Synthesis, dna binding and topoisomerase i inhibition activity of thiazacridine and imidazacridine derivatives. Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase i inhibitors article pdf available in journal of medicinal chemistry 4917. Topoisomerase ii inhibitors include doxorubicin, etoposide, and mitoxantrone. Despite the popular applications of topo ii inhibitors in cancer therapy, there is.
Topoisomerase i inhibitors include camptothecin, topotecan, and irinotecan. The aromathecin or rosettacin class of topoisomerase i top1 inhibitors is effectively a composite of the natural products camptothecin and luotonin a and the synthetic indenoisoquinolines. Pdf dna topoisomerase inhibitors, known for their broad antitumour activity, represent one of the most. Investigating the hypothesis of shared structureactivity relationships. Synthesis and evaluation of indenoisoquinoline topoisomerase i inhibitors substituted with nitrogen heterocycles november 2006 journal of medicinal chemistry 4921. Topoisomerase inhibitors and types of them international journal. The manual provided by intergen recommended hl60 cells to be. Alcohol, diol, and carbohydratesubstituted indenoisoquinolines as topoisomerase i inhibitors. Inhibitors of the mammalian enzymes are widely used antitumor drugs. Activity of topotecan, a new topoisomerase inhibitor, against human tumor colony forming units in vitro. Polyphenols also help in the bacterial protein precipitation and enzymatic. Novel nonfluoroquinolone inhibitors of bacterial type ii topoisomerases dna gyrase and topoisomerase iv have the potential to become such drugs because they display potent antibacterial activity and exhibit no targetmediated crossresistance with fluoroquinolones.
Thus, it might be interfering with the replication and transcription of the bacteria. Synthesis of arylsubstituted naphthalenoids as potent. Synthesis of arylsubstituted naphthalenoids as potent topoisomerase inhibitors authors. Dna topoisomerases are the cellular enzymes that change the topological state of dna. Investigating the relationships involving stereochemistry, hydrogen bonding, and biological. This causes proteinlinked dna singlestrand breaks and replication doublestrand breaks. Synthesis of nitrated indenoisoquinolines as topoisomerase. This causes proteinlinked dna single and doublestrand breaks.
Topoisomerase inhibitor an overview sciencedirect topics. Design and synthesis of 4amino2phenylquinazolines as novel topoisomerase i inhibitors with molecular modeling. Topoisomerase inhibitors are agents designed to interfere with the action. Request pdf synthesis and evaluation of mansonone f derivatives as topoisomerase inhibitors a series of mansonone f mf derivatives were designed and synthesized. Design, synthesis, and anticancer evaluation of novel indole derivatives of ursolic acid as potential topoisomerase ii inhibitors aliang li, yun hao, wenyan wang, qingsong liu, yue sun and wen gu jiangsu provincial key lab for the chemistry and utilization of agroforest biomass, jiangsu key lab of.
Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase i inhibitors. Inhibitors of nucleotide synthesis drug mechanism of. Synthesis and characterization of tetrahydropyranbased. Secondary metabolites as dna topoisomerase inhibitors. Synthesis and biological evaluation of 14aminoalkylaminomethylaromathecins as topoisomerase i inhibitors. Design, synthesis, and biological evaluation of 14.
Synthesis and evaluation of mansonone f derivatives as. Dibasic tetrahydropyranbased compounds such as 6 and 21 are potent inhibitors of both dna gyrase and topoisomerase iv, displaying antibacterial activities against grampositive and gramnegative pathogens staphylococcus aureus, enterobacteriaceae, pseudomonas aeruginosa, and acinetobacter baumannii. The indenoisoquinolines represent a class of noncamptothecin topoisomerase i top1 inhibitors that exert cytotoxicity by trapping the covalent complex formed between dna and top1 during relaxation of dna supercoils. Pdf design and synthesis of 4amino2phenylquinazolines. The indenoisoquinolines represent a class of noncamptothecin topoisomerase i top1 inhibitors that exert cytotoxicity by trapping the covalent complex formed between dna and top1 during relaxation of. Pdf synthesis, dna binding and topoisomerase i inhibition.508 308 1448 903 1423 889 822 462 919 18 1107 76 1262 878 497 383 1259 185 400 1289 420 1345 637 925 264 861 1264 1469 496 1