http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2018237140-A1

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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C211-30
filingDate 2018-06-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_abac116277f3870652fe89b2f7abcee3
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publicationDate 2018-12-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2018237140-A1
titleOfInvention TOPOISOMERASE INHIBITORS HAVING ANTIBACTERIAL ACTIVITY AND ANTI-CANCER ACTIVITY
abstract The present invention relates to human type II topoisomerase inhibitors (Top2) which are the backbone of many cancer chemotherapy regimens. Unfortunately, the onset of toxicity severely limits the usefulness of these potent drugs. There is some conservation between the human Top2 and bacterial homologs (DNA gyrase and TopoIV). Thus, the conversion of antibacterial inhibitors of topoisomerase into antineoplastic agents is a strategy for introducing anticancer compounds. The invention relates to the conversion of deoxynybomycin (DNM) from a natural product and a DNA gyrase inhibitor with minimal cytotoxicity to a compound having anticancer activity. Detailed in vitro and cell culture experiments demonstrate that these compounds inhibit Top2 and also act on topoisomerase I. Similar approaches are applicable to other classes of gyrase inhibitors and other antibacterial targets for the discovery of new drugs. cancer.
priorityDate 2017-06-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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