List of works - Andrea Scozzafava

Carbonic anhydrase inhibitors

scientific article (publication date: March 2003)

Targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors.

scientific article published on 17 March 2011

Hypoxia activates the capacity of tumor-associated carbonic anhydrase IX to acidify extracellular pH.

scientific article

Carbonic anhydrases as targets for medicinal chemistry

scientific article published on 19 April 2007

Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis.

scientific article

Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX

scientific article

Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition

scientific article

Non-zinc mediated inhibition of carbonic anhydrases: coumarins are a new class of suicide inhibitors

scientific article

Anticancer and antiviral sulfonamides

scientific article

Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes.

scientific article

Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins

scientific article

Highly active antiretroviral therapy: current state of the art, new agents and their pharmacological interactions useful for improving therapeutic outcome

scientific article

Antiglaucoma carbonic anhydrase inhibitors: a patent review

scientific article published on 30 April 2013

Characterization of CA XIII, a novel member of the carbonic anhydrase isozyme family

scientific journal article

Carbonic anhydrase inhibitors: sulfonamides as antitumor agents?

scientific article published in March 2001

Carbonic anhydrase activators: X-ray crystallographic and spectroscopic investigations for the interaction of isozymes I and II with histamine

scientific article

Antiobesity carbonic anhydrase inhibitors: a literature and patent review

scientific article published on April 22, 2013

Carbonic anhydrase IX from cancer-associated fibroblasts drives epithelial-mesenchymal transition in prostate carcinoma cells

scientific article published on 08 May 2013

Protease inhibitors of the sulfonamide type: anticancer, antiinflammatory, and antiviral agents

scientific article

Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?

scientific article

Imaging of CA IX with fluorescent labelled sulfonamides distinguishes hypoxic and (re)-oxygenated cells in a xenograft tumour model

scientific article published on 16 July 2009

Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted-ureido-benzenesulfonamides and correlate to inhibitor potency

scientific article

ESI mass spectrometry and X-ray diffraction studies of adducts between anticancer platinum drugs and hen egg white lysozyme

scientific article

Carbonic Anhydrase Inhibitors. Synthesis of Water-Soluble, Topically Effective, Intraocular Pressure-Lowering Aromatic/Heterocyclic Sulfonamides Containing Cationic or Anionic Moieties: Is the Tail More Important than the Ring?1

scientific article published on 01 July 1999

Sulfonamides: a patent review (2008 – 2012)

scientific article published on June 15, 2012

Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX.

scientific article published in January 2004

Specific inhibition of carbonic anhydrase IX activity enhances the in vivo therapeutic effect of tumor irradiation.

scientific article published on 14 June 2011

Glycosyl coumarin carbonic anhydrase IX and XII inhibitors strongly attenuate the growth of primary breast tumors.

scientific article published on 22 November 2011

Carbonic Anhydrase and Matrix Metalloproteinase Inhibitors: Sulfonylated Amino Acid Hydroxamates with MMP Inhibitory Properties Act as Efficient Inhibitors of CA Isozymes I, II, and IV, andN-Hydroxysulfonamides Inhibit Both These Zinc Enzymes1

scientific article published on 01 October 2000

Carbonic anhydrase IX: a new druggable target for the design of antitumor agents.

scientific article published on May 2008

Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides

scientific article published in March 2003

Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.

scientific article published in June 2005

Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes

scientific article

Bacterial protease inhibitors

scientific article

Taking advantage of tumor cell adaptations to hypoxia for developing new tumor markers and treatment strategies

scientific article published on April 2009

Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule

scientific article

Antimetastatic effect of sulfamate carbonic anhydrase IX inhibitors in breast carcinoma xenografts.

scientific article published on 5 June 2012

Applications of carbonic anhydrase inhibitors and activators in therapy

Carbonic Anhydrase Inhibitors: Synthesis of Water-Soluble, Aminoacyl/Dipeptidyl Sulfonamides Possessing Long-Lasting Intraocular Pressure-Lowering Properties via the Topical Route1

scientific article published on 01 September 1999

Carbonic anhydrase inhibitors

scientific article published on 01 November 1999

Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors.

scientific article published on July 2005

Dithiocarbamates Strongly Inhibit Carbonic Anhydrases and Show Antiglaucoma Action in Vivo

scientific article

Carbonic Anhydrase Inhibitors: X-ray and Molecular Modeling Study for the Interaction of a Fluorescent Antitumor Sulfonamide with Isozyme II and IX

article

Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.

scientific article published in March 2002

Carbonic anhydrase inhibitors: the first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX.

scientific article published in February 2004

Carbonic Anhydrase Inhibitors: Clash with Ala65 as a Means for Designing Inhibitors with Low Affinity for the Ubiquitous Isozyme II, Exemplified by the Crystal Structure of the Topiramate Sulfamide Analogue†

scientific article published on 01 November 2006

Sulfocoumarins (1,2-benzoxathiine-2,2-dioxides): a class of potent and isoform-selective inhibitors of tumor-associated carbonic anhydrases

scientific article

Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs

scientific article published in March 2006

Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors

scientific article published in December 2005

Carbonic Anhydrase Inhibitors: Perfluoroalkyl/Aryl-Substituted Derivatives of Aromatic/Heterocyclic Sulfonamides as Topical Intraocular Pressure-Lowering Agents with Prolonged Duration of Action

scientific article published on 01 November 2000

List of works by Andrea Scozzafava

Carbonic anhydrase inhibitors

Targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase IX inhibitors.

