Results 181 to 190 of about 29,245 (221)

Topoisomerase I and II Inhibitors: A Patent Review

Recent Patents on Anti-Cancer Drug Discovery, 2016
Topoisomerases are a set of nuclear enzymes that play a vital role in handling of topological consequences of DNA during various genetic activities necessary for vitality of cell. Inhibition of these enzymes consequently leads to the blockage of ligation step of the cell cycle which generates single and double strand breakage in DNA strand ...
Arshdeep, Singh, Navdeep, Kaur, Gurpreet, Singh, Pooja, Sharma, Pms, Bedi, Sahil, Sharma, Kunal, Nepali   +6 more
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Synthesis of the topoisomerase II inhibitor BE 10988

Tetrahedron Letters, 1993
Abstract The naturally occurring indoloquinone BE 10988 1 , an inhibitor of topoisomerase II, has been synthesised in an overall yield of 28%.
Christopher J. Moody, Elizabeth Swann
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DNA Topoisomerase II Inhibitors

1997
DNA topoisomerases represent a major focus of research not only for cancer chemotherapy, but also for gene regulation, cell cycle, mitosis, and chromosome structure. A number of reviews have been written on the subject (1–8).
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Dual topoisomerase I/II inhibitors

Journal of Oncology Pharmacy Practice, 2000
Topoisomerase (topo) I and II are nuclear enzymes, which play a major role in the topological rearrangement of DNA during replication and transcription processes. In the course of years, many different agents have been found which can inhibit the topos and thereby exploit cytotoxicity, also against tumour cells.
R. van Gijn, R.R.H. Lendfers, J.H.M. Schellens, A. Bult, J.H. Beijnen   +4 more
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HToPred: A Tool for Human Topoisomerase II Inhibitor Prediction

Molecular Informatics, 2018
AbstractThe enzyme human topoisomerase IIα (hTopoIIα) is an important anticancer drug target. Due to the availability of multiple inhibitor‐binding sites in this enzyme, the anti‐hTopoII agents possess high chemical diversity. Chemoinformatics methods can be used to identify lead compounds from large databases for hTopoII inhibitory activity and ...
Neha Tripathi, Naeem Shaikh, Prasad V. Bharatam, Prabha Garg   +3 more
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Genotoxicity of several clinically used topoisomerase II inhibitors

Toxicology Letters, 2000
DNA topoisomerase II is an essential nuclear enzyme that modulates DNA topology during multiple cellular processes such as DNA replication and chromosome segregation. Several important clinical antitumor drugs and antibiotics act through inhibition of topoisomerase II.
G, Boos, H, Stopper
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Tannins as Potent Inhibitors of DNA Topoisomerase II In Vitro

Journal of Pharmaceutical Sciences, 1993
Fifty-two out of 60 tannins, including gallo-, ellagi-, condensed, and complex tannins, are inhibitors of human DNA topoisomerase II in vitro. Thirty-six compounds that completely inhibited enzyme activity at a concentration of 500 nM or less, as assessed by ATP-dependent unknotting of P4 phage DNA, were at least 100-fold more potent than the ...
Y, Kashiwada, G, Nonaka, I, Nishioka, K J, Lee, I, Bori, Y, Fukushima, K F, Bastow, K H, Lee   +7 more
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Topoisomerase II Inhibitors: Chemical Biology

2011
DNA topoisomerase II (Top2) is the target of a chemically diverse set of compounds with substantial antitumor activity. Agents such as doxorubicin and etoposide are FDA approved for the treatment of both leukemias and solid tumors. Most clinically active drugs targeting Top2 lead to elevated levels of covalent Top2-cleaved DNA complexes and exert their
Anna Rogojina, Stefan Gajewski, Karim Bahmed, Neil Osheroff, John L. Nitiss   +4 more
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Topoisomerase II Inhibitors in Cancer Treatment

International Journal of Pharmaceutical Sciences and Nanotechnology, 2011
Topoisomerase II constitutes a family of nuclear enzymes essential to all living cells. These enzymes are capable of transferring one DNA double helix through a transient break in another DNA double helix. Type II topoisomerases play important roles in DNA metabolic processes, in which they are involved in DNA replication, transcription, chromosome ...
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Pyrroloquinolinone-based dual topoisomerase I/II inhibitor

European Journal of Medicinal Chemistry, 2014
A new series of pyrroloquinolinones bearing different alkylamino side chains were synthesized and evaluated as cytotoxic compounds against three different human tumor cell lines (HeLa, HL-60 and A431). Some compounds showed interesting antiproliferative activity, in particular against A431 cells.
DALLA VIA, LISA, MARZARO, GIOVANNI, FERRARESE, ALESSANDRO, GIA, ORNELLA MARIA, CHILIN, ADRIANA   +4 more
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