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Items: 1 to 50 of 93

1.

Dual Kit/Aur Inhibitors as Chemosensitizing Agents for the Treatment of Melanoma: Design, Synthesis, Docking Studies and Functional Investigation.

Quattrini L, Coviello V, Sartini S, Di Desidero T, Orlandi P, Ke YY, Liu KL, Hsieh HP, Bocci G, La Motta C.

Sci Rep. 2019 Jul 9;9(1):9943. doi: 10.1038/s41598-019-46287-5.

2.

Aldose reductase inhibitors: 2013-present.

Quattrini L, La Motta C.

Expert Opin Ther Pat. 2019 Mar;29(3):199-213. doi: 10.1080/13543776.2019.1582646. Epub 2019 Feb 27. Review.

PMID:
30760060
3.

Soyasaponins from Zolfino bean as aldose reductase differential inhibitors.

Balestri F, De Leo M, Sorce C, Cappiello M, Quattrini L, Moschini R, Pineschi C, Braca A, La Motta C, Da Settimo F, Del-Corso A, Mura U.

J Enzyme Inhib Med Chem. 2019 Dec;34(1):350-360. doi: 10.1080/14756366.2018.1553166.

4.

Antineoplastic Effect of Lenvatinib and Vandetanib in Primary Anaplastic Thyroid Cancer Cells Obtained From Biopsy or Fine Needle Aspiration.

Ferrari SM, La Motta C, Elia G, Ragusa F, Ruffilli I, Quattrini L, Paparo SR, Piaggi S, Patrizio A, Ulisse S, Baldini E, Materazzi G, Fallahi P, Antonelli A.

Front Endocrinol (Lausanne). 2018 Dec 18;9:764. doi: 10.3389/fendo.2018.00764. eCollection 2018.

5.

Acid Derivatives of Pyrazolo[1,5-a]pyrimidine as Aldose Reductase Differential Inhibitors.

Balestri F, Quattrini L, Coviello V, Sartini S, Da Settimo F, Cappiello M, Moschini R, Del Corso A, Mura U, La Motta C.

Cell Chem Biol. 2018 Nov 15;25(11):1414-1418.e3. doi: 10.1016/j.chembiol.2018.07.008. Epub 2018 Aug 16.

PMID:
30122369
6.

Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.

La Pietra V, Sartini S, Botta L, Antonelli A, Ferrari SM, Fallahi P, Moriconi A, Coviello V, Quattrini L, Ke YY, Hsing-Pang H, Da Settimo F, Novellino E, La Motta C, Marinelli L.

Eur J Med Chem. 2018 Apr 25;150:491-505. doi: 10.1016/j.ejmech.2018.02.080. Epub 2018 Mar 2.

PMID:
29549836
7.

New insights in the structure-activity relationships of 2-phenylamino-substituted benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors.

Salerno S, García-Argáez AN, Barresi E, Taliani S, Simorini F, La Motta C, Amendola G, Tomassi S, Cosconati S, Novellino E, Da Settimo F, Marini AM, Via LD.

Eur J Med Chem. 2018 Apr 25;150:446-456. doi: 10.1016/j.ejmech.2018.03.013. Epub 2018 Mar 7.

PMID:
29547832
8.

Vandetanib has antineoplastic activity in anaplastic thyroid cancer, in vitro and in vivo.

Ferrari SM, Bocci G, Di Desidero T, Ruffilli I, Elia G, Ragusa F, Fioravanti A, Orlandi P, Paparo SR, Patrizio A, Piaggi S, La Motta C, Ulisse S, Baldini E, Materazzi G, Miccoli P, Antonelli A, Fallahi P.

Oncol Rep. 2018 May;39(5):2306-2314. doi: 10.3892/or.2018.6305. Epub 2018 Mar 8.

PMID:
29517106
9.

Lenvatinib exhibits antineoplastic activity in anaplastic thyroid cancer in vitro and in vivo.

Ferrari SM, Bocci G, Di Desidero T, Elia G, Ruffilli I, Ragusa F, Orlandi P, Paparo SR, Patrizio A, Piaggi S, La Motta C, Ulisse S, Baldini E, Materazzi G, Miccoli P, Antonelli A, Fallahi P.

Oncol Rep. 2018 May;39(5):2225-2234. doi: 10.3892/or.2018.6306. Epub 2018 Mar 8.

PMID:
29517103
10.

Quinazolinone-based rhodanine-3-acetic acids as potent aldose reductase inhibitors: Synthesis, functional evaluation and molecular modeling study.

El-Sayed S, Metwally K, El-Shanawani AA, Abdel-Aziz LM, El-Rashedy AA, Soliman MES, Quattrini L, Coviello V, la Motta C.

