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Cadoni R, Pala N, Lomelino C, et al. Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors. ACS Med Chem Lett. 2017;8(9):941-946doi: 10.1021/acsmedchemlett.7b00229.
Cadoni, R., Pala, N., Lomelino, C., Mahon, B. P., McKenna, R., Dallocchio, R., Dessì, A., Carcelli, M., Rogolino, D., Sanna, V., Rassu, M., Iaccarino, C., Vullo, D., Supuran, C. T., & Sechi, M. (2017). Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors. ACS medicinal chemistry letters, 8(9), 941-946. https://doi.org/10.1021/acsmedchemlett.7b00229
Cadoni, Roberta, et al. "Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors." ACS medicinal chemistry letters vol. 8,9 (2017): 941-946. doi: https://doi.org/10.1021/acsmedchemlett.7b00229
Cadoni R, Pala N, Lomelino C, Mahon BP, McKenna R, Dallocchio R, Dessì A, Carcelli M, Rogolino D, Sanna V, Rassu M, Iaccarino C, Vullo D, Supuran CT, Sechi M. Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors. ACS Med Chem Lett. 2017 Jul 31;8(9):941-946. doi: 10.1021/acsmedchemlett.7b00229. eCollection 2017 Sep 14. PMID: 28947941; PMCID: PMC5601383.
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ACS Med Chem Lett. 2017 Jul 31;8(9):941-946. doi: 10.1021/acsmedchemlett.7b00229. eCollection 2017 Sep 14.

Exploring Heteroaryl-pyrazole Carboxylic Acids as Human Carbonic Anhydrase XII Inhibitors.

ACS medicinal chemistry letters

Roberta Cadoni, Nicolino Pala, Carrie Lomelino, Brian P Mahon, Robert McKenna, Roberto Dallocchio, Alessandro Dessì, Mauro Carcelli, Dominga Rogolino, Vanna Sanna, Mauro Rassu, Ciro Iaccarino, Daniela Vullo, Claudiu T Supuran, Mario Sechi

Affiliations

  1. Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100 Sassari, Italy.
  2. Department of Biochemistry and Molecular Biology, College of Medicine, University of Florida, 1600 SW Archer Road, PO Box 100245, Gainesville, Florida 32610, United States.
  3. Istituto CNR di Chimica Biomolecolare, Traversa La Crucca 3, 07100 Sassari, Italy.
  4. Department of Chemical, Life Science and Environmental Sustinability, University of Parma, Parco Area delle Scienze 17/A, 43124 Parma, Italy.
  5. Department of Biomedical Sciences, University of Sassari, Via Muroni 25, 07100 Sassari, Italy.
  6. Polo Scientifico, Neurofarba Department and Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Room 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy.

PMID: 28947941 PMCID: PMC5601383 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 prototypes of a new class of chemotherapeutics. Both X-ray crystallography and computational modeling provide insights into the CA inhibition mechanism. Results indicate that this chemotype produces an indirect interference with the zinc ion, thus behaving differently from other related nonclassical inhibitors. Among the tested compounds,

Keywords: Carbonic anhydrase; X-ray crystallography; computational docking; hCA XII inhibitors; heteroaryl-pyrazole carboxylic acids; hypoxic tumors

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