ChemInform Abstract: Chemistry of the Pyrrolo(1,2-a)benzimidazole Antitumor Agents: Influence of the 7-Substituent on the Ability to Alkylate DNA and Inhibit Topoisomerase II.

ChemInform ◽  
2010 ◽  
Vol 28 (5) ◽  
pp. no-no
Author(s):  
R. ZHOU ◽  
E. B. SKIBO
Keyword(s):  
Topoisomerase Ii ◽  
Antitumor Agents ◽  
Alkylate Dna

Antitumor Agents, 107. New Cytotoxic 4-Alkylamino Analogues of 4'-Demethyl-Epipodophyllotoxin as Inhibitors of Human DNA Topoisomerase II

1989 ◽  
Vol 52 (3) ◽  
pp. 606-613 ◽  
Author(s):  
Kuo-Hsiung Lee ◽  
Yasuhiro Imakura ◽  
Mitsumasa Haruna ◽  
Scott A. Beers ◽  
Lee S. Thurston ◽  
...  
Keyword(s):  
Topoisomerase Ii ◽  
Antitumor Agents ◽  
Dna Topoisomerase Ii ◽  
Dna Topoisomerase ◽  
Human Dna

scholarly journals Use of a Rapid Throughput In Vivo Screen To Investigate Inhibitors of Eukaryotic Topoisomerase II Enzymes

1998 ◽  
Vol 42 (4) ◽  
pp. 889-894 ◽  
Author(s):  
Timothy R. Hammonds ◽  
Anthony Maxwell ◽  
John R. Jenkins
Keyword(s):  
Topoisomerase Ii ◽  
Antitumor Agents ◽  
Viable Cell ◽  
Cytotoxic Agents ◽  
New Method ◽  
Temperature Sensitive ◽  
Cell Counts ◽  
Similar Drug ◽  
In Vivo Screen

ABSTRACT Topoisomerase II catalyzes the passage of one DNA helix through another via a transient double-stranded break. The essential nature of this enzyme in cell proliferation and its mechanism of action make it an ideal target for cytotoxic agents. Saccharomyces cerevisiae topoisomerase II has been frequently used as a model for testing potential inhibitors of eukaryotic topoisomerase II as antitumor agents. The standard in vivo method of estimating the sensitivity of S. cerevisiae to the antitopoisomerase drugs is via inhibition or kill curves which rely on viable-cell counts and is labor intensive. We present an alternative to this, a high-throughput in vivo screen. This method makes use of a drug-permeable S. cerevisiae strain lacking endogenous topoisomerase II, which is modified to express either human topoisomerase IIα or IIβ or S. cerevisiae topoisomerase II carried on plasmids. Each modified strain expresses a full-length topoisomerase II enzyme, as opposed to the more commonly used temperature-sensitive S. cerevisiae mutant expressing yeast or yeast/human hybrid enzymes. A comparison of this new method with a plating-and-counting method gave similar drug sensitivity results, with increased accuracy and reduced manual input for the new method. The information generated has highlighted the sensitivities of different topoisomerase II enzymes and isoenzymes to several different classes of topoisomerase II inhibitor.

Antitumor Agents. 185.†Synthesis and Biological Evaluation of Tridemethylthiocolchicine Analogues as Novel Topoisomerase II Inhibitors

1998 ◽  
Vol 41 (11) ◽  
pp. 1956-1961 ◽  
Author(s):  
Jian Guan ◽  
Xiao-Kang Zhu ◽  
Yoko Tachibana ◽  
Kenneth F. Bastow ◽  
Arnold Brossi ◽  
...  
Keyword(s):  
Topoisomerase Ii ◽  
Antitumor Agents ◽  
Biological Evaluation ◽  
Topoisomerase Ii Inhibitors ◽  
Synthesis And Biological Evaluation

scholarly journals Antiproliferative and Enzyme Docking Analysis of Engleromycin from Engleromyces goetzei

Molecules ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 166 ◽  
Author(s):  
Yongli Zhang ◽  
Guilin Chen ◽  
Hong Ma ◽  
Mingquan Guo
Keyword(s):  
Antiproliferative Activity ◽  
Topoisomerase Ii ◽  
Antitumor Agents ◽  
Human Cancer ◽  
Biological Effects ◽  
A549 Cells ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Ht 29

Engleromyces goetzei P. Henn. (E. goetzei) has been widely used as a traditional herb for many years in Kenya due to its diverse biological effects. Although engleromycin was first isolated from E. goetzei in 1980, its pharmacological activity is still unknown. In this study, engleromycin from E. goetzei was identified by spectroscopic analyses, and subsequently examined for its antiproliferative activity using human cancer cell lines of SGC-7901, HT-29, HeLa and A549. As a result, it was revealed that engleromycin strongly inhibited the growth of SGC-7901, HT-29, HeLa and A549 cells with IC50 values at 26.77 ± 1.69 µM, 7.73 ± 0.18 µM, 7.00 ± 0.12 µM and 3.14 ± 0.03 µM, respectively. The results of topoisomerase II (Top II) inhibition assay in vitro implied that engleromycin might be a Top II inhibitor. Further insights into the potential mechanism of antiproliferative activity displayed that engleromycin could dock into the binding pockets of Top II, like the clinical inhibitor doxorubicin, and then inhibit the biological activity of Top II. Taken together, our findings suggest that engleromycin has an anticancer potential, and may serve as a leading compound for the development of antitumor agents.

Sign in / Sign up

Export Citation Format

Share Document