Bioorg Med Chem Lett. 2017 Oct 15;27(20):4760-4764. doi: 10.1016/j.bmcl.2017.08.050. Epub 2017 Aug 24.

PMID:
28935265
11.

Novel therapeutic clues in thyroid carcinomas: The role of targeting cancer stem cells.

Antonelli A, La Motta C.

Med Res Rev. 2017 Nov;37(6):1299-1317. doi: 10.1002/med.21448. Epub 2017 Jun 6. Review.

PMID:
28586525
12.

Synthesis and Functional Evaluation of Novel Aldose Reductase Inhibitors Bearing a Spirobenzopyran Scaffold.

Digiacomo M, Sartini S, Nesi G, Sestito S, Coviello V, La Motta C, Rapposelli S.

Open Med Chem J. 2017 Jan 31;11:9-23. doi: 10.2174/1874104501711010009. eCollection 2017.

13.

Cyclodextrin-based nanosponges for the targeted delivery of the anti-restenotic agent DB103: A novel opportunity for the local therapy of vessels wall subjected to percutaneous intervention.

Coviello V, Sartini S, Quattrini L, Baraldi C, Gamberini MC, La Motta C.

Eur J Pharm Biopharm. 2017 Aug;117:276-285. doi: 10.1016/j.ejpb.2017.04.028. Epub 2017 Apr 26.

PMID:
28456606
14.

N-(Aroyl)-N-(arylmethyloxy)-α-alanines: Selective inhibitors of aldose reductase.

Nencetti S, La Motta C, Rossello A, Sartini S, Nuti E, Ciccone L, Orlandini E.

Bioorg Med Chem. 2017 Jun 15;25(12):3068-3076. doi: 10.1016/j.bmc.2017.03.056. Epub 2017 Mar 28.

PMID:
28392277
15.

FOXD1-ALDH1A3 Signaling Is a Determinant for the Self-Renewal and Tumorigenicity of Mesenchymal Glioma Stem Cells.

Cheng P, Wang J, Waghmare I, Sartini S, Coviello V, Zhang Z, Kim SH, Mohyeldin A, Pavlyukov MS, Minata M, Valentim CL, Chhipa RR, Bhat KP, Dasgupta B, La Motta C, Kango-Singh M, Nakano I.

Cancer Res. 2016 Dec 15;76(24):7219-7230. Epub 2016 Aug 28.

16.

1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.

Coviello V, Marchi B, Sartini S, Quattrini L, Marini AM, Simorini F, Taliani S, Salerno S, Orlandi P, Fioravanti A, Desidero TD, Vullo D, Da Settimo F, Supuran CT, Bocci G, La Motta C.

J Med Chem. 2016 Jul 14;59(13):6547-52. doi: 10.1021/acs.jmedchem.6b00616. Epub 2016 Jun 27.

PMID:
27305384
17.

A Series of COX-2 Inhibitors Endowed with NO-Releasing Properties: Synthesis, Biological Evaluation, and Docking Analysis.

Consalvi S, Poce G, Ragno R, Sabatino M, La Motta C, Sartini S, Calderone V, Martelli A, Ghelardini C, Di Cesare Mannelli L, Biava M.

ChemMedChem. 2016 Aug 19;11(16):1804-11. doi: 10.1002/cmdc.201600086. Epub 2016 May 27.

PMID:
27229194
18.

Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas.

Daniele S, La Pietra V, Barresi E, Di Maro S, Da Pozzo E, Robello M, La Motta C, Cosconati S, Taliani S, Marinelli L, Novellino E, Martini C, Da Settimo F.

J Med Chem. 2016 May 26;59(10):4526-38. doi: 10.1021/acs.jmedchem.5b01767. Epub 2016 May 3.

PMID:
27050782
19.

Effects of the New Aldose Reductase Inhibitor Benzofuroxane Derivative BF-5m on High Glucose Induced Prolongation of Cardiac QT Interval and Increase of Coronary Perfusion Pressure.

Di Filippo C, Ferraro B, Maisto R, Trotta MC, Di Carluccio N, Sartini S, La Motta C, Ferraraccio F, Rossi F, D'Amico M.

J Diabetes Res. 2016;2016:5281267. doi: 10.1155/2016/5281267. Epub 2015 Dec 29.

20.

Sulfonamides incorporating heteropolycyclic scaffolds show potent inhibitory action against carbonic anhydrase isoforms I, II, IX and XII.

Barresi E, Salerno S, Marini AM, Taliani S, La Motta C, Simorini F, Da Settimo F, Vullo D, Supuran CT.

