Results 31 to 40 of about 32,790 (255)

Fluoroquinolones as HIV-1 integrase, topoisomerase I and II inhibitors.

, 2023
Fluoroquinolones as HIV-1 integrase, topoisomerase I and II inhibitors.
Kulsoom Ghulam Ali (14992580), Zohaib Raza (9186430), Ameer Fawad Zahoor (10728633), Samreen Gul Khan (14992577), Asim Mansha (1290051), Rabia Akhtar (14992574), Shagufta Kamal (13565544)   +6 more
core   +1 more source

A Novel Copper(II) Indenoisoquinoline Complex Inhibits Topoisomerase I, Induces G2 Phase Arrest, and Autophagy in Three Adenocarcinomas

Frontiers in Oncology, 2022
Topoisomerases, targets of inhibitors used in chemotherapy, induce DNA breaks accumulation leading to cancer cell death. A newly synthesized copper(II) indenoisoquinoline complex WN197 exhibits a cytotoxic effect below 0.5 µM, on MDA-MB-231, HeLa, and HT-
Caroline Molinaro, Nathalie Wambang, Till Bousquet, Anne-Sophie Vercoutter-Edouart, Lydie Pélinski, Katia Cailliau, Alain Martoriati   +6 more
doaj   +1 more source

Small-Molecule Inhibitors Targeting Topoisomerase I as Novel Antituberculosis Agents

, 2016
Bacterial topoisomerase functions are required for regulation of DNA supercoiling and overcoming the DNA topological barriers that are encountered during many vital cellular processes.
Sandhaus, Shayna, Tse-Dinh, Yuk-Ching, Gupta, Rashmi, Rohde, Kyle H, Welmaker, Greg, Houghten, Richard A, Annamalai, Thirunavukkarasu, Garcia, Pamela K, Giulianotti, Marc A, Netherton, Mandy, Narula, Gagandeep, Paz, Carlos, Geden, Sandra, Andres, Angelo, Rodrigues Felix, Carolina   +14 more
core   +2 more sources

Novel DNA topoisomerase IIα inhibitors from combined ligand- and structure-based virtual screening.

PLoS ONE, 2014
DNA topoisomerases are enzymes responsible for the relaxation of DNA torsional strain, as well as for the untangling of DNA duplexes after replication, and are important cancer drug targets.
Malgorzata N Drwal, Jessica Marinello, Stefano G Manzo, Laurence P G Wakelin, Giovanni Capranico, Renate Griffith   +5 more
doaj   +1 more source

Heterocyclic bibenzimidazole derivatives as topoisomerase I inhibitors [PDF]

Bioorganic & Medicinal Chemistry Letters, 2000
A series of 2'-heterocyclic derivatives of 5-phenyl-2,5'-1H-bibenzimidazoles were evaluated for topoisomerase I poisoning activity and cytotoxicity. Topo I poisoning activity was associated with 2'-derivatives that possessed a hydrogen atom capable of hydrogen bond formation, suggesting that the interatomic distances between such hydrogen atoms and the
Jin, S., Kim, J.S., Sim, S.P, Liu, A., Pilch, D.S., Liu, L.F., LaVoie, E.J.   +6 more
openaire   +2 more sources

Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold

, 2019
A new class of topoisomerase I inhibitors containing the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one (abbreviated as BBPI) ring system have been developed based on structure-activity relationship studies of the cytotoxic marine alkaloid ...
Iwao, Masatomo, Fujimoto, Masahiro, Ishibashi, Fumito, Okazaki, Fumiyasu, Nanjo, Yusuke, Yoshida, Kenyu, Fukuda, Tsutomu, Natsui, Yuko, To, Hideto   +8 more
core   +1 more source

Inhibition of Topoisomerase (DNA) I (TOP1): DNA Damage Repair and Anticancer Therapy

Biomolecules, 2015
Most chemotherapy regimens contain at least one DNA-damaging agent that preferentially affects the growth of cancer cells. This strategy takes advantage of the differences in cell proliferation between normal and cancer cells.
Yang Xu, Chengtao Her
doaj   +1 more source

Hybrid topoisomerase I and HDAC inhibitors as dual action anticancer agents. [PDF]

PLoS ONE, 2018
Recent studies have shown that HDAC inhibitors act synergistically with camptothecin derivatives in combination therapies. To exploit this synergy, new hybrid molecules targeting simultaneously topoisomerase I and HDAC were designed.
Raffaella Cincinelli, Loana Musso, Roberto Artali, Mario B Guglielmi, Ilaria La Porta, Carmela Melito, Fabiana Colelli, Francesco Cardile, Giacomo Signorino, Alessandra Fucci, Martina Frusciante, Claudio Pisano, Sabrina Dallavalle   +12 more
doaj   +1 more source

Proteasome inhibitor, ixazomib prevents topoisomerase‐I degradation and reverses irinotecan resistance in colorectal cancer

Molecular Oncology, EarlyView.
Ixazomib inhibits proteasome‐mediated degradation of topoisomerase I induced by irinotecan, thereby restoring drug sensitivity and promoting tumor cell death in colorectal cancer. Irinotecan, a topoisomerase I (topoI) inhibitor, is widely used for colorectal cancer, but resistance remains a major clinical challenge.
Yuho Ebata, Koji Ando, Hirofumi Hasuda, Koshi Mimori, Elizabeth C. Unan, Siddhartha Pulukuri, Aahana Tiku, Allison Berger, Eiji Oki, Ajit Bharti, Tomoharu Yoshizumi   +10 more
wiley   +1 more source

Antibacterial activity of a DNA topoisomerase I inhibitor versus fluoroquinolones in Streptococcus pneumoniae.

PLoS ONE, 2020
The DNA topoisomerase complement of Streptococcus pneumoniae is constituted by two type II enzymes (topoisomerase IV and gyrase), and a single type I enzyme (topoisomerase I).
Myriam V Valenzuela, Mirian Domenech, Patricia Mateos-Martínez, Fernando González-Camacho, Adela G de la Campa, Maria Teresa García   +5 more
doaj   +1 more source