Novel N-1 substituted fluoroquinolones inhibit human topoisomerase I activity and exhibit anti-proliferative activity

Summary Fluoroquinolone-class agents selectively target the bacterial type IIA topoisomerases DNA gyrase and topoisomerase IV, with a few exceptions that target eukaryotic type IIA topoisomerases. Fluoroquinolones bind and stabilize type IIA topoisomerase-DNA covalent complexes that contain a double...

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Bibliographic Details
Published in:	Investigational new drugs Vol. 37; no. 2; pp. 378 - 383
Main Authors:	Oppegard, Lisa M., Delgado, Justine L., Kulkarni, Chaitanya A., Towle, Tyrell R., Hart, Delaney E., Williams, Bridget P., Lentz, Sarah R. C., Norris, Beverly J., Flory, Craig M., Schumacher, Robert J., Murry, Daryl J., Kerns, Robert J., Hiasa, Hiroshi
Format:	Journal Article
Language:	English
Published:	New York Springer US 01.04.2019 Springer Nature B.V
Subjects:	5-Fluorouracil Animals Antibiotics Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antineoplastic drugs Antiproliferatives Antitumor agents Apoptosis Aromatic compounds Biotechnology Cancer Catalysis Catalytic activity Cell Proliferation Colonic Neoplasms - drug therapy Colonic Neoplasms - enzymology Colonic Neoplasms - pathology Colorectal cancer Colorectal carcinoma Coordination compounds Deoxyribonucleic acid DNA DNA topoisomerase DNA topoisomerase (ATP-hydrolysing) DNA topoisomerase IV DNA Topoisomerases, Type I - chemistry Drug development Female Fluoroquinolones Fluoroquinolones - chemistry Fluoroquinolones - pharmacology Humans In vivo methods and tests Lead compounds Medicine Medicine & Public Health Mice Mice, Nude Mode of action Oncology Pharmacology/Toxicology Poisoning Short Report Studies Topoisomerase I Inhibitors - chemistry Topoisomerase I Inhibitors - pharmacology Tumor cell lines Tumor Cells, Cultured Xenograft Model Antitumor Assays Xenografts Xenotransplantation Topoisomerase I Fluoroquinolone Colon cancer DNA intercalator Topoisomerase II
ISSN:	0167-6997, 1573-0646, 1573-0646
Online Access:	Get full text
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