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Items: 1 to 50 of 167

1.

An Update on JAK Inhibitors.

Musumeci F, Greco C, Giacchello I, Fallacara AL, Ibrahim MM, Grossi G, Brullo C, Schenone S.

Curr Med Chem. 2018 Mar 26. doi: 10.2174/0929867325666180327093502. [Epub ahead of print]

PMID:
29589523
2.

Water Solubility Enhancement of Pyrazolo[3,4-d]pyrimidine Derivatives via Miniaturized Polymer-Drug Microarrays.

Sanna M, Sicilia G, Alazzo A, Singh N, Musumeci F, Schenone S, Spriggs KA, Burley JC, Garnett MC, Taresco V, Alexander C.

ACS Med Chem Lett. 2018 Jan 29;9(3):193-197. doi: 10.1021/acsmedchemlett.7b00456. eCollection 2018 Mar 8.

PMID:
29541359
3.

The small molecule SI113 synergizes with mitotic spindle poisons in arresting the growth of human glioblastoma multiforme.

Abbruzzese C, Catalogna G, Gallo E, di Martino S, Mileo AM, Carosi M, Dattilo V, Schenone S, Musumeci F, Lavia P, Perrotti N, Amato R, Paggi MG.

Oncotarget. 2017 Nov 18;8(67):110743-110755. doi: 10.18632/oncotarget.22500. eCollection 2017 Dec 19.

4.

Matrine in association with FD‑2 stimulates F508del‑cystic fibrosis transmembrane conductance regulator activity in the presence of corrector VX809.

Marengo B, Speciale A, Senatore L, Garibaldi S, Musumeci F, Nieddu E, Pollarolo B, Pronzato MA, Schenone S, Mazzei M, Domenicotti C.

Mol Med Rep. 2017 Dec;16(6):8849-8853. doi: 10.3892/mmr.2017.7736. Epub 2017 Oct 6.

5.

The SGK1 Kinase Inhibitor SI113 Sensitizes Theranostic Effects of the 64CuCl2 in Human Glioblastoma Multiforme Cells.

Catalogna G, Talarico C, Dattilo V, Gangemi V, Calabria F, D'Antona L, Schenone S, Musumeci F, Bianco C, Perrotti N, Amato R, Cascini GL.

Cell Physiol Biochem. 2017;43(1):108-119. doi: 10.1159/000480328. Epub 2017 Aug 25.

6.

Differentially activated Src kinase in chemo-naïve human primary osteosarcoma cells and effects of a Src kinase inhibitor.

Laschi M, Bernardini G, Geminiani M, Manetti F, Mori M, Spreafico A, Campanacci D, Capanna R, Schenone S, Botta M, Santucci A.

Biofactors. 2017 Nov;43(6):801-811. doi: 10.1002/biof.1382. Epub 2017 Aug 8.

PMID:
28786551
7.

Pyrrolo[2,3-d]pyrimidines active as Btk inhibitors.

Musumeci F, Sanna M, Greco C, Giacchello I, Fallacara AL, Amato R, Schenone S.

Expert Opin Ther Pat. 2017 Dec;27(12):1305-1318. doi: 10.1080/13543776.2017.1355908. Epub 2017 Jul 20. Review.

PMID:
28705083
8.

Phenotype-based variation as a biomarker of sensitivity to molecularly targeted therapy in melanoma.

Senses KM, Ghasemi M, Akbar MW, Isbilen M, Fallacara AL, Frankenburg S, Schenone S, Lotem M, Botta M, Gure AO.

Medchemcomm. 2017 Jan 1;8(1):88-95. doi: 10.1039/C6MD00466K. Epub 2016 Oct 27.

9.

Prodrugs of Pyrazolo[3,4-d]pyrimidines: From Library Synthesis to Evaluation as Potential Anticancer Agents in an Orthotopic Glioblastoma Model.

Vignaroli G, Iovenitti G, Zamperini C, Coniglio F, Calandro P, Molinari A, Fallacara AL, Sartucci A, Calgani A, Colecchia D, Mancini A, Festuccia C, Dreassi E, Valoti M, Musumeci F, Chiariello M, Angelucci A, Botta M, Schenone S.

J Med Chem. 2017 Jul 27;60(14):6305-6320. doi: 10.1021/acs.jmedchem.7b00637. Epub 2017 Jul 18.

PMID:
28650650
10.

Pyrazolo[3,4-d]pyrimidines-loaded human serum albumin (HSA) nanoparticles: Preparation, characterization and cytotoxicity evaluation against neuroblastoma cell line.