Bioorg Med Chem. 2016 Feb 15;24(4):921-7. doi: 10.1016/j.bmc.2016.01.018. Epub 2016 Jan 11.

PMID:
26796953
21.

Nanostructured ultra-thin patches for ultrasound-modulated delivery of anti-restenotic drug.

Vannozzi L, Ricotti L, Filippeschi C, Sartini S, Coviello V, Piazza V, Pingue P, La Motta C, Dario P, Menciassi A.

Int J Nanomedicine. 2015 Dec 23;11:69-91. doi: 10.2147/IJN.S92031. eCollection 2016.

22.

Pyrazolopyrimidine Derivatives as Antineoplastic Agents: with a Special Focus on Thyroid Cancer.

Ferrari SM, La Motta C, Sartini S, Baldini E, Materazzi G, Politti U, Ruffilli I, Ulisse S, Miccoli P, Antonelli A, Fallahi P.

Mini Rev Med Chem. 2016;16(2):86-93. Review.

PMID:
26471970
23.

Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.

Salerno S, Marini AM, Fornaciari G, Simorini F, La Motta C, Taliani S, Sartini S, Da Settimo F, García-Argáez AN, Gia O, Cosconati S, Novellino E, D'Ocon P, Fioravanti A, Orlandi P, Bocci G, Dalla Via L.

Eur J Med Chem. 2015 Oct 20;103:29-43. doi: 10.1016/j.ejmech.2015.08.027. Epub 2015 Aug 14.

PMID:
26318056
24.

CLM29 and CLM24, pyrazolopyrimidine derivatives, have antitumoral activity in vitro in anaplastic thyroid cancer, with or without BRAF mutation.

Fallahi P, Ferrari SM, La Motta C, Materazzi G, Bocci G, Da Settimo F, Miccoli P, Antonelli A.

Endocrine. 2016 Jul;53(1):136-44. doi: 10.1007/s12020-015-0717-4. Epub 2015 Aug 19.

PMID:
26286966
25.

Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides.

Barresi E, Bruno A, Taliani S, Cosconati S, Da Pozzo E, Salerno S, Simorini F, Daniele S, Giacomelli C, Marini AM, La Motta C, Marinelli L, Cosimelli B, Novellino E, Greco G, Da Settimo F, Martini C.

J Med Chem. 2015 Aug 13;58(15):6081-92. doi: 10.1021/acs.jmedchem.5b00689. Epub 2015 Jul 28.

PMID:
26177193
26.

Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors.

Consalvi S, Alfonso S, Di Capua A, Poce G, Pirolli A, Sabatino M, Ragno R, Anzini M, Sartini S, La Motta C, Di Cesare Mannelli L, Ghelardini C, Biava M.

Bioorg Med Chem. 2015 Feb 15;23(4):810-20. doi: 10.1016/j.bmc.2014.12.041. Epub 2014 Dec 26.

PMID:
25596758
27.

Synthetic analogues of flavonoids with improved activity against platelet activation and aggregation as novel prototypes of food supplements.

Del Turco S, Sartini S, Cigni G, Sentieri C, Sbrana S, Battaglia D, Papa A, Da Settimo F, La Motta C, Basta G.

Food Chem. 2015 May 15;175:494-9. doi: 10.1016/j.foodchem.2014.12.005. Epub 2014 Dec 16.

PMID:
25577111
28.

Inhibition of ocular aldose reductase by a new benzofuroxane derivative ameliorates rat endotoxic uveitis.

Di Filippo C, Zippo MV, Maisto R, Trotta MC, Siniscalco D, Ferraro B, Ferraraccio F, La Motta C, Sartini S, Cosconati S, Novellino E, Gesualdo C, Simonelli F, Rossi S, D'Amico M.

Mediators Inflamm. 2014;2014:857958. doi: 10.1155/2014/857958. Epub 2014 Nov 11.

29.

Antineoplastic activity of the multitarget tyrosine kinase inhibitors CLM3 and CLM94 in medullary thyroid cancer in vitro.

Ferrari SM, Fallahi P, La Motta C, Bocci G, Corrado A, Materazzi G, Galleri D, Piaggi S, Danesi R, Da Settimo F, Miccoli P, Antonelli A.

Surgery. 2014 Nov;156(5):1167-76. doi: 10.1016/j.surg.2014.05.005. Epub 2014 Aug 21.

PMID:
25151558
30.

CLM29, a multi-target pyrazolopyrimidine derivative, has anti-neoplastic activity in medullary thyroid cancer in vitro and in vivo.

