New 1,2,4-oxadiazole/pyrrolidine hybrids as topoisomerase IV and DNA gyrase inhibitors with promising antibacterial activity.
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202100516
Abstract: A series of hybridized pyrrolidine compounds with a 1,2,4-oxadiazole moiety were synthesized to develop effective molecules against the enzymes DNA gyrase and topoisomerase IV (Topo IV). Compounds 8-20 were developed based on a previously disclosed… read more here.
Keywords: new oxadiazole; gyrase; activity; topoisomerase ... See more keywords
Novel substituted 1,8-naphthyridines: Design, synthesis, radiolabeling, and evaluation of apoptosis and topoisomerase II inhibition.
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202300035
Abstract: A series of seventeen 1,8-naphthyridine derivatives (5a-5q) conjugated at N1 to various substituted phenyl rings were designed and synthesized as potential topoisomerase II (Topo II) inhibitors. The antiproliferative activity of the target compounds against three… read more here.
Keywords: inhibition; apoptosis; naphthyridines design; topoisomerase ... See more keywords
Synthesis and Biological Activities of 11‐ and 12‐Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB and Tyrosyl‐DNA Phosphodiesterase 1 Inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "ChemMedChem"
DOI: 10.1002/cmdc.202200593
Abstract: Herein, a series of 11‐ or 12‐substituted benzophenanthridinone derivatives was designed and synthesized for the discovery of dual topoisomerase IB (TOP1) and tyrosyl‐DNA phosphodiesterase 1 (TDP1) inhibitors. Enzyme‐based assays indicated that two compounds 12 and… read more here.
Keywords: topoisomerase; dna phosphodiesterase; benzophenanthridinone derivatives; substituted benzophenanthridinone ... See more keywords
Synthesis, biological evaluation, and in silico studies of indole‐tethered pyrazoline derivatives as anticancer agents targeting topoisomerase IIα
Sign Up to like & getrecommendations! Published in 2022 at "Drug Development Research"
DOI: 10.1002/ddr.21976
Abstract: We herein report a new series of indole‐tethered pyrazoline derivatives as potent anticancer agents. A total of 12 compounds were designed and synthesized by conventional as well as microwave‐irradiated synthesis methods. The latter method results… read more here.
Keywords: anticancer agents; synthesis; topoisomerase; indole tethered ... See more keywords
Substitutions in Spodoptera exigua topoisomerase I modulate its relaxation activity and camptothecin sensitivity.
Sign Up to like & getrecommendations! Published in 2017 at "Pest management science"
DOI: 10.1002/ps.4440
Abstract: BACKGROUND Topoisomerase I (Top I) is referred as the cellular target of the camptothecins (CPTs) which are now being explored as potential pesticides for insect control. Three amino acid substitutions, including L530P, A653T and S729T,… read more here.
Keywords: relaxation; sensitivity; topoisomerase; spodoptera exigua ... See more keywords
Mapping E. coli Topoisomerase IV Binding and Activity Sites.
Sign Up to like & getrecommendations! Published in 2018 at "Methods in molecular biology"
DOI: 10.1007/978-1-4939-7459-7_6
Abstract: This methods article described a protocol aiming at mapping E. coli Topoisomerase IV (Topo IV) binding and cleavage activity sites on the genome. The approach is readily applicable to any Type II topoisomerase on a… read more here.
Keywords: activity sites; mapping coli; topoisomerase; topoisomerase binding ... See more keywords
Structural modification of ellipticine derivatives with alkyl groups of varying length is influential on their effects on human DNA topoisomerase II: a combined experimental and computational study
Sign Up to like & getrecommendations! Published in 2019 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-019-02472-9
Abstract: The compounds reducing tumor cell viability and disrupting DNA topoisomerase reactions have been widely used in anticancer drug development. Ellipticine (5,11-dimethyl-6H-pyrido[4,3-b]carbazole) is a potent intercalating agent that interferes with nucleic acid processing through interaction with… read more here.
Keywords: ellipticine derivatives; dna topoisomerase; topoisomerase; effects human ... See more keywords
The human DNA topoisomerase I mutant Gly717Asp: Higher religation rate is not always associated with camptothecin resistance.
Sign Up to like & getrecommendations! Published in 2019 at "Archives of biochemistry and biophysics"
DOI: 10.1016/j.abb.2019.01.007
Abstract: DNA topoisomerases are key enzyme responsible for modulating the topological state of the DNA by breaking and rejoining of DNA strand. Characterization of a Gly717Asp mutation in the human topoisomerase was performed using several catalytic… read more here.
Keywords: dna; gly717asp; drug; topoisomerase ... See more keywords
Structural optimizations and bioevaluation of N-substituted acridone derivatives as strong topoisomerase II inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.105543
Abstract: Previously, an array of N-substituted acridone derivatives have been reported as potent topoisomerase II (topo II) inhibitors, and preliminary structure-activity relationship (SAR) outcomes revealed that the linker between 1-NH and N-methyl piperazine motif of the… read more here.
Keywords: structural optimizations; optimizations bioevaluation; acridone derivatives; acridone ... See more keywords
Biological evaluation of a halogenated triterpenoid, 2α-bromo-dihydrobelulonic acid as inhibitor of human topoisomerase IIα and HeLa cell proliferation.
Sign Up to like & getrecommendations! Published in 2017 at "Chemico-biological interactions"
DOI: 10.1016/j.cbi.2017.02.015
Abstract: BACKGROUND The pentacyclic lupane-type (6-6-6-6-5 type) triterpenoid, Betulinic acid (BA) is a potent inhibitor of topoisomerases and is of immense interest as anticancer drugs. However, the compound being highly lipophilic, has limited in vivo uptake capacity.… read more here.
Keywords: hela cell; inhibitor; cell proliferation; topoisomerase ... See more keywords
Synthesis, evaluation, and CoMFA study of fluoroquinophenoxazine derivatives as bacterial topoisomerase IA inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.09.053
Abstract: New antibacterial agents with novel target and mechanism of action are urgently needed to combat problematic bacterial infections and mounting antibiotic resistances. Topoisomerase IA represents an attractive and underexplored antibacterial target, as such, there is… read more here.
Keywords: topoisomerase inhibitors; comfa; study; fluoroquinophenoxazine derivatives ... See more keywords