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Items: 15

1.

Antibody drug conjugates of cleavable amino-alkyl and aryl maytansinoids.

Nittoli T, Kelly MP, Delfino F, Rudge J, Kunz A, Markotan T, Spink J, Chen Z, Shan J, Navarro E, Tait M, Provoncha K, Giurleo J, Zhao F, Jiang X, Hylton D, Makonnen S, Hickey C, Kirshner JR, Thurston G, Papadopoulos N.

Bioorg Med Chem. 2018 May 15;26(9):2271-2279. doi: 10.1016/j.bmc.2018.02.025. Epub 2018 Feb 21.

PMID:
29605304
2.

Preclinical Activity of the Novel Anti-Prolactin Receptor (PRLR) Antibody-Drug Conjugate REGN2878-DM1 in PRLR-Positive Breast Cancers.

Kelly MP, Hickey C, Makonnen S, Coetzee S, Jalal S, Wang Y, Delfino F, Shan J, Potocky TB, Chatterjee I, Andreev J, Kunz A, D'Souza C, Giurleo JT, Nittoli T, Trail PA, Thurston G, Kirshner JR.

Mol Cancer Ther. 2017 Jul;16(7):1299-1311. doi: 10.1158/1535-7163.MCT-16-0839. Epub 2017 Apr 4.

3.

Bispecific Antibodies and Antibody-Drug Conjugates (ADCs) Bridging HER2 and Prolactin Receptor Improve Efficacy of HER2 ADCs.

Andreev J, Thambi N, Perez Bay AE, Delfino F, Martin J, Kelly MP, Kirshner JR, Rafique A, Kunz A, Nittoli T, MacDonald D, Daly C, Olson W, Thurston G.

Mol Cancer Ther. 2017 Apr;16(4):681-693. doi: 10.1158/1535-7163.MCT-16-0658. Epub 2017 Jan 20.

4.

Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.

Zapf CW, Bloom JD, Li Z, Dushin RG, Nittoli T, Otteng M, Nikitenko A, Golas JM, Liu H, Lucas J, Boschelli F, Vogan E, Olland A, Johnson M, Levin JI.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4602-7. doi: 10.1016/j.bmcl.2011.05.102. Epub 2011 Jun 27.

PMID:
21715165
5.

Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activity.

Zapf CW, Bloom JD, McBean JL, Dushin RG, Nittoli T, Otteng M, Ingalls C, Golas JM, Liu H, Lucas J, Boschelli F, Hu Y, Vogan E, Levin JI.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3411-6. doi: 10.1016/j.bmcl.2011.03.112. Epub 2011 Apr 5.

PMID:
21515049
6.

Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity.

Zapf CW, Bloom JD, McBean JL, Dushin RG, Nittoli T, Ingalls C, Sutherland AG, Sonye JP, Eid CN, Golas J, Liu H, Boschelli F, Hu Y, Vogan E, Levin JI.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2278-82. doi: 10.1016/j.bmcl.2011.02.101. Epub 2011 Feb 28.

PMID:
21420297
7.

The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).

Nittoli T, Dushin RG, Ingalls C, Cheung K, Floyd MB, Fraser H, Olland A, Hu Y, Grosu G, Han X, Arndt K, Guo B, Wissner A.

Eur J Med Chem. 2010 Apr;45(4):1379-86. doi: 10.1016/j.ejmech.2009.12.036. Epub 2009 Dec 28.

PMID:
20074837
8.

Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles.

Dushin RG, Nittoli T, Ingalls C, Boschelli DH, Cole DC, Wissner A, Lee J, Yang X, Morgan P, Brennan A, Chaudhary D.

Bioorg Med Chem Lett. 2009 May 1;19(9):2461-3. doi: 10.1016/j.bmcl.2009.03.053. Epub 2009 Mar 18.

PMID:
19345579
9.

Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.

Wissner A, Fraser HL, Ingalls CL, Dushin RG, Floyd MB, Cheung K, Nittoli T, Ravi MR, Tan X, Loganzo F.

Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. Epub 2007 Mar 23.

PMID:
17416531
10.

Identification of anthranilic acid derivatives as a novel class of allosteric inhibitors of hepatitis C NS5B polymerase.

Nittoli T, Curran K, Insaf S, DiGrandi M, Orlowski M, Chopra R, Agarwal A, Howe AY, Prashad A, Floyd MB, Johnson B, Sutherland A, Wheless K, Feld B, O'Connell J, Mansour TS, Bloom J.

J Med Chem. 2007 May 3;50(9):2108-16. Epub 2007 Apr 3. Erratum in: J Med Chem. 2007 Nov 29;50(24):6290.

PMID:
17402724
11.

2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.

Wissner A, Floyd MB, Johnson BD, Fraser H, Ingalls C, Nittoli T, Dushin RG, Discafani C, Nilakantan R, Marini J, Ravi M, Cheung K, Tan X, Musto S, Annable T, Siegel MM, Loganzo F.

J Med Chem. 2005 Dec 1;48(24):7560-81.

PMID:
16302797
12.
13.

Design, synthesis, and evaluation of a pyrrolinone-based matrix metalloprotease inhibitor.

Smith AB 3rd, Nittoli T, Sprengeler PA, Duan JJ, Liu RQ, Hirschmann RF.

Org Lett. 2000 Nov 30;2(24):3809-12.

PMID:
11101425
14.
15.

Silanediols: A New Class of Potent Protease Inhibitors.

Sieburth SM, Nittoli T, Mutahi AM, Guo L.

Angew Chem Int Ed Engl. 1998 Apr 3;37(6):812-814. doi: 10.1002/(SICI)1521-3773(19980403)37:6<812::AID-ANIE812>3.0.CO;2-I.

PMID:
29711373

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