Ricolinostat suppresses proliferation, promotes apoptosis, and enhances the antiproliferative activity of topoisomerase inhibitors in cervical cancer cells
Sign Up to like & getrecommendations! Published in 2022 at "Drug Development Research"
DOI: 10.1002/ddr.21999
Abstract: Ricolinostat has been found to exhibit anticancer effects alone and in combination with various chemotherapeutic drugs in several cancer types. However, to the best of our knowledge, the efficacy of ricolinostat in cervical cancer is… read more here.
Keywords: cervical cancer; cancer; proliferation; topoisomerase inhibitors ... See more keywords
Recent advancements in the medicinal chemistry of bacterial type II topoisomerase inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104266
Abstract: Replication proteins are sought as a potential targets for antimicrobial agents. Despite their promising target characteristics, only topoisomerase II inhibitors targeting DNA gyrase and/or topoisomerase IV have reached clinical use. Topoisomerases are the enzymes that… read more here.
Keywords: topoisomerase inhibitors; medicinal chemistry; chemistry; recent advancements ... 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
Synthesis of podophyllotoxin linked β-carboline congeners as potential anticancer agents and DNA topoisomerase II inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.12.055
Abstract: A series of new podophyllotoxin linked β-carboline congeners have been synthesized by coupling various substituted β-carboline acids with 4β-aminopodophyllotoxin. Evaluation of their anticancer activity against a panel of human cancer cell lines such as lung… read more here.
Keywords: topoisomerase inhibitors; linked carboline; topoisomerase; cancer ... See more keywords
A comprehensive review of topoisomerase inhibitors as anticancer agents in the past decade.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.03.034
Abstract: The topoisomerase enzymes play an important role in DNA metabolism, and searching for enzyme inhibitors is an important target in the search for new anticancer drugs. Discovery of new anticancer chemotherapeutical capable of inhibiting topoisomerase… read more here.
Keywords: past decade; topoisomerase inhibitors; topoisomerase; review ... See more keywords
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00347
Abstract: Since their discovery over 5 decades ago, quinolone antibiotics have found enormous success as broad spectrum agents that exert their activity through dual inhibition of bacterial DNA gyrase and topoisomerase IV. Increasing rates of resistance,… read more here.
Keywords: topoisomerase inhibitors; gram negative; topoisomerase; resistance ... See more keywords
Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs)
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.9b01738
Abstract: The emergence of bacterial resistance against life-saving medicines has forced the scientific community and pharmaceutical industry to take actions in the quest for novel antibacterials. These should not only overcome the existing bacterial resistance but… read more here.
Keywords: novel bacterial; topoisomerase inhibitors; topoisomerase; inhibitors nbtis ... See more keywords
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00111
Abstract: Antibacterial resistance continues its devastation of available therapies. Novel bacterial topoisomerase inhibitors (NBTIs) offer one solution to this critical issue. Two series of amine NBTIs bearing tricyclic DNA-binding moieties as well as amide NBTIs with… read more here.
Keywords: bacterial topoisomerase; novel bacterial; dioxane linked; topoisomerase inhibitors ... See more keywords
Discovery of novel bacterial topoisomerase I inhibitors by use of in silico docking and in vitro assays
Sign Up to like & getrecommendations! Published in 2018 at "Scientific Reports"
DOI: 10.1038/s41598-018-19944-4
Abstract: Topoisomerases are important targets for antibacterial and anticancer therapies. Bacterial topoisomerase I remains to be exploited for antibiotics that can be used in the clinic. Inhibitors of bacterial topoisomerase I may provide leads for novel… read more here.
Keywords: topoisomerase inhibitors; vitro assays; topoisomerase; silico screening ... See more keywords
Ansavaricins F–I, new DNA topoisomerase inhibitors produced by Streptomyces sp. S012
Sign Up to like & getrecommendations! Published in 2017 at "RSC Advances"
DOI: 10.1039/c7ra00961e
Abstract: Ansamycins are a family of macrolactams characterized by an aromatic chromophore with an aliphatic chain (ansa chain) connected back to a nonadjacent position through an amide bond. In this study, four new polyketides of ansamycin… read more here.
Keywords: streptomyces s012; topoisomerase inhibitors; dna; dna topoisomerase ... See more keywords
Small DNA circles as bacterial topoisomerase I inhibitors
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DOI: 10.1039/c9ra02398d
Abstract: It is demonstrated that small DNA circles showed high inhibitory effect on the activity of bacterial topoisomerase I and the single-stranded regions associated with bending deformation are believed to be the crucial factor for trapping… read more here.
Keywords: circles bacterial; small dna; bacterial topoisomerase; dna circles ... See more keywords