
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 12, no. 7, pp. 1623 - 1628
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
The 6,11-dihydro-pyridazo[2,3-b]phenazine-6,11-dione and 6,11-dihydro-pyrido[2,3-b]phenazine-6,11-dione derivatives were synthesized from 6,7-dichloro-5,8-phthalazinedione and 6,7-dichloro-5,8-quinolinedione, respectively, producing a series of new anticancer drugs. The cytotoxic activities of the prepared compounds were evaluated by a SRB (Sulforhodamine B) assay against the following tumor cell lines: A459 (human lung), SK-OV-3 (human ovarian), SK-MEL-2 (human melanoma), XF498 (human CNS), and HCT 15 (human colon). Almost all the derivatives of the 6,11-dihydro-pyridazo[2[,3-b] phenazine-6,11-dione and 6,11-dihydro-pyrido[2,3-b]phenazine-6,11-dione, tetracyclic heteroquinone analogues with four or three nitrogen atoms, exhibited excellent cytotoxicity on almost all the human tumor cell lines tested. Specifically, 6,11-dihydro-pyridazo[2,3-b]phenazine-6,11-dione (4a) exhibited potent activity against all the tumor cell lines, and in particular, its cytotoxic effect against HCT 15 (ED50=0.004 μg/mL) was 25 times greater than that of doxorubicin (ED50=0.093 μg/mL). © 2004 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2004.01.029
Appears in Collections:
약학대학 > 약학과 > Journal papers
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