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Items: 21

1.

Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.

Methot JL, Zhou H, Kattar SD, McGowan MA, Wilson K, Garcia Y, Deng Y, Altman M, Fradera X, Lesburg C, Fischmann T, Li C, Alves S, Shah S, Fernandez R, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Yu H, Bass A, Kemper R, Gatto NT, LaFranco-Scheuch L, Trotter BW, Guzi T, Katz JD.

J Med Chem. 2019 May 9;62(9):4370-4382. doi: 10.1021/acs.jmedchem.8b01818. Epub 2019 Apr 22.

PMID:
30986068
2.

Precision Targeted Therapy with BLU-667 for RET-Driven Cancers.

Subbiah V, Gainor JF, Rahal R, Brubaker JD, Kim JL, Maynard M, Hu W, Cao Q, Sheets MP, Wilson D, Wilson KJ, DiPietro L, Fleming P, Palmer M, Hu MI, Wirth L, Brose MS, Ou SI, Taylor M, Garralda E, Miller S, Wolf B, Lengauer C, Guzi T, Evans EK.

Cancer Discov. 2018 Jul;8(7):836-849. doi: 10.1158/2159-8290.CD-18-0338. Epub 2018 Apr 15.

3.

A precision therapy against cancers driven by KIT/PDGFRA mutations.

Evans EK, Gardino AK, Kim JL, Hodous BL, Shutes A, Davis A, Zhu XJ, Schmidt-Kittler O, Wilson D, Wilson K, DiPietro L, Zhang Y, Brooijmans N, LaBranche TP, Wozniak A, Gebreyohannes YK, Schöffski P, Heinrich MC, DeAngelo DJ, Miller S, Wolf B, Kohl N, Guzi T, Lydon N, Boral A, Lengauer C.

Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690. doi: 10.1126/scitranslmed.aao1690.

PMID:
29093181
4.

First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.

Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N, Shutes A, Winter C, Lengauer C, Kohl NE, Guzi T.

Cancer Discov. 2015 Apr;5(4):424-37. doi: 10.1158/2159-8290.CD-14-1029. Epub 2015 Mar 16.

5.

Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.

Ma Y, Lahue BR, Gibeau CR, Shipps GW Jr, Bogen SL, Wang Y, Guo Z, Guzi TJ.

ACS Med Chem Lett. 2014 Feb 24;5(5):572-5. doi: 10.1021/ml500019s. eCollection 2014 May 8.

6.

The identification of novel 5'-amino gemcitabine analogs as potent RRM1 inhibitors.

Labroli MA, Dwyer MP, Shen R, Popovici-Muller J, Pu Q, Wyss D, McCoy M, Barrett D, Davis N, Seghezzi W, Shanahan F, Taricani L, Beaumont M, Malinao MC, Parry D, Guzi TJ.

Bioorg Med Chem. 2014 Apr 1;22(7):2303-10. doi: 10.1016/j.bmc.2014.02.007. Epub 2014 Feb 15.

PMID:
24588962
7.

Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.

Dwyer MP, Keertikar K, Paruch K, Alvarez C, Labroli M, Poker C, Fischmann TO, Mayer-Ezell R, Bond R, Wang Y, Azevedo R, Guzi TJ.

Bioorg Med Chem Lett. 2013 Nov 15;23(22):6178-82. doi: 10.1016/j.bmcl.2013.08.110. Epub 2013 Sep 7.

PMID:
24091081
8.

Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening.

Guzi TJ, Paruch K, Dwyer MP, Labroli M, Shanahan F, Davis N, Taricani L, Wiswell D, Seghezzi W, Penaflor E, Bhagwat B, Wang W, Gu D, Hsieh Y, Lee S, Liu M, Parry D.

Mol Cancer Ther. 2011 Apr;10(4):591-602. doi: 10.1158/1535-7163.MCT-10-0928. Epub 2011 Feb 14.

9.

Phenotypic enhancement of thymidylate synthetase pathway inhibitors following ablation of Neil1 DNA glycosylase/lyase.