Hypoxia activates the capacity of tumor-associated carbonic anhydrase IX to acidify extracellular pH.

Carbonic anhydrases as targets for medicinal chemistry

Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis.

Crystal structure of the catalytic domain of the tumor-associated human carbonic anhydrase IX

Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological opportunities due to related binding site recognition

Non-zinc mediated inhibition of carbonic anhydrases: coumarins are a new class of suicide inhibitors

Anticancer and antiviral sulfonamides

Biochemical characterization of CA IX, one of the most active carbonic anhydrase isozymes.

Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins

Highly active antiretroviral therapy: current state of the art, new agents and their pharmacological interactions useful for improving therapeutic outcome

Antiglaucoma carbonic anhydrase inhibitors: a patent review

Characterization of CA XIII, a novel member of the carbonic anhydrase isozyme family

Carbonic anhydrase inhibitors: sulfonamides as antitumor agents?

Carbonic anhydrase activators: X-ray crystallographic and spectroscopic investigations for the interaction of isozymes I and II with histamine

Antiobesity carbonic anhydrase inhibitors: a literature and patent review

Carbonic anhydrase IX from cancer-associated fibroblasts drives epithelial-mesenchymal transition in prostate carcinoma cells

Protease inhibitors of the sulfonamide type: anticancer, antiinflammatory, and antiviral agents

Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?

Imaging of CA IX with fluorescent labelled sulfonamides distinguishes hypoxic and (re)-oxygenated cells in a xenograft tumour model

Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted-ureido-benzenesulfonamides and correlate to inhibitor potency

ESI mass spectrometry and X-ray diffraction studies of adducts between anticancer platinum drugs and hen egg white lysozyme

Carbonic Anhydrase Inhibitors. Synthesis of Water-Soluble, Topically Effective, Intraocular Pressure-Lowering Aromatic/Heterocyclic Sulfonamides Containing Cationic or Anionic Moieties: Is the Tail More Important than the Ring?1

Sulfonamides: a patent review (2008 – 2012)

Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX.

Specific inhibition of carbonic anhydrase IX activity enhances the in vivo therapeutic effect of tumor irradiation.

Glycosyl coumarin carbonic anhydrase IX and XII inhibitors strongly attenuate the growth of primary breast tumors.

Carbonic Anhydrase and Matrix Metalloproteinase Inhibitors: Sulfonylated Amino Acid Hydroxamates with MMP Inhibitory Properties Act as Efficient Inhibitors of CA Isozymes I, II, and IV, andN-Hydroxysulfonamides Inhibit Both These Zinc Enzymes1

Carbonic anhydrase IX: a new druggable target for the design of antitumor agents.

Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides

Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.

Carbonic anhydrase inhibitors: synthesis of membrane-impermeant low molecular weight sulfonamides possessing in vivo selectivity for the membrane-bound versus cytosolic isozymes

Bacterial protease inhibitors

Taking advantage of tumor cell adaptations to hypoxia for developing new tumor markers and treatment strategies

Polyamines inhibit carbonic anhydrases by anchoring to the zinc-coordinated water molecule

Antimetastatic effect of sulfamate carbonic anhydrase IX inhibitors in breast carcinoma xenografts.

Applications of carbonic anhydrase inhibitors and activators in therapy

Carbonic Anhydrase Inhibitors: Synthesis of Water-Soluble, Aminoacyl/Dipeptidyl Sulfonamides Possessing Long-Lasting Intraocular Pressure-Lowering Properties via the Topical Route1

Carbonic anhydrase inhibitors

Carbonic anhydrase inhibitors. Design of fluorescent sulfonamides as probes of tumor-associated carbonic anhydrase IX that inhibit isozyme IX-mediated acidification of hypoxic tumors.

Dithiocarbamates Strongly Inhibit Carbonic Anhydrases and Show Antiglaucoma Action in Vivo

Carbonic Anhydrase Inhibitors: X-ray and Molecular Modeling Study for the Interaction of a Fluorescent Antitumor Sulfonamide with Isozyme II and IX

Carbonic anhydrase inhibitors. A general approach for the preparation of water-soluble sulfonamides incorporating polyamino-polycarboxylate tails and of their metal complexes possessing long-lasting, topical intraocular pressure-lowering properties.

Carbonic anhydrase inhibitors: the first selective, membrane-impermeant inhibitors targeting the tumor-associated isozyme IX.

Carbonic Anhydrase Inhibitors: Clash with Ala65 as a Means for Designing Inhibitors with Low Affinity for the Ubiquitous Isozyme II, Exemplified by the Crystal Structure of the Topiramate Sulfamide Analogue†

Sulfocoumarins (1,2-benzoxathiine-2,2-dioxides): a class of potent and isoform-selective inhibitors of tumor-associated carbonic anhydrases

Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs

Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors

Carbonic Anhydrase Inhibitors: Perfluoroalkyl/Aryl-Substituted Derivatives of Aromatic/Heterocyclic Sulfonamides as Topical Intraocular Pressure-Lowering Agents with Prolonged Duration of Action