Antonelli A, Bocci G, La Motta C, Ferrari SM, Fallahi P, Corrado A, Fioravanti A, Sartini S, Orlandi P, Piaggi S, Corti A, Materazzi G, Galleri D, Ulisse S, Fontanini G, Danesi R, Da Settimo F, Miccoli P.

Mol Cell Endocrinol. 2014 Aug 5;393(1-2):56-64. doi: 10.1016/j.mce.2014.06.002. Epub 2014 Jun 12.

PMID:
24931161
31.

Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies.

Sartini S, Coviello V, Bruno A, La Pietra V, Marinelli L, Simorini F, Taliani S, Salerno S, Marini AM, Fioravanti A, Orlandi P, Antonelli A, Da Settimo F, Novellino E, Bocci G, La Motta C.

J Med Chem. 2014 Feb 27;57(4):1225-35. doi: 10.1021/jm401358b. Epub 2014 Feb 5.

PMID:
24447248
32.

CLM3, a multitarget tyrosine kinase inhibitor with antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo.

Antonelli A, Bocci G, Fallahi P, La Motta C, Ferrari SM, Mancusi C, Fioravanti A, Di Desidero T, Sartini S, Corti A, Piaggi S, Materazzi G, Spinelli C, Fontanini G, Danesi R, Da Settimo F, Miccoli P.

J Clin Endocrinol Metab. 2014 Apr;99(4):E572-81. doi: 10.1210/jc.2013-2321. Epub 2014 Jan 1.

PMID:
24423321
33.

A novel 2,3-diphenyl-4H-pyrido[1,2-a]pyrimidin-4-one derivative inhibits endothelial cell dysfunction and smooth muscle cell proliferation/activation.

Del Turco S, Sartini S, Sentieri C, Saponaro C, Navarra T, Dario B, Da Settimo F, La Motta C, Basta G.

Eur J Med Chem. 2014 Jan 24;72:102-9. doi: 10.1016/j.ejmech.2013.11.021. Epub 2013 Dec 1.

PMID:
24361522
34.

PMMA/polysaccharides nanofilm loaded with adenosine deaminase inhibitor for targeted anti-inflammatory drug delivery.

Redolfi Riva E, Desii A, Sartini S, La Motta C, Mazzolai B, Mattoli V.

Langmuir. 2013 Oct 29;29(43):13190-7. doi: 10.1021/la402229k. Epub 2013 Oct 14.

PMID:
24073802
35.

A new approach to control the enigmatic activity of aldose reductase.

Del-Corso A, Balestri F, Di Bugno E, Moschini R, Cappiello M, Sartini S, La-Motta C, Da-Settimo F, Mura U.

PLoS One. 2013 Sep 3;8(9):e74076. doi: 10.1371/journal.pone.0074076. eCollection 2013.

36.

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.

Taliani S, Pugliesi I, Barresi E, Salerno S, Marchand C, Agama K, Simorini F, La Motta C, Marini AM, Di Leva FS, Marinelli L, Cosconati S, Novellino E, Pommier Y, Di Santo R, Da Settimo F.

J Med Chem. 2013 Sep 26;56(18):7458-62. doi: 10.1021/jm400932c. Epub 2013 Sep 16.

37.

Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2).

Perspicace E, Jouan-Hureaux V, Ragno R, Ballante F, Sartini S, La Motta C, Da Settimo F, Chen B, Kirsch G, Schneider S, Faivre B, Hesse S.

Eur J Med Chem. 2013 May;63:765-81. doi: 10.1016/j.ejmech.2013.03.022. Epub 2013 Mar 19.

PMID:
23583911
38.

Benzofuroxane derivatives as multi-effective agents for the treatment of cardiovascular diabetic complications. Synthesis, functional evaluation, and molecular modeling studies.

Sartini S, Cosconati S, Marinelli L, Barresi E, Di Maro S, Simorini F, Taliani S, Salerno S, Marini AM, Da Settimo F, Novellino E, La Motta C.

J Med Chem. 2012 Dec 13;55(23):10523-31. doi: 10.1021/jm301124s. Epub 2012 Nov 20.

PMID:
23134227
39.

Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.

Marini AM, Maresca A, Aggarwal M, Orlandini E, Nencetti S, Da Settimo F, Salerno S, Simorini F, La Motta C, Taliani S, Nuti E, Scozzafava A, McKenna R, Rossello A, Supuran CT.

J Med Chem. 2012 Nov 26;55(22):9619-29. doi: 10.1021/jm300878g. Epub 2012 Nov 8.

PMID:
23067387
40.

Progresses in the pursuit of aldose reductase inhibitors: the structure-based lead optimization step.