Fallacara AL, Mancini A, Zamperini C, Dreassi E, Marianelli S, Chiariello M, Pozzi G, Santoro F, Botta M, Schenone S.

Bioorg Med Chem Lett. 2017 Jul 15;27(14):3196-3200. doi: 10.1016/j.bmcl.2017.05.015. Epub 2017 May 17.

PMID:
28558969
11.

SGK1 affects RAN/RANBP1/RANGAP1 via SP1 to play a critical role in pre-miRNA nuclear export: a new route of epigenomic regulation.

Dattilo V, D'Antona L, Talarico C, Capula M, Catalogna G, Iuliano R, Schenone S, Roperto S, Bianco C, Perrotti N, Amato R.

Sci Rep. 2017 Mar 30;7:45361. doi: 10.1038/srep45361.

12.

Pyrrolo[2,3-d]Pyrimidines as Kinase Inhibitors.

Musumeci F, Sanna M, Grossi G, Brullo C, Fallacara AL, Schenone S.

Curr Med Chem. 2017;24(19):2059-2085. doi: 10.2174/0929867324666170303162100. Review.

PMID:
28266267
13.

The SGK1 inhibitor SI113 induces autophagy, apoptosis, and endoplasmic reticulum stress in endometrial cancer cells.

Conza D, Mirra P, Calì G, Tortora T, Insabato L, Fiory F, Schenone S, Amato R, Beguinot F, Perrotti N, Ulianich L.

J Cell Physiol. 2017 Dec;232(12):3735-3743. doi: 10.1002/jcp.25850. Epub 2017 Apr 27.

PMID:
28177128
14.

Identification of new pyrrolo[2,3-d]pyrimidines as Src tyrosine kinase inhibitors in vitro active against Glioblastoma.

Musumeci F, Fallacara AL, Brullo C, Grossi G, Botta L, Calandro P, Chiariello M, Kissova M, Crespan E, Maga G, Schenone S.

Eur J Med Chem. 2017 Feb 15;127:369-378. doi: 10.1016/j.ejmech.2016.12.036. Epub 2016 Dec 19.

PMID:
28076826
15.

A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies.

Laurenzana I, Caivano A, La Rocca F, Trino S, De Luca L, D'Alessio F, Schenone S, Falco G, Botta M, Del Vecchio L, Musto P.

Front Pharmacol. 2016 Nov 7;7:416. eCollection 2016.

16.

SGK1, the New Player in the Game of Resistance: Chemo-Radio Molecular Target and Strategy for Inhibition.

Talarico C, Dattilo V, D'Antona L, Menniti M, Bianco C, Ortuso F, Alcaro S, Schenone S, Perrotti N, Amato R.

Cell Physiol Biochem. 2016;39(5):1863-1876. Epub 2016 Oct 24. Review.

17.

A Pyrazolo[3,4-d]pyrimidine compound inhibits Fyn phosphorylation and induces apoptosis in natural killer cell leukemia.

Laurenzana I, Caivano A, Trino S, De Luca L, La Rocca F, Simeon V, Tintori C, D'Alessio F, Teramo A, Zambello R, Traficante A, Maietti M, Semenzato G, Schenone S, Botta M, Musto P, Del Vecchio L.

Oncotarget. 2016 Oct 4;7(40):65171-65184. doi: 10.18632/oncotarget.11496.

18.

A cascade screening approach for the identification of Bcr-Abl myristate pocket binders active against wild type and T315I mutant.

Radi M, Schneider R, Fallacara AL, Botta L, Crespan E, Tintori C, Maga G, Kissova M, Calgani A, Richters A, Musumeci F, Rauh D, Schenone S.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3436-40. doi: 10.1016/j.bmcl.2016.06.051. Epub 2016 Jun 18.

PMID:
27374241
19.

Suppression of SRC Signaling Is Effective in Reducing Synergy between Glioblastoma and Stromal Cells.

Calgani A, Vignaroli G, Zamperini C, Coniglio F, Festuccia C, Di Cesare E, Gravina GL, Mattei C, Vitale F, Schenone S, Botta M, Angelucci A.

Mol Cancer Ther. 2016 Jul;15(7):1535-44. doi: 10.1158/1535-7163.MCT-15-1011. Epub 2016 May 11.

20.

SRC Family Kinase Inhibition in Ewing Sarcoma Cells Induces p38 MAP Kinase-Mediated Cytotoxicity and Reduces Cell Migration.

Indovina P, Casini N, Forte IM, Garofano T, Cesari D, Iannuzzi CA, Del Porro L, Pentimalli F, Napoliello L, Boffo S, Schenone S, Botta M, Giordano A.

