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Items: 1 to 50 of 177

1.

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).

Woodward HL, Innocenti P, Cheung KJ, Hayes A, Roberts J, Henley AT, Faisal A, Mak GW, Box G, Westwood IM, Cronin N, Carter M, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Burke R, Broccatelli F, van Montfort RLM, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S.

J Med Chem. 2018 Sep 10. doi: 10.1021/acs.jmedchem.8b00690. [Epub ahead of print]

PMID:
30199249
2.

Correction to: An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models.

Banerji U, Sain N, Sharp SY, Valenti M, Asad Y, Ruddle R, Raynaud F, Walton M, Eccles SA, Judson I, Jackman AL, Workman P.

Cancer Chemother Pharmacol. 2018 Sep 1. doi: 10.1007/s00280-018-3674-9. [Epub ahead of print]

PMID:
30173339
3.

Evaluating Imaging Biomarkers of Acquired Resistance to Targeted EGFR Therapy in Xenograft Models of Human Head and Neck Squamous Cell Carcinoma.

Baker LCJ, Sikka A, Price JM, Boult JKR, Lepicard EY, Box G, Jamin Y, Spinks TJ, Kramer-Marek G, Leach MO, Eccles SA, Box C, Robinson SP.

Front Oncol. 2018 Jul 23;8:271. doi: 10.3389/fonc.2018.00271. eCollection 2018.

4.

HSF1 Is Essential for Myeloma Cell Survival and A Promising Therapeutic Target.

Fok JHL, Hedayat S, Zhang L, Aronson LI, Mirabella F, Pawlyn C, Bright MD, Wardell CP, Keats JJ, De Billy E, Rye CS, Chessum NEA, Jones K, Morgan GJ, Eccles SA, Workman P, Davies FE.

Clin Cancer Res. 2018 May 15;24(10):2395-2407. doi: 10.1158/1078-0432.CCR-17-1594. Epub 2018 Feb 1.

PMID:
29391353
5.

Functional imaging and circulating biomarkers of response to regorafenib in treatment-refractory metastatic colorectal cancer patients in a prospective phase II study.

Khan K, Rata M, Cunningham D, Koh DM, Tunariu N, Hahne JC, Vlachogiannis G, Hedayat S, Marchetti S, Lampis A, Damavandi MD, Lote H, Rana I, Williams A, Eccles SA, Fontana E, Collins D, Eltahir Z, Rao S, Watkins D, Starling N, Thomas J, Kalaitzaki E, Fotiadis N, Begum R, Bali M, Rugge M, Temple E, Fassan M, Chau I, Braconi C, Valeri N.

Gut. 2018 Aug;67(8):1484-1492. doi: 10.1136/gutjnl-2017-314178. Epub 2017 Aug 8.

6.

Evaluation of the Response of Intracranial Xenografts to VEGF Signaling Inhibition Using Multiparametric MRI.

Boult JKR, Box G, Vinci M, Perryman L, Eccles SA, Jones C, Robinson SP.

Neoplasia. 2017 Sep;19(9):684-694. doi: 10.1016/j.neo.2017.05.007. Epub 2017 Aug 4.

7.

Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma.

Ang JE, Pal A, Asad YJ, Henley AT, Valenti M, Box G, de Haven Brandon A, Revell VL, Skene DJ, Venturi M, Rueger R, Meresse V, Eccles SA, de Bono JS, Kaye SB, Workman P, Banerji U, Raynaud FI.

Mol Cancer Ther. 2017 Oct;16(10):2315-2323. doi: 10.1158/1535-7163.MCT-16-0881. Epub 2017 Jun 21.

8.

Coupling between the TRPC3 ion channel and the NCX1 transporter contributed to VEGF-induced ERK1/2 activation and angiogenesis in human primary endothelial cells.

Andrikopoulos P, Eccles SA, Yaqoob MM.

Cell Signal. 2017 Sep;37:12-30. doi: 10.1016/j.cellsig.2017.05.013. Epub 2017 May 20.

PMID:
28535874
9.

High ASMA+ Fibroblasts and Low Cytoplasmic HMGB1+ Breast Cancer Cells Predict Poor Prognosis.

Amornsupak K, Jamjuntra P, Warnnissorn M, O-Charoenrat P, Sa-Nguanraksa D, Thuwajit P, Eccles SA, Thuwajit C.

Clin Breast Cancer. 2017 Oct;17(6):441-452.e2. doi: 10.1016/j.clbc.2017.04.007. Epub 2017 Apr 21.

10.

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy.

Faisal A, Mak GWY, Gurden MD, Xavier CPR, Anderhub SJ, Innocenti P, Westwood IM, Naud S, Hayes A, Box G, Valenti MR, De Haven Brandon AK, O'Fee L, Schmitt J, Woodward HL, Burke R, vanMontfort RLM, Blagg J, Raynaud FI, Eccles SA, Hoelder S, Linardopoulos S.

Br J Cancer. 2017 Apr 25;116(9):1166-1176. doi: 10.1038/bjc.2017.75. Epub 2017 Mar 23.

11.

Noninvasive Imaging of Cycling Hypoxia in Head and Neck Cancer Using Intrinsic Susceptibility MRI.

Panek R, Welsh L, Baker LCJ, Schmidt MA, Wong KH, Riddell AM, Koh DM, Dunlop A, Mcquaid D, d'Arcy JA, Bhide SA, Harrington KJ, Nutting CM, Hopkinson G, Richardson C, Box C, Eccles SA, Leach MO, Robinson SP, Newbold KL.

Clin Cancer Res. 2017 Aug 1;23(15):4233-4241. doi: 10.1158/1078-0432.CCR-16-1209. Epub 2017 Mar 17.

