Novel thiazolotriazole and triazolothiadiazine scaffolds as selective tumor associated carbonic anhydrase inhibitors endowed with cathepsin B inhibition
Sign Up to like & getrecommendations! Published in 2024 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202400366
Abstract: The present research focused on the tail‐approach synthesis of novel extended thiazolotriazoles (8a–8j) and triazolothiadiazines (11a–11j) including aminotriazole intermediate 10. After successful synthesis, all the compounds were evaluated for their inhibition potential against cytosolic isoforms… read more here.
Keywords: hca xii; carbonic anhydrase; inhibition; thiazolotriazole triazolothiadiazine ... See more keywords
New 7‐hydroxycoumarin acetamide derivatives as human carbonic anhydrase IX and XII inhibitors: Design, synthesis, biological evaluation and molecular docking studies
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DOI: 10.1002/ardp.202400482
Abstract: Carbonic anhydrases (CAs) are crucial in regulating various physiological processes in the body. The overexpression of isoforms human carbonic anhydrases (hCA) IX and hCA XII is linked to tumour progression. The selective inhibition of CA… read more here.
Keywords: hca xii; carbonic anhydrase; xii; human carbonic ... See more keywords
Synthesis and biological evaluation of some coumarin hybrids as selective carbonic anhydrase IX and XII inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104272
Abstract: Two series, coumarin-linked to thiazolidinone via a pyrazole linker (6a-m, Series 1) and coumarin-linked 1,2,3-triazoles (5a-j, Series 2) were synthesized and the synthesized compounds were subjected for evaluation against the four physiologically and pharmacologically relevant… read more here.
Keywords: coumarin; xii inhibitors; inhibition; series ... See more keywords
5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.04.072
Abstract: Sixteen 5-aryl-substituted isothiazol-3(2H)-one-1,(1)-(di)oxide analogs have been prepared from the corresponding 5-chloroisothiazol-3(2H)-one-1-oxide or -1,1-dioxide by a Suzuki-Miyaura cross-coupling reaction and screened for their inhibition potency against four human carbonic anhydrase isoenzymes: the transmembrane tumor-associated hCA IX and… read more here.
Keywords: arylisothiazol one; hca xii; inhibition; tumor associated ... See more keywords
Natural inspired ligustrazine-based SLC-0111 analogues as novel carbonic anhydrase inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.114008
Abstract: Ligustrazine is the principle bioactive alkaloid in the widely-used Chinese herb Chuan Xiong rhizome. Herein, a series of novel derivatives has been designed as human carbonic anhydrases inhibitors (hCAIs) starting from the natural product Ligustrazine… read more here.
Keywords: hca xii; slc 0111; hca; inspired ligustrazine ... 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
4-(Pyrazolyl)benzenesulfonamide Ureas as Carbonic Anhydrases Inhibitors and Hypoxia-Mediated Chemo-Sensitizing Agents in Colorectal Cancer Cells
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.4c01894
Abstract: Hypoxia in tumors contributes to chemotherapy resistance, worsened by acidosis driven by carbonic anhydrases (hCA IX and XII). Targeting these enzymes can mitigate acidosis, thus enhancing tumor sensitivity to cytotoxic drugs. Herein, novel 4-(pyrazolyl)benzenesulfonamide ureas… read more here.
Keywords: colorectal cancer; cancer cells; hca xii; carbonic anhydrases ... See more keywords
Design, Synthesis, and In Vitro Anticancer Evaluation of Thiazole-Based Chalcones Linked to Sulfanilamide as Tumor-Associated Carbonic Anhydrase IX and XII Inhibitors.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c01392
Abstract: Human carbonic anhydrases IX and XII (hCA IX/XII) are overexpressed in various solid tumors and play critical roles in tumor survival and progression, particularly under hypoxic conditions. In this study, a tail-focused design strategy was… read more here.
Keywords: hca xii; anticancer; xii; tumor associated ... See more keywords
Novel benzofuran-based sulphonamides as selective carbonic anhydrases IX and XII inhibitors: synthesis and in vitro biological evaluation
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2019.1697250
Abstract: Abstract Pursuing on our efforts toward searching for efficient hCA IX and hCA XII inhibitors, herein we report the design and synthesis of new sets of benzofuran-based sulphonamides (4a,b, 5a,b, 9a–c, and 10a–d), featuring the… read more here.
Keywords: based sulphonamides; xii inhibitors; novel benzofuran; hca xii ... See more keywords
S-substituted 2-mercaptoquinazolin-4(3H)-one and 4-ethylbenzensulfonamides act as potent and selective human carbonic anhydrase IX and XII inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2020.1742117
Abstract: Abstract We evaluated the hCA (CA, EC 4.2.1.1) inhibitory activity of novel 4-(2-(2-substituted-thio-4-oxoquinazolin-3(4H)-yl)ethyl)benzenesulfonamides (compounds 2–20) towards the isoforms I, II, IX, and XII. hCA Isoforms were effectively inhibited by most of new compounds comparable to… read more here.
Keywords: hca selectivity; hca xii; hca; selective hca ... See more keywords
Isocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2041630
Abstract: Abstract Isocoumarins, isomeric to comarins which act as effective carbonic anhydrase (CA, EC 4.2.1.1) inhibitors, were investigated for the first time as inhibitors of this enzyme. A series of 3-substituted and 3,4-disubstituted isocoumarins incorporating phenylhydrazone,… read more here.
Keywords: new class; xii; carbonic anhydrase; hca xii ... See more keywords