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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
- Synthesis and cytotoxicity evaluation of substituted pyridazino[4,5-b]phenazine-5,12-diones and tri/tetra-azabenzofluorene-5,6-diones
- 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
- 김춘미; 박혜영; 김화정; 이상국; 서은경
- SCOPUS Author ID
- 김춘미; 박혜영; 김화정; 서은경
- Issue Date
- Journal Title
- European Journal of Medicinal Chemistry
- vol. 42, no. 2, pp. 168 - 174
- SCI; SCIE; SCOPUS
- 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.
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