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The design and discovery of topoisomerase I inhibitors as anticancer therapies

Expert Opinion on Drug Discovery, 2022
Endika Martin-Encinas   +2 more
exaly  

Topoisomerase I inhibitors

Drugs & Therapy Perspectives, 1995
openaire   +1 more source

Topoisomerase I Inhibitors: Chemical Biology

2011
Topoisomerase I (Top1), an essential enzyme, produces a DNA single-strand break allowing DNA relaxation for replication. The enzymatic mechanism involves sequential transesterifications and the reaction is freely reversible. The Top1 reaction intermediate consists of enzyme covalently linked to DNA, thus a “cleavable complex”. Covalently bound Top1-DNA
openaire   +1 more source

Mutagenic activity of topoisomerase I inhibitors

Clinical cancer research : an official journal of the American Association for Cancer Research
Topoisomerase I-directed agents are now in Phase I and II clinical trials and show great promise as potentially important agents for cancer chemotherapy. Because of their mechanism of action they may also be potential mutagens; however, their mutagenicity and oncogenicity still remain to be elucidated.
, Hashimoto, , Chatterjee, , Berger
openaire   +1 more source

The clinical pharmacology of topoisomerase I inhibitors.

Seminars in hematology, 1999
The Chinese tree Camptotheca acuminata, or Xi Shu, brings us a unique class of chemotherapeutic agents known as the camptothecins. Because the parent compound exhibited excessive toxicity and poor aqueous solubility, synthetic and semisynthetic analogs were developed.
openaire   +1 more source

Metal complexes as topoisomerase inhibitors

Inorganica Chimica Acta, 2022
V Badireenath Konkimalla   +1 more
exaly  

Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors

ACS Medicinal Chemistry Letters, 2015
Shipeng He, Guoqiang Dong, Wei Chen
exaly  

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