Design, synthesis, and evaluation of novel 6-chloro-/fluorochromone derivatives as potential topoisomerase inhibitor anticancer agents

Biological activity of bis-benzimidazole derivatives on DNA topoisomerase I and HeLa, MCF7 and A431 cells

“…Many reports in recent years have shown that DNA topoisomerase inhibition by numerous natural and synthetic compounds is closely associated with the cytotoxic potentials of the inhibitory compounds [14,16,18,20]. A representative number of compounds (4/12) were selected to carry out MTTassays in vitro on HeLa, MCF7 and A431 cells to identify if their effects on topo I reactions coincided with their cytotoxicity.…”

An efficient synthesis of some new isolated and fused 2-oxo-2H-chromene derivatives as antimicrobial and antitumor agents

“…Fused and isolated 2-oxo-2H-chromenes (coumarins) comprise a very interesting class of compounds due to their significant antibacterial [1], antifungal [2][3][4], antimycobecterial [5,6], anticoagulants [7,8], inhibition of some enzymes [9,10] and antitumor [11][12][13] activities. With the expectations to find biological activity, we decided to investigate the synthesis of some novel systems of 2-oxo-2H-chromene derivatives bearing fused and isolated moieties.…”

Gossypol Interferes with Both Type I and Type II Topoisomerase Activities Without Generating Strand Breaks

“…Since the identification of Camptothecine (CPT) from Camptotheca acuminata as topoisomerase-targeting compound, several compounds with therapeutical potential were analyzed through topoisomerase reactions [12][13][14][15][16][17][18][19]. However, biological activity assays employing DNA topoisomerases in vast majority of these studies are limited to supercoil relaxations, a well-known approach to monitor either type I or type II activities in the presence of a test compound.…”