J Cell Physiol. 2017 Jan;232(1):129-35. doi: 10.1002/jcp.25397. Epub 2016 Apr 19.

PMID:
27037775
21.

SI113, a SGK1 inhibitor, potentiates the effects of radiotherapy, modulates the response to oxidative stress and induces cytotoxic autophagy in human glioblastoma multiforme cells.

Talarico C, Dattilo V, D'Antona L, Barone A, Amodio N, Belviso S, Musumeci F, Abbruzzese C, Bianco C, Trapasso F, Schenone S, Alcaro S, Ortuso F, Florio T, Paggi MG, Perrotti N, Amato R.

Oncotarget. 2016 Mar 29;7(13):15868-84. doi: 10.18632/oncotarget.7520.

22.

Improvement of pyrazolo[3,4-d]pyrimidines pharmacokinetic properties: nanosystem approaches for drug delivery.

Vignaroli G, Calandro P, Zamperini C, Coniglio F, Iovenitti G, Tavanti M, Colecchia D, Dreassi E, Valoti M, Schenone S, Chiariello M, Botta M.

Sci Rep. 2016 Feb 22;6:21509. doi: 10.1038/srep21509.

23.

Phenylhydrazones as Correctors of a Mutant Cystic Fibrosis Transmembrane Conductance Regulator.

Nieddu E, Pollarolo B, Mazzei MT, Anzaldi M, Schenone S, Pedemonte N, Galietta LJ, Mazzei M.

Arch Pharm (Weinheim). 2016 Feb;349(2):112-23. doi: 10.1002/ardp.201500352. Epub 2015 Dec 23.

PMID:
26701662
24.

Identification of Aminoimidazole and Aminothiazole Derivatives as Src Family Kinase Inhibitors.

Francini CM, Fallacara AL, Artusi R, Mennuni L, Calgani A, Angelucci A, Schenone S, Botta M.

ChemMedChem. 2015 Dec;10(12):2027-41. doi: 10.1002/cmdc.201500428. Epub 2015 Oct 30.

PMID:
26514807
25.

Preclinical model in HCC: the SGK1 kinase inhibitor SI113 blocks tumor progression in vitro and in vivo and synergizes with radiotherapy.

Talarico C, D'Antona L, Scumaci D, Barone A, Gigliotti F, Fiumara CV, Dattilo V, Gallo E, Visca P, Ortuso F, Abbruzzese C, Botta L, Schenone S, Cuda G, Alcaro S, Bianco C, Lavia P, Paggi MG, Perrotti N, Amato R.

Oncotarget. 2015 Nov 10;6(35):37511-25. doi: 10.18632/oncotarget.5527.

26.

Analogs, formulations and derivatives of imatinib: a patent review.

Musumeci F, Schenone S, Grossi G, Brullo C, Sanna M.

Expert Opin Ther Pat. 2015;25(12):1411-21. doi: 10.1517/13543776.2015.1089233. Epub 2015 Sep 15. Review.

PMID:
26372795
27.

Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors.

Tintori C, La Sala G, Vignaroli G, Botta L, Fallacara AL, Falchi F, Radi M, Zamperini C, Dreassi E, Dello Iacono L, Orioli D, Biamonti G, Garbelli M, Lossani A, Gasparrini F, Tuccinardi T, Laurenzana I, Angelucci A, Maga G, Schenone S, Brullo C, Musumeci F, Desogus A, Crespan E, Botta M.

J Med Chem. 2015 Jun 11;58(11):4590-609. doi: 10.1021/acs.jmedchem.5b00140. Epub 2015 May 20.

PMID:
25923950
28.

Click chemistry, a potent tool in medicinal sciences.

Musumeci F, Schenone S, Desogus A, Nieddu E, Deodato D, Botta L.

Curr Med Chem. 2015;22(17):2022-50. Review.

PMID:
25895896
29.

SI113, a specific inhibitor of the Sgk1 kinase activity that counteracts cancer cell proliferation.

D'Antona L, Amato R, Talarico C, Ortuso F, Menniti M, Dattilo V, Iuliano R, Gigliotti F, Artese A, Costa G, Schenone S, Musumeci F, Abbruzzese C, Botta L, Trapasso F, Alcaro S, Paggi MG, Perrotti N.

Cell Physiol Biochem. 2015;35(5):2006-18. doi: 10.1159/000374008. Epub 2015 Mar 27.

30.

SRC family kinase (SFK) inhibition reduces rhabdomyosarcoma cell growth in vitro and in vivo and triggers p38 MAP kinase-mediated differentiation.

