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Synthesis and cytotoxicity evaluation of substituted pyridazino[4,5-b]phenazine-5,12-diones and tri/tetra-azabenzofluorene-5,6-diones

Title
Synthesis and cytotoxicity evaluation of substituted pyridazino[4,5-b]phenazine-5,12-diones and tri/tetra-azabenzofluorene-5,6-diones
Authors
Lee H.-J.Kim J.S.Suh M.-E.Park H.J.Lee S.K.Rhee H.-K.Kim H.J.Seo E.-K.Kim C.Lee C.-O.Park Choo H.-Y.
Ewha Authors
김춘미박혜영김화정이상국서은경
SCOPUS Author ID
김춘미scopus; 박혜영scopus; 김화정scopus; 서은경scopus
Issue Date
2007
Journal Title
European Journal of Medicinal Chemistry
ISSN
0223-5234JCR Link
Citation
vol. 42, no. 2, pp. 168 - 174
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
The substituted pyridazino[4,5-b]phenazine-5,12-diones and tri/tetra-azabenzo[a]fluorene-5,6-diones were synthesized from 6,7-dichlorophthalazine-5,8-dione and 6,7-dichloroquinoline-5,8-dione, respectively. The cytotoxic activities of the prepared compounds were evaluated by an SRB (Sulforhodamine B) assay against the following human cancer cell lines: A549 (lung), SK-OV-3 (ovarian), SK-MEL-2 (melanoma), XF 498 (CNS), and HCT 15 (colon). Almost all synthesized pyridazino[4,5-b]phenazine-5,12-diones (7a-j) presented higher cytotoxicity than that of doxorubicin (IC50 = 0.097-0.225 μM) against the cancer cell lines. In particular, the cytotoxicity of compounds 7f (R1 = Et) and 7h (R1, R2 = Me) against all human cancer cell lines examined was about 10 times higher than that of doxorubicin. However, the cytotoxicities of several synthesized azabenzo[a]fluorene-5,6-diones (12a, 12c, 12d, 12e, and 12g) against the cancer cell lines in vitro were comparable to those of doxorubicin. © 2006 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2006.09.007
Appears in Collections:
약학대학 > 약학과 > Journal papers
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