Ramunno A, Cosconati S, Sartini S, Maglio V, Angiuoli S, La Pietra V, Di Maro S, Giustiniano M, La Motta C, Da Settimo F, Marinelli L, Novellino E.

Eur J Med Chem. 2012 May;51:216-26. doi: 10.1016/j.ejmech.2012.02.045. Epub 2012 Mar 5.

PMID:
22436396
41.

CLM94, a novel cyclic amide with anti-VEGFR-2 and antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo.

Antonelli A, Bocci G, La Motta C, Ferrari SM, Fallahi P, Ruffilli I, Di Domenicantonio A, Fioravanti A, Sartini S, Minuto M, Piaggi S, Corti A, Alì G, Di Desidero T, Berti P, Fontanini G, Danesi R, Da Settimo F, Miccoli P.

J Clin Endocrinol Metab. 2012 Apr;97(4):E528-36. doi: 10.1210/jc.2011-1987. Epub 2012 Jan 25.

PMID:
22278419
42.

3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.

Taliani S, Pugliesi I, Barresi E, Simorini F, Salerno S, La Motta C, Marini AM, Cosimelli B, Cosconati S, Di Maro S, Marinelli L, Daniele S, Trincavelli ML, Greco G, Novellino E, Martini C, Da Settimo F.

J Med Chem. 2012 Feb 23;55(4):1490-9. doi: 10.1021/jm201177b. Epub 2012 Feb 7.

PMID:
22257095
43.

Adenosine deaminase in the modulation of immune system and its potential as a novel target for treatment of inflammatory disorders.

Antonioli L, Colucci R, La Motta C, Tuccori M, Awwad O, Da Settimo F, Blandizzi C, Fornai M.

Curr Drug Targets. 2012 Jun;13(6):842-62. Review.

PMID:
22250650
44.

Sampling protein motion and solvent effect during ligand binding.

Limongelli V, Marinelli L, Cosconati S, La Motta C, Sartini S, Mugnaini L, Da Settimo F, Novellino E, Parrinello M.

Proc Natl Acad Sci U S A. 2012 Jan 31;109(5):1467-72. doi: 10.1073/pnas.1112181108. Epub 2012 Jan 11.

45.

Geometrically constrained derivatives of indolylglyoxylamides as ligands binding the GABAA/BzR complex.

Sartini S, Morelli M, Simorini F, Taliani S, Salerno S, Marini AM, Da Settimo F, La Motta C.

Curr Top Med Chem. 2012;12(4):312-20. Review.

PMID:
22204489
46.

Medicinal chemistry of indolylglyoxylamide TSPO high affinity ligands with anxiolytic-like effects.

Simorini F, Marini AM, Taliani S, La Motta C, Salerno S, Pugliesi I, Da Settimo F.

Curr Top Med Chem. 2012;12(4):333-51. Review.

PMID:
22204487
47.

Medicinal chemistry of indolylglyoxylamide GABAA/BzR high affinity ligands: identification of novel anxiolytic/non sedative agents.

Salerno S, Da Settimo F, Taliani S, Simorini F, La Motta C, Fornaciari G, Marini AM.

Curr Top Med Chem. 2012;12(4):286-311. Review.

PMID:
22204484
48.

Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization.

La Pietra V, Marinelli L, Cosconati S, Di Leva FS, Nuti E, Santamaria S, Pugliesi I, Morelli M, Casalini F, Rossello A, La Motta C, Taliani S, Visse R, Nagase H, da Settimo F, Novellino E.

Eur J Med Chem. 2012 Jan;47(1):143-52. doi: 10.1016/j.ejmech.2011.10.035. Epub 2011 Oct 25.

PMID:
22088955
49.

Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.

Cosimelli B, Simorini F, Taliani S, La Motta C, Da Settimo F, Severi E, Greco G, Novellino E, Costa B, Da Pozzo E, Bendinelli S, Martini C.

Eur J Med Chem. 2011 Sep;46(9):4506-20. doi: 10.1016/j.ejmech.2011.07.025. Epub 2011 Jul 23.

PMID:
21824692
50.

Derivatives of benzimidazol-2-ylquinoline and benzimidazol-2-ylisoquinoline as selective A1 adenosine receptor antagonists with stimulant activity on human colon motility.

Cosimelli B, Taliani S, Greco G, Novellino E, Sala A, Severi E, Da Settimo F, La Motta C, Pugliesi I, Antonioli L, Fornai M, Colucci R, Blandizzi C, Daniele S, Trincavelli ML, Martini C.

ChemMedChem. 2011 Oct 4;6(10):1909-18. doi: 10.1002/cmdc.201100284. Epub 2011 Jul 27.

PMID:
21796795

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