The synthesis of furoquinolinedione and isoxazoloquinolinedione derivatives as selective Tyrosyl-DNA phosphodiesterase 2 (TDP2) inhibitors

Suppression of Drug-Resistant Non-Small-Cell Lung Cancer with Inhibitors Targeting Minichromosomal Maintenance Protein

(2020) Chia-Yi Lin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Deazaflavin Inhibitors of TDP2 with Cellular Activity Can Affect Etoposide Influx and/or Efflux

(2019) Emilia Komulainen et al.   ACS Chemical Biology

Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide

(2019) Jayakanth Kankanala et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Simplified Sampangine Derivatives with Potent Antifungal Activities against Cryptococcal Meningitis

(2019) Zhuang Li et al.   ACS Infectious Diseases

Novel deazaflavin tyrosyl-DNA phosphodiesterase 2 (TDP2) inhibitors

(2019) Evgeny Kiselev et al.   DNA REPAIR

Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2)

(2018) Le-Mao Yu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, cytotoxicity and structure-activity relationship of indolizinoquinolinedione derivatives as DNA topoisomerase IB catalytic inhibitors

(2018) Qian Yu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

New fluorescence-based high-throughput screening assay for small molecule inhibitors of tyrosyl-DNA phosphodiesterase 2 (TDP2)

(2018) Carlos J.A. Ribeiro et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Design, synthesis and biological evaluation N2-(2-alkyoxy-6-aliphatic aminopyridin-3-yl)-2,4-diaminepyrimidine derivatives bearing acylamino or DBTD ‘head’ as potential ALK inhibitors

(2018) Lingyun Xing et al.   BIOORGANIC CHEMISTRY

Triazolopyrimidine and triazolopyridine scaffolds as TDP2 inhibitors

(2018) Carlos J.A. Ribeiro et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl–DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl–DNA Phosphodiesterase 2 (Tdp2)

(2017) Ping Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Deazaflavin Inhibitors of Tyrosyl-DNA Phosphodiesterase 2 (TDP2) Specific for the Human Enzyme and Active against Cellular TDP2

(2016) Christophe Marchand et al.   ACS Chemical Biology

Mode of action of DNA-competitive small molecule inhibitors of tyrosyl DNA phosphodiesterase 2

(2016) P. Hornyak et al.   BIOCHEMICAL JOURNAL

Discovery of selective inhibitors of tyrosyl-DNA phosphodiesterase 2 by targeting the enzyme DNA-binding cleft

(2016) Bradley R. Kossmann et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Depletion of tyrosyl DNA phosphodiesterase 2 activity enhances etoposide-mediated double-strand break formation and cell killing

(2016) Yasemin Saygideger Kont et al.   DNA REPAIR

Isoquinoline-1,3-diones as Selective Inhibitors of Tyrosyl DNA Phosphodiesterase II (TDP2)

(2016) Jayakanth Kankanala et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tyrosyl-DNA-phosphodiesterases (TDP1 and TDP2)

(2014) Yves Pommier et al.   DNA REPAIR

Toxoflavins and Deazaflavins as the First Reported Selective Small Molecule Inhibitors of Tyrosyl-DNA Phosphodiesterase II

(2013) Ali Raoof et al.   JOURNAL OF MEDICINAL CHEMISTRY

Iodine(III)-Mediated [3 + 2] Cyclization for One-Pot Synthesis of Benzo[d]isoxazole-4,7-diols in Aqueous Medium

(2013) Yingwei Hou et al.   JOURNAL OF ORGANIC CHEMISTRY

TDP2–Dependent Non-Homologous End-Joining Protects against Topoisomerase II–Induced DNA Breaks and Genome Instability in Cells and In Vivo

(2013) Fernando Gómez-Herreros et al.   PLoS Genetics

Mutant p53 cooperates with ETS2 to promote etoposide resistance

(2012) P. M. Do et al.   GENES & DEVELOPMENT

Biochemical Characterization of Human Tyrosyl-DNA Phosphodiesterase 2 (TDP2/TTRAP)

(2012) Rui Gao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Tyrosyl DNA phosphodiesterase 2, an enzyme fit for purpose

(2012) Keith W. Caldecott   NATURE STRUCTURAL & MOLECULAR BIOLOGY

An RNA virus hijacks an incognito function of a DNA repair enzyme

(2012) R. Virgen-Slane et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Design, Synthesis, and Cytotoxicity of Indolizinoquinoxaline-5,12-dione Derivatives, Novel DNA Topoisomerase IB Inhibitors

(2010) De-Qing Shen et al.   AUSTRALIAN JOURNAL OF CHEMISTRY

The anti-cancer, anti-inflammatory and tuberculostatic activities of a series of 6,7-substituted-5,8-quinolinequinones

(2010) Benjamin J. Mulchin et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors

(2010) De-Qing Shen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

TDP2/TTRAP Is the Major 5′-Tyrosyl DNA Phosphodiesterase Activity in Vertebrate Cells and Is Critical for Cellular Resistance to Topoisomerase II-induced DNA Damage

(2010) Zhihong Zeng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

New Substructure Filters for Removal of Pan Assay Interference Compounds (PAINS) from Screening Libraries and for Their Exclusion in Bioassays

(2010) Jonathan B. Baell et al.   JOURNAL OF MEDICINAL CHEMISTRY

4-Pregnen-21-ol-3,20-dione-21-(4-bromobenzenesufonate) (NSC 88915) and Related Novel Steroid Derivatives as Tyrosyl-DNA Phosphodiesterase (Tdp1) Inhibitors

(2009) Thomas S. Dexheimer et al.   JOURNAL OF MEDICINAL CHEMISTRY

A human 5′-tyrosyl DNA phosphodiesterase that repairs topoisomerase-mediated DNA damage

(2009) Felipe Cortes Ledesma et al.   NATURE

Synthesis, cytotoxic activities and structure–activity relationships of topoisomerase I inhibitors: Indolizinoquinoline-5,12-dione derivatives

(2008) Yu Cheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

DNA cleavage assay for the identification of topoisomerase I inhibitors

(2008) Thomas S Dexheimer et al.   Nature Protocols