Novel benzenesulfonamide‐thiouracil conjugates with a flexible N‐ethyl acetamide linker as selective CA IX and CA XII inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200434
Abstract: Novel benzenesulfonamide derivatives linked to diverse functionalized thiouracils through a flexible N‐ethyl acetamide linker were designed and synthesized as carbonic anhydrase (CA) inhibitors. The synthesized candidates demonstrated a potent inhibitory activity against four different CA… read more here.
Keywords: novel benzenesulfonamide; xii; acetamide linker; linker ... See more keywords
A Series of Thiadiazolyl‐Benzenesulfonamides Incorporating an Aromatic Tail as Isoform‐Selective, Potent Carbonic Anhydrase II/XII Inhibitors
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DOI: 10.1002/cmdc.202200056
Abstract: We describe the synthesis of a series of thiadiazolyl‐benzenesulfonamide derivatives carrying an aromatic tail linked by an amide linker (12–34), as human carbonic anhydrase (hCA) inhibitors. These thiadiazol derivatives were evaluated against four physiologically relevant… read more here.
Keywords: series thiadiazolyl; xii; carbonic anhydrase; aromatic tail ... See more keywords
Anti‐inflammatory activities of natural cyclopeptide RA‐XII in colitis‐associated colon cancer mouse model and its effect on gut microbiome
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DOI: 10.1002/ptr.7482
Abstract: Colorectal cancer (CRC), the third most common cancer globally, is associated with intestinal inflammation that leads to poor prognosis. RA‐XII, a natural cyclopeptide, has previously been reported to possess anti‐tumor activities. Here, the anti‐inflammatory activities… read more here.
Keywords: xii; colitis associated; anti inflammatory; colon cancer ... See more keywords
Synthesis of novel dipeptide sulfonamide conjugates with effective carbonic anhydrase I, II, IX, and XII inhibitory properties.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.08.032
Abstract: Twenty-four novel sulfonamide derivatives incorporating dipeptide tails were synthesized by facile acylation reactions of homosulfanilamide through benzotriazole or dicyclohexyl carbodiimide (DCC) mediated coupling reactions. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new… read more here.
Keywords: carbonic anhydrase; dipeptide; inhibitory properties; xii ... See more keywords
Inhibitory effects and structural insights for a novel series of coumarin-based compounds that selectively target human CA IX and CA XII carbonic anhydrases.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.11.061
Abstract: Coumarin derivatives are a peculiar class of inhibitors of the family of metalloenzymes carbonic anhydrases (CA, EC 4.2.1.1). Several coumarins display higher affinity and selectivity toward most relevant and druggable CA isoforms. By decorating the… read more here.
Keywords: coumarin based; coumarin; series coumarin; carbonic anhydrases ... See more keywords
Inclusion of a 5-fluorouracil moiety in nitrogenous bases derivatives as human carbonic anhydrase IX and XII inhibitors produced a targeted action against MDA-MB-231 and T47D breast cancer cells.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112112
Abstract: A new series of pyrimidine derivatives as human carbonic anhydrases (CA, EC 4.2.1.1) inhibitors is here designed by including a 5-fluorouracil (5-FU) moiety, broadly used anticancer medication, in nitrogenous base modulators of the tumor-associated CAs.… read more here.
Keywords: human carbonic; derivatives human; xii; fluorouracil moiety ... See more keywords
Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112219
Abstract: Two new series of 1,3,4-oxadiazole benzenesulfonamide hybrids 3 and 4, having twenty novel compounds, have been designed and synthesized in order to assess their inhibition potential as CAIs against hCA I, II, IX, and XII.… read more here.
Keywords: chemistry; tail approach; xii; hca isoform ... See more keywords
Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112449
Abstract: In the present work, we report the design and synthesis of a set of iodinated quinazolinones carrying benzenesulfonamide moiety as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The target compounds showed promising inhibitory activity against the… read more here.
Keywords: carbonic anhydrase; radiosensitizing activity; xii; hca ... See more keywords
Céphalées, sténose bilatérale des carotides et parésie du XII isolés révélant une granulomatose avec polyangéite
Sign Up to like & getrecommendations! Published in 2017 at "Revue Neurologique"
DOI: 10.1016/j.neurol.2017.01.167
Abstract: Introduction La granulomatose avec polyangeite (GPA/Wegener) est une vascularite necrosante systemique des petits vaisseaux. L’atteinte neurologique centrale combine classiquement une meningite lymphocytaire et une atteinte multiple de nerfs crâniens. Observation Une patiente de 54 ans, sans… read more here.
Keywords: espaces carotidiens; des carotides; gauche; phal nose ... See more keywords
New Dual P-Glycoprotein (P-gp) and Human Carbonic Anhydrase XII (hCA XII) Inhibitors as Multidrug Resistance (MDR) Reversers in Cancer Cells
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01175
Abstract: In a continuing search of dual P-gp and hCA XII inhibitors, we synthesized and studied new N,N-bis(alkanol)amine aryl diester derivatives characterized by the presence of a coumarin group. These hybrids contain both P-gp and hCA… read more here.
Keywords: mdr; xii; cancer cells; hca xii ... See more keywords
Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.7b00229
Abstract: We report the synthesis, biological evaluation, and structural study of a series of substituted heteroaryl-pyrazole carboxylic acid derivatives. These compounds have been developed as inhibitors of specific isoforms of carbonic anhydrase (CA), with potential as… read more here.
Keywords: carbonic anhydrase; exploring heteroaryl; pyrazole carboxylic; carboxylic acids ... See more keywords