• Bulletin of the Korean Chemical Society
• /
• v.32 no.7
• /
• pp.2391-2396
• /
• 2011

Benzonaphthofurandiones containing four coplanar fused aromatic rings were synthesized and evaluated for their cytotoxicity against five human cancer cell lines, and their inhibitory activity on topoisomerases. These benzonaphthofurandiones were prepared by condensation of 2,3-dichloronaphthoquinone and three aromatic diols with base catalysts in alcohol. The synthesized compounds were o-alkylated with six dialkylaminoalkyl halides. The hydroxy derivatives (8a-8g) exhibited relatively potent cytotoxicity among the prepared compounds. These compounds were evaluated as excellent inhibitors against topoisomerase II (topo II). Especially, the hydroxy analogue with branched methyl side chain (8e) showed high cytotoxicity against cancer cell lines and good inhibitory activity on topo II.

• Archives of Pharmacal Research
• /
• v.22 no.5
• /
• pp.507-514
• /
• 1999

6-(1-azidoalkyl)-DMNQ derivatives compared to 2-(1-azidoalkyl)-DMNQ isomers, exhibited higher cytotoxic activity against L1210 mouse leukemia cells and stronger inhibition of DNA topoisomerase-I (TOPO-I), suggesting involvement of steric hindrance. However, similar antitumor activity against mice bearing S-180 cell was shown by 2-an 6-(1-azidoalkyl)-DMNQ derivatives.

• Bulletin of the Korean Chemical Society
• /
• v.32 no.10
• /
• pp.3566-3570
• /
• 2011

A series of 2,4,6-tripyridyl pyridines were synthesized, and evaluated for their antitumor cytotoxicity, topoisomerase I and II inhibitory activity. From the eighteen prepared compounds, compounds 10-12 have shown better or similar cytotoxicity against several human cancer cell lines as compared to 2,2':6',2"-terpyridine and doxorubicin. Especially, compound 10 exhibited the most potent cytotoxicity better than positive controls. Structure-activity relationship study indicated that 2,2':6',2"-terpyridine skeleton has an important role in displaying significant cytotoxicity against several human cancer cell lines.

• Journal of the Korean Chemical Society
• /
• v.49 no.5
• /
• pp.449-460
• /
• 2005

• Proceedings of the PSK Conference
• /
• 2003.10b
• /
• pp.70.2-71
• /
• 2003

Quinolone resistance in Streptococcus pneumoniae is related to mutations in the DNA gyrase and topoisomerase IV genes. DW-286a displayed potent activity against S. pneumoniae C9211 (MIC, 0.015 ${\mu}$g/ml) compared with gemifloxacin (MIC, 0.06 ${\mu}$g/ml). This study was performed to analyze the ability of DW-286a to cause resistance development in S. pneumoniae and to establish whether DNA gyrase or topoisomerase IV is primary target. DW-286a resistant mutants of S. pneumoniae C9211 were generated by stepwise selection at increasing drug concentration. (omitted)

• Journal of Microbiology
• /
• v.37 no.2
• /
• pp.97-101
• /
• 1999

Random hexapeptide library on the surface of filamentous bacteriophage was constructed using the SurfZAP vector. The size of the library was approximately 105. The peptide insert was flanked by two cysteines to constrain the peptide structure with a disulfide bond. This library was screened for the topoisomerase II binding peptide. Dramatic enrichment of the fusion phage over the VCS M13 helper phage was demonstrated by bio-panning affinity selection.

• Proceedings of the PSK Conference
• /
• 2003.04a
• /
• pp.236.2-237
• /
• 2003

Several studies of terbenzimidazoles and bibenzimidazoles suggested that benzimidazoles, especially 5-nitro-2-(para-methoxyphenyl)benzimidazole. possess topoisomerase I inhibition activities. In order to find out the structure activity relationship of 5-nitro-2-phenyl-benzimidazoles. eight derivatives that are substituted at the para position of 2-phenyl moiety were selected, synthesized ＆ evaluated considering their electronic or lipophilic parameters. (omitted)

• Bulletin of the Korean Chemical Society
• /
• v.29 no.2
• /
• pp.471-474
• /
• 2008

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.347.1-347.1
• /
• 2002

In cancer chemotherapy. it is becoming increasingly clear that the DNA topoisomerases play an active role in the expression of the cytotoxic action of drugs. The amino substituted azaanthraquinones have attracted much interest due to their possible role as topoisomerase inhibitors. In connection with our interests in the design and synthesis of potent topoisomerase inhibitor. we herein described the preparation of a series of benzoquinoxalinedione derivatives. These were designed based on the SAR of azaanthraquinones and structural analysis of products which are fitted with doxorubicin.

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.314.2-314.2
• /
• 2002

DNA topoisomerases catalyze changes in DNA topology through cycles of transient DNA strand breakage and religation. During this process. the active site tyrosine in human DNA topoisomerase Ⅰ(Top Ⅰ) becomes covalently linked to the 3'-ends of a single-stranded nick in the DNA duplex, Stabilization of the Top Ⅰ-DNA cleavable complex is the common initial event leading to the cytotoxicity of top 1 inhibitors. (omitted)