Casini N, Forte IM, Mastrogiovanni G, Pentimalli F, Angelucci A, Festuccia C, Tomei V, Ceccherini E, Di Marzo D, Schenone S, Botta M, Giordano A, Indovina P.

Oncotarget. 2015 May 20;6(14):12421-35.

31.

Hck inhibitors as potential therapeutic agents in cancer and HIV infection.

Musumeci F, Schenone S, Brullo C, Desogus A, Botta L, Tintori C.

Curr Med Chem. 2015;22(13):1540-64. Review.

PMID:
25666803
32.

Bcr-Abl tyrosine kinase inhibitors: a patent review.

Desogus A, Schenone S, Brullo C, Tintori C, Musumeci F.

Expert Opin Ther Pat. 2015 Apr;25(4):397-412. doi: 10.1517/13543776.2015.1012155. Epub 2015 Feb 6. Review.

PMID:
25656651
33.

SRC family kinase inhibition through a new pyrazolo[3,4-d]pyrimidine derivative as a feasible approach for glioblastoma treatment.

Ceccherini E, Indovina P, Zamperini C, Dreassi E, Casini N, Cutaia O, Forte IM, Pentimalli F, Esposito L, Polito MS, Schenone S, Botta M, Giordano A.

J Cell Biochem. 2015 May;116(5):856-63. doi: 10.1002/jcb.25042.

PMID:
25521525
34.

The search for a common structural moiety among selected pharmacological correctors of the mutant CFTR chloride channel.

Nieddu E, Pollarolo B, Mazzei MT, Anzaldi M, Schenone S, Pedemonte N, Pesce E, Galietta LJ, Mazzei M.

Future Med Chem. 2014;6(17):1857-68. doi: 10.4155/fmc.14.118.

PMID:
25495980
35.

Combining X-ray crystallography and molecular modeling toward the optimization of pyrazolo[3,4-d]pyrimidines as potent c-Src inhibitors active in vivo against neuroblastoma.

Tintori C, Fallacara AL, Radi M, Zamperini C, Dreassi E, Crespan E, Maga G, Schenone S, Musumeci F, Brullo C, Richters A, Gasparrini F, Angelucci A, Festuccia C, Delle Monache S, Rauh D, Botta M.

J Med Chem. 2015 Jan 8;58(1):347-61. doi: 10.1021/jm5013159. Epub 2014 Dec 3.

PMID:
25469771
36.

Src inhibition potentiates antitumoral effect of paclitaxel by blocking tumor-induced angiogenesis.

Delle Monache S, Sanità P, Calgani A, Schenone S, Botta L, Angelucci A.

Exp Cell Res. 2014 Oct 15;328(1):20-31. doi: 10.1016/j.yexcr.2014.08.002. Epub 2014 Aug 14.

PMID:
25128812
37.

Protein-protein interactions and human cellular cofactors as new targets for HIV therapy.

Tintori C, Brai A, Fallacara AL, Fazi R, Schenone S, Botta M.

Curr Opin Pharmacol. 2014 Oct;18:1-8. doi: 10.1016/j.coph.2014.06.005. Epub 2014 Jul 1. Review.

PMID:
24993074
38.

Pyrazolo[3,4-d]pyrimidine Prodrugs: Strategic Optimization of the Aqueous Solubility of Dual Src/Abl Inhibitors.

Vignaroli G, Zamperini C, Dreassi E, Radi M, Angelucci A, Sanità P, Crespan E, Kissova M, Maga G, Schenone S, Musumeci F, Botta M.

ACS Med Chem Lett. 2013 May 20;4(7):622-6. doi: 10.1021/ml4000782. eCollection 2013 Jul 11.

39.

In silico identification and biological evaluation of novel selective serum/glucocorticoid-inducible kinase 1 inhibitors based on the pyrazolo-pyrimidine scaffold.

Ortuso F, Amato R, Artese A, D'antona L, Costa G, Talarico C, Gigliotti F, Bianco C, Trapasso F, Schenone S, Musumeci F, Botta L, Perrotti N, Alcaro S.

J Chem Inf Model. 2014 Jul 28;54(7):1828-32. doi: 10.1021/ci500235f. Epub 2014 Jun 13.

PMID:
24896223
40.

Biologically driven synthesis of pyrazolo[3,4-d]pyrimidines as protein kinase inhibitors: an old scaffold as a new tool for medicinal chemistry and chemical biology studies.

Schenone S, Radi M, Musumeci F, Brullo C, Botta M.

Chem Rev. 2014 Jul 23;114(14):7189-238. doi: 10.1021/cr400270z. Epub 2014 May 29. Review. No abstract available.

