Topoisomerase I inhibitors: Challenges, progress and the road ahead

A Talukdar, B Kundu, D Sarkar, S Goon… - European Journal of …, 2022 - Elsevier
Abstract Topoisomerase IB (Top1), a subcategory of DNA topoisomerase enzymes is
expressed much higher in several tumor cells. Therefore, modulating the activity of Top1 in …

Palladium‐Catalyzed C3 or C4 Direct Arylation of Heteroaromatic Compounds with Aryl Halides by C H Bond Activation

J Roger, AL Gottumukkala, H Doucet - ChemCatChem, 2010 - Wiley Online Library
In recent years, palladium‐catalyzed direct C2 or C5 arylation of heteroaromatic compounds
with aryl halides by C H bond activation has become a popular method for generating …

Nitro-group-containing drugs

K Nepali, HY Lee, JP Liou - Journal of medicinal chemistry, 2018 - ACS Publications
The nitro group is considered to be a versatile and unique functional group in medicinal
chemistry. Despite a long history of use in therapeutics, the nitro group has toxicity issues …

DNA topoisomerases as molecular targets for anticancer drugs

K Buzun, A Bielawska, K Bielawski… - Journal of Enzyme …, 2020 - Taylor & Francis
The significant role of topoisomerases in the control of DNA chain topology has been
confirmed in numerous research conducted worldwide. The prevalence of these enzymes …

Type i DNA topoisomerases

G Capranico, J Marinello… - Journal of medicinal …, 2017 - ACS Publications
DNA topoisomerases constitute a large family of enzymes that are essential for all domains
of life. Although they share general reaction chemistry and the capacity to govern DNA …

Overcoming tumor multidrug resistance using drugs able to evade P‐glycoprotein or to exploit its expression

S Nobili, I Landini, T Mazzei… - Medicinal research reviews, 2012 - Wiley Online Library
Multidrug resistance (MDR) is a major obstacle to the effective treatment of cancer. Cellular
overproduction of P‐glycoprotein (P‐gp), which acts as an efflux pump for various anticancer …

In vitro and in vivo evaluation of recombinant silk-elastinlike hydrogels for cancer gene therapy

Z Megeed, M Haider, D Li, BW O'Malley Jr… - Journal of Controlled …, 2004 - Elsevier
The objectives of this study were to evaluate:(i) the influences of hydrogel geometry, DNA
molecular weight, and DNA conformation on DNA release from a silk-elastinlike protein …

Next generation topoisomerase I inhibitors: Rationale and biomarker strategies

BA Teicher - Biochemical pharmacology, 2008 - Elsevier
Topoisomerase I (TopoI), an essential enzyme, produces a DNA single strand break
allowing DNA relaxation for replication. The enzymatic mechanism involves sequential …

Topoisomerase inhibitors as anticancer agents: a patent update

DB Khadka, WJ Cho - Expert opinion on therapeutic patents, 2013 - Taylor & Francis
Introduction: Topoisomerases (topos) are nuclear enzymes that resolve topological
problems associated with DNA during various genetic processes. The essential role of topos …

5-(2-Aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones:  Variation of N-Alkyl Substituents Modulates Sensitivity to Efflux Transporters Associated with Multidrug …

AL Ruchelman, PJ Houghton, N Zhou… - Journal of medicinal …, 2005 - ACS Publications
5 H-8, 9-Dimethoxy-5-(2-N, N-dimethylaminoethyl)-2, 3-methylenedioxydibenzo [c, h][1, 6]
naphthyridin-6-one (ARC-111) has potent TOP1-targeting activity and pronounced antitumor …