Institution Author
Now showing items 1-20 of 25
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Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors.
RUCKTOOA, P; JONGEJAN, A; Akdemir, ATİLLA; de, Esch; de, Graaf; LEURS, R; SMIT, AB; BERTRAND, D; SIXMA, TK; BERTRAND, S; ELK, RV (2011-10-15) -
Anti-Candida activity and cytotoxicity of a large library of new N-substituted-1,3-thiazolidin-4-one derivatives.
BIZZARRI, B; MARI, E; ZICARI, A; CARRADORI, S; BOLASCO, A; Akdemir, ATİLLA; De, Monte; SECCI, D; RIVANERA, D; MOLLICA, A; CAPRARA, F (2016-01-01) -
Anticholinesterase and Antioxidant Activities of Natural Abietane Diterpenoids with Molecular Docking Studies
TOPÇU, GÜLAÇTI; AKDEMİR, ATİLLA; Kolak, Ufuk; Ozturk, Mehmet; Boga, Mehmet; BAHADORİ, FATEMEH; Cakmar, Seda Damla Hatipoglu (2020-01-01)Background: Alzheimer-s Disease (AD) is one of the most prevalent causes of dementia in the world, and no drugs available that can provide a complete cure. Cholinergic neurons of the cerebral cortex of AD patients are lost ... -
Aromatase inhibition by 2-methyl indole hydrazone derivatives evaluated via molecular docking and in vitro activity studies.
OZCAN-SEZER, S; INCE, E; Akdemir, ATİLLA; CEYLAN, ÖÖ; Suzen, S; GURER-ORHAN, H (2019-05-01)A causal association is reported between prolonged exposures to elevated levels of estrogen and breast cancer. Therefore inhibiting aromatase (CYP19A), which catalyses the conversion of androgens to estrogens, is an important ... -
Carbonic Anhydrase Inhibitors Targeting Metabolism and Tumor Microenvironment
Angeli, Andrea; Carta, Fabrizio; Nocentini, Alessio; Winum, Jean-Yves; Zalubovskis, Raivis; AKDEMİR, ATİLLA; Onnis, Valentina; Eldehna, Wagdy M.; Capasso, Clemente; De Simone, Giuseppina; Monti, Simona Maria; Carradori, Simone; Donald, William A.; Dedhar, Shoukat; Supuran, Claudiu T. (2020-10-01)The tumor microenvironment is crucial for the growth of cancer cells, triggering particular biochemical and physiological changes, which frequently influence the outcome of anticancer therapies. The biochemical rationale ... -
Computational investigation of the selectivity of salen and tetrahydrosalen compounds towards the tumor-associated hCA XII isozyme.
Akdemir, ATİLLA; SUPURAN, CT; De, Monte; CARRADORI, S (2015-02-01)In previous work, 14 salen and tetrahydrosalen compounds have been synthesized and tested in enzyme inhibition assays against cytosolic human carbonic anhydrase isozymes I and II (hCA I and II) and tumor-associated isozymes ... -
Development of Thiazolidinones as Fungal Carbonic Anhydrase Inhibitors.
Güzel-Akdemir, Ö; Carradori, S; Grande, R; Akdemir, ATİLLA; Demir-Yazıcı, K; Angeli, A; Supuran, CT (2020-04-22)In our efforts to find new and selective thiazolidinone-based anti-Candida agents, we synthesized and tested 26 thiazolidinones against several Candida spp. and Gram-positive and Gram-negative bacteria. The compounds ... -
Discovery of novel isatin-based sulfonamides with potent and selective inhibition of the tumor-associated carbonic anhydrase isoforms IX and XII.
GÜZEL-AKDEMIR, Ö; Akdemir, ATİLLA; KARALı, N; SUPURAN, CT (2015-06-21)A series of 2/3/4-[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)amino]benzenesulfonamides, obtained from substituted isatins and 2-, 3- or 4-aminobenzenesulfonamide, showed low nanomolar inhibitory activity against the tumor ... -
Exploring new Probenecid-based carbonic anhydrase inhibitors: Synthesis, biological evaluation and docking studies.
MOLLICA, A; COSTANTE, R; Akdemir, ATİLLA; CARRADORI, S; STEFANUCCI, A; MACEDONIO, G; CERUSO, M; SUPURAN, CT (2015-09-01) -
Fibrate-based N-acylsulphonamides targeting carbonic anhydrases: synthesis, biochemical evaluation, and docking studies.