PMID:
24873489
41.

CYP-dependent metabolism of antitumor pyrazolo[3,4-d]pyrimidine derivatives is characterized by an oxidative dechlorination reaction.

Zamperini C, Dreassi E, Vignaroli G, Radi M, Dragoni S, Schenone S, Musumeci F, Valoti M, Antiochia R, Botta M.

Drug Metab Pharmacokinet. 2014;29(6):433-40. doi: 10.2133/dmpk.DMPK-13-RG-094. Epub 2014 May 20.

42.

Insight into the allosteric inhibition of Abl kinase.

Fallacara AL, Tintori C, Radi M, Schenone S, Botta M.

J Chem Inf Model. 2014 May 27;54(5):1325-38. doi: 10.1021/ci500060k. Epub 2014 May 8.

PMID:
24787133
43.

Proteomics and phosphoproteomics provide insights into the mechanism of action of a novel pyrazolo[3,4-d]pyrimidine Src inhibitor in human osteosarcoma.

Bernardini G, Laschi M, Serchi T, Spreafico A, Botta M, Schenone S, Arena S, Geminiani M, Scaloni A, Collodel G, Orlandini M, Niccolai N, Santucci A.

Mol Biosyst. 2014 Jun;10(6):1305-12. doi: 10.1039/c3mb70328b. Epub 2014 Mar 11.

PMID:
24615350
44.

Exploring the chemical space around the privileged pyrazolo[3,4-d]pyrimidine scaffold: toward novel allosteric inhibitors of T315I-mutated Abl.

Vignaroli G, Mencarelli M, Sementa D, Crespan E, Kissova M, Maga G, Schenone S, Radi M, Botta M.

ACS Comb Sci. 2014 Apr 14;16(4):168-75. doi: 10.1021/co500004e. Epub 2014 Mar 18.

PMID:
24597676
45.

Identification of new Fyn kinase inhibitors using a FLAP-based approach.

Poli G, Tuccinardi T, Rizzolio F, Caligiuri I, Botta L, Granchi C, Ortore G, Minutolo F, Schenone S, Martinelli A.

J Chem Inf Model. 2013 Oct 28;53(10):2538-47. doi: 10.1021/ci4002553. Epub 2013 Sep 16.

PMID:
24001328
46.

Identification of Hck inhibitors as hits for the development of antileukemia and anti-HIV agents.

Tintori C, Laurenzana I, La Rocca F, Falchi F, Carraro F, Ruiz A, Esté JA, Kissova M, Crespan E, Maga G, Biava M, Brullo C, Schenone S, Botta M.

ChemMedChem. 2013 Aug;8(8):1353-60. doi: 10.1002/cmdc.201300204. Epub 2013 Jun 28.

PMID:
23813855
47.

Design, synthesis, and biological evaluation of pyrazolo[3,4-d]pyrimidines active in vivo on the Bcr-Abl T315I mutant.

Radi M, Tintori C, Musumeci F, Brullo C, Zamperini C, Dreassi E, Fallacara AL, Vignaroli G, Crespan E, Zanoli S, Laurenzana I, Filippi I, Maga G, Schenone S, Angelucci A, Botta M.

J Med Chem. 2013 Jul 11;56(13):5382-94. doi: 10.1021/jm400233w. Epub 2013 Jun 20.

PMID:
23746084
48.

A class of pyrrole derivatives endowed with analgesic/anti-inflammatory activity.

Battilocchio C, Poce G, Alfonso S, Porretta GC, Consalvi S, Sautebin L, Pace S, Rossi A, Ghelardini C, Di Cesare Mannelli L, Schenone S, Giordani A, Di Francesco L, Patrignani P, Biava M.

Bioorg Med Chem. 2013 Jul 1;21(13):3695-701. doi: 10.1016/j.bmc.2013.04.031. Epub 2013 Apr 26.

PMID:
23680444
49.

A combination strategy to inhibit Pim-1: synergism between noncompetitive and ATP-competitive inhibitors.

Mori M, Tintori C, Christopher RS, Radi M, Schenone S, Musumeci F, Brullo C, Sanità P, Delle Monache S, Angelucci A, Kissova M, Crespan E, Maga G, Botta M.

ChemMedChem. 2013 Mar;8(3):484-96. doi: 10.1002/cmdc.201200480.

PMID:
23436791
50.

F508del-CFTR rescue: a matter of cell stress response.

Nieddu E, Pollarolo B, Merello L, Schenone S, Mazzei M.

Curr Pharm Des. 2013;19(19):3476-96. Review.

PMID:
23331026

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