Taricani L, Shanahan F, Pierce RH, Guzi TJ, Parry D.

Cell Cycle. 2010 Dec 15;9(24):4876-83. Epub 2010 Dec 15.

PMID:
21131780
10.

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.

Dwyer MP, Paruch K, Labroli M, Alvarez C, Keertikar KM, Poker C, Rossman R, Fischmann TO, Duca JS, Madison V, Parry D, Davis N, Seghezzi W, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):467-70. doi: 10.1016/j.bmcl.2010.10.113. Epub 2010 Oct 27.

PMID:
21094608
11.

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2.

Labroli M, Paruch K, Dwyer MP, Alvarez C, Keertikar K, Poker C, Rossman R, Duca JS, Fischmann TO, Madison V, Parry D, Davis N, Seghezzi W, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):471-4. doi: 10.1016/j.bmcl.2010.10.114. Epub 2010 Oct 28.

PMID:
21094607
12.

Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors.

Zhao L, Zhang Y, Dai C, Guzi T, Wiswell D, Seghezzi W, Parry D, Fischmann T, Siddiqui MA.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7216-21. doi: 10.1016/j.bmcl.2010.10.105. Epub 2010 Oct 26.

PMID:
21074424
13.

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann T, Hruza A, Madison V, Nomeir AA, Wang Y, Kirschmeier P, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ.

ACS Med Chem Lett. 2010 May 17;1(5):204-8. doi: 10.1021/ml100051d. eCollection 2010 Aug 12.

14.

Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor.

Parry D, Guzi T, Shanahan F, Davis N, Prabhavalkar D, Wiswell D, Seghezzi W, Paruch K, Dwyer MP, Doll R, Nomeir A, Windsor W, Fischmann T, Wang Y, Oft M, Chen T, Kirschmeier P, Lees EM.

Mol Cancer Ther. 2010 Aug;9(8):2344-53. doi: 10.1158/1535-7163.MCT-10-0324. Epub 2010 Jul 27.

15.

Structure-guided discovery of cyclin-dependent kinase inhibitors.

Fischmann TO, Hruza A, Duca JS, Ramanathan L, Mayhood T, Windsor WT, Le HV, Guzi TJ, Dwyer MP, Paruch K, Doll RJ, Lees E, Parry D, Seghezzi W, Madison V.

Biopolymers. 2008 May;89(5):372-9.

PMID:
17937404
16.

Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.

Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann TO, Hruza A, Madison V, Nomeir AA, Wang Y, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6220-3. Epub 2007 Sep 8.

PMID:
17904841
17.

Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.

Dwyer MP, Paruch K, Alvarez C, Doll RJ, Keertikar K, Duca J, Fischmann TO, Hruza A, Madison V, Lees E, Parry D, Seghezzi W, Sgambellone N, Shanahan F, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. Epub 2007 Sep 8.

PMID:
17904366
18.

CYC-202 Cyclacel.

Guzi T.

Curr Opin Investig Drugs. 2004 Dec;5(12):1311-8. Review.

PMID:
15648953
19.
20.

Analogues of 1-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo-[5,6]-cyclohepta [1,2-b]pyridin-11-yl)piperidine as inhibitors of farnesyl protein transferase.

Afonso A, Weinstein J, Kelly J, Wolin R, Rosenblum SB, Connolly M, Guzi T, James L, Carr D, Patton R, Bishop WR, Kirshmeier P, Liu M, Heimark L, Chen KJ, Nomeir AA.

Bioorg Med Chem. 1999 Sep;7(9):1845-55.

PMID:
10530932
21.

Rational design and molecular effects of a new topoisomerase II inhibitor, azatoxin.

Leteurtre F, Madalengoitia J, Orr A, Guzi TJ, Lehnert E, Macdonald T, Pommier Y.

Cancer Res. 1992 Aug 15;52(16):4478-83. Erratum in: Cancer Res 1992 Nov 1;52(21):6136. Cuzi TJ [corrected to Guzi TJ].

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