Probing structural requirements for human topoisomerase I inhibition by a novel N1-Biphenyl fluoroquinolone

Fluoroquinolones substituted with N-1 biphenyl and napthyl groups were discovered to act as catalytically inhibitors of human topoisomerases I and II, and to possess anti-proliferative activity in vivo. Structural requirements for these novel quinolones to inhibit catalytic activity of human topoiso...

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Veröffentlicht in:	European journal of medicinal chemistry Jg. 172; S. 109 - 130
Hauptverfasser:	Delgado, Justine L., Lentz, Sarah R.C., Kulkarni, Chaitanya A., Chheda, Pratik R., Held, Hailey A., Hiasa, Hiroshi, Kerns, Robert J.
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	ISSY-LES-MOULINEAUX Elsevier Masson SAS 15.06.2019 Elsevier
Schlagworte:	Anti-cancer Biphenyl Compounds - chemical synthesis Biphenyl Compounds - chemistry Biphenyl Compounds - pharmacology Catalytic inhibitors Chemistry, Medicinal DNA Topoisomerases, Type I - metabolism Dose-Response Relationship, Drug Fluoroquinolones Fluoroquinolones - chemical synthesis Fluoroquinolones - chemistry Fluoroquinolones - pharmacology hTopoI inhibitor Humans Life Sciences & Biomedicine Molecular Structure Pharmacology & Pharmacy Science & Technology Structure-Activity Relationship Topoisomerase Topoisomerase I Inhibitors - chemical synthesis Topoisomerase I Inhibitors - chemistry Topoisomerase I Inhibitors - pharmacology Fluoroquinolones Topoisomerase hTopoI inhibitor Anti-cancer Catalytic inhibitors MECHANISM BIPHENYL ROLES MODE hTopol inhibitor DNA GYRASE DERIVATIVES
ISSN:	0223-5234, 1768-3254, 1768-3254
Online-Zugang:	Volltext
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