GIAMPIETRO, L; AMMAZZALORSO, A; CARRADORI, S; ANGELI, A; De, Filippis; FANTACUZZI, M; MACCALLINI, C; Akdemir, ATİLLA; SUPURAN, CT; AMOROSO, R (2019-12-01)A large library of fibrate-based N-acylsulphonamides was designed, synthesised, and fully characterised in order to propose them as zinc binders for the inhibition of human carbonic anhydrase (hCA) enzymatic activity. ... -
Fragment growing induces conformational changes in acetylcholine-binding protein: a structural and thermodynamic analysis.
SIXMA, TK; SMIT, AB; Akdemir, ATİLLA; de, Esch; LEURS, R; van, Muijlwijk-Koezen; van, Nierop; JANSSEN, E; van, Elk; ZUIDERVELD, O; NAHAR, T; RETRA, K; RUCKTOOA, P; EDINK, E (2011-04-13) -
Indole-Based Hydrazones Containing A Sulfonamide Moiety as Selective Inhibitors of Tumor-Associated Human Carbonic Anhydrase Isoforms IX and XII
Demir-Yazici, Kubra; BUA, Silvia; Akgunes, Nurgul Mutlu; Akdemir, ATİLLA; Supuran, Claudiu T.; Guzel-Akdemir, Ozlen (2019-05-01)Novel sulfonamidoindole-based hydrazones with a 2-(hydrazinocarbonyl)-3-phenyl-1Hindole-5-sulfonamide scaffold were synthesized and tested in enzyme inhibition assays against the tumor-associated carbonic anhydrase isoforms, ... -
Isatin analogs as novel inhibitors of Candida spp. β-carbonic anhydrase enzymes.
Akdemir, ATİLLA; GÜZEL-AKDEMIR, Ö; KARALı, N; SUPURAN, CT (2016-04-15) -
New amide derivatives of Probenecid as selective inhibitors of carbonic anhydrase IX and XII: biological evaluation and molecular modelling studies.
De, Monte; SABIA, R; MOLLICA, A; CERUSO, M; CARRADORI, S; D'ASCENZIO, M; CHIMENTI, P; Akdemir, ATİLLA; SUPURAN, CT (2015-07-01) -
Novel 2-indolinones containing a sulfonamide moiety as selective inhibitors of candida β-carbonic anhydrase enzyme.
Akdemir, ATİLLA; ANGELI, A; GÖKTAŞ, F; Eraslan, Elma; KARALı, N; SUPURAN, CT (2019-12-01)Inhibition of the b-carbonic anhydrase (CA, EC 4.2.1.1) from pathogenic Candida glabrata (CgNce103) by 1H-indole-2,3-dione 3-[N-(4-sulfamoylphenyl)thiosemicarbazones] 4a–m was investigated. All the compounds were found ... -
Novel Indole-Based Hydrazones as Potent Inhibitors of the α-class Carbonic Anhydrase from Pathogenic Bacterium <i>Vibrio cholerae</i>.
Demir-Yazıcı, K; Güzel-Akdemir, Ö; Angeli, A; Supuran, Ct; Akdemir, Atilla (2020-04-29)Due to the increasing resistance of currently used antimicrobial drugs, there is an urgent problem for the treatment of cholera disease, selective inhibition of the α-class carbonic anhydrases (CA, EC 4.2.1.1) from the ... -
Novel sulfonamide-containing 2-indolinones that selectively inhibit tumor-associated alpha carbonic anhydrases.
KARALı, N; Akdemir, ATİLLA; GÖKTAŞ, F; Eraslan, Elma; ANGELI, A; KıZıLıRMAK, M; SUPURAN, CT (2017-07-15) -
o-Benzenedisulfonimido-sulfonamides are potent inhibitors of the tumor-associated carbonic anhydrase isoforms CA IX and CA XII.
GÜZEL-AKDEMIR, Ö; Akdemir, ATİLLA; ISIK, S; VULLO, D; SUPURAN, CT (2013-03-15) -
Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms.
D'ASCENZIO, M; GUGLIELMI, P; CARRADORI, S; SECCI, D; FLORIO, R; MOLLICA, A; CERUSO, M; Akdemir, ATİLLA; SOBOLEV, AP; SUPURAN, CT (2017-12-01)A large number of novel secondary sulfonamides based on the open saccharin scaffold were synthesized and evaluated as selective inhibitors of four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC ... -
Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein.
de, Esch; EDINK, E; LEURS, R; Akdemir, ATİLLA; SMIT, AB; van, Muijlwijk-Koezen; de, Kanter; ZUIDERVELD, O; van, Elk; JANSEN, C (2012-02-01)