12.

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.

Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K.

J Med Chem. 2017 Jan 12;60(1):180-201. doi: 10.1021/acs.jmedchem.6b01055. Epub 2016 Dec 22.

13.

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases.

Clarke PA, Ortiz-Ruiz MJ, TePoele R, Adeniji-Popoola O, Box G, Court W, Czasch S, El Bawab S, Esdar C, Ewan K, Gowan S, De Haven Brandon A, Hewitt P, Hobbs SM, Kaufmann W, Mallinger A, Raynaud F, Roe T, Rohdich F, Schiemann K, Simon S, Schneider R, Valenti M, Weigt S, Blagg J, Blaukat A, Dale TC, Eccles SA, Hecht S, Urbahns K, Workman P, Wienke D.

Elife. 2016 Dec 9;5. pii: e20722. doi: 10.7554/eLife.20722.

14.

Pre-clinical quantitative imaging and mouse-specific dosimetry for 111In-labelled radiotracers.

Denis-Bacelar AM, Cronin SE, Da Pieve C, Paul RL, Eccles SA, Spinks TJ, Box C, Hall A, Sosabowski JK, Kramer-Marek G, Flux GD.

EJNMMI Res. 2016 Dec;6(1):85. Epub 2016 Nov 25.

15.

Investigating intracranial tumour growth patterns with multiparametric MRI incorporating Gd-DTPA and USPIO-enhanced imaging.

Boult JK, Borri M, Jury A, Popov S, Box G, Perryman L, Eccles SA, Jones C, Robinson SP.

NMR Biomed. 2016 Nov;29(11):1608-1617. doi: 10.1002/nbm.3594. Epub 2016 Sep 27.

16.

Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.

Czodrowski P, Mallinger A, Wienke D, Esdar C, Pöschke O, Busch M, Rohdich F, Eccles SA, Ortiz-Ruiz MJ, Schneider R, Raynaud FI, Clarke PA, Musil D, Schwarz D, Dale T, Urbahns K, Blagg J, Schiemann K.

J Med Chem. 2016 Oct 27;59(20):9337-9349. Epub 2016 Oct 7.

17.

2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.

Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R, Schwarz D, Musil D, Burke R, Urbahns K, Workman P, Wienke D, Clarke PA, Raynaud FI, Eccles SA, Esdar C, Rohdich F, Blagg J.

ACS Med Chem Lett. 2016 Mar 28;7(6):573-8. doi: 10.1021/acsmedchemlett.6b00022. eCollection 2016 Jun 9.

18.

In Vitro Assays for Endothelial Cell Functions Required for Angiogenesis: Proliferation, Motility, Tubular Differentiation, and Matrix Proteolysis.

Eccles SA, Court W, Patterson L.

Methods Mol Biol. 2016;1430:121-47. doi: 10.1007/978-1-4939-3628-1_8.

PMID:
27172950
19.

Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).

Osborne JD, Matthews TP, McHardy T, Proisy N, Cheung KM, Lainchbury M, Brown N, Walton MI, Eve PD, Boxall KJ, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Jamin Y, Robinson SP, Westwood IM, van Montfort RL, Leonard PM, Lamers MB, Reader JC, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I.

J Med Chem. 2016 Jun 9;59(11):5221-37. doi: 10.1021/acs.jmedchem.5b01938. Epub 2016 May 23.

20.

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.

Innocenti P, Woodward HL, Solanki S, Naud S, Westwood IM, Cronin N, Hayes A, Roberts J, Henley AT, Baker R, Faisal A, Mak GW, Box G, Valenti M, De Haven Brandon A, O'Fee L, Saville H, Schmitt J, Matijssen B, Burke R, van Montfort RL, Raynaud FI, Eccles SA, Linardopoulos S, Blagg J, Hoelder S.

J Med Chem. 2016 Apr 28;59(8):3671-88. doi: 10.1021/acs.jmedchem.5b01811. Epub 2016 Apr 7.

21.

Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation.

Ang JE, Pandher R, Ang JC, Asad YJ, Henley AT, Valenti M, Box G, de Haven Brandon A, Baird RD, Friedman L, Derynck M, Vanhaesebroeck B, Eccles SA, Kaye SB, Workman P, de Bono JS, Raynaud FI.

Mol Cancer Ther. 2016 Jun;15(6):1412-24. doi: 10.1158/1535-7163.MCT-15-0815. Epub 2016 Apr 5.

22.

Synthesis and Evaluation of a 2,11-Cembranoid-Inspired Library.

Welford AJ, Caldwell JJ, Liu M, Richards M, Brown N, Lomas C, Tizzard GJ, Pitak MB, Coles SJ, Eccles SA, Raynaud FI, Collins I.

Chemistry. 2016 Apr 11;22(16):5657-64. doi: 10.1002/chem.201505093. Epub 2016 Mar 1.

23.

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.

Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J.

Bioorg Med Chem Lett. 2016 Mar 1;26(5):1443-51. doi: 10.1016/j.bmcl.2016.01.062. Epub 2016 Jan 22.

PMID:
26852363
24.

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.

Mallinger A, Schiemann K, Rink C, Stieber F, Calderini M, Crumpler S, Stubbs M, Adeniji-Popoola O, Poeschke O, Busch M, Czodrowski P, Musil D, Schwarz D, Ortiz-Ruiz MJ, Schneider R, Thai C, Valenti M, de Haven Brandon A, Burke R, Workman P, Dale T, Wienke D, Clarke PA, Esdar C, Raynaud FI, Eccles SA, Rohdich F, Blagg J.

J Med Chem. 2016 Feb 11;59(3):1078-101. doi: 10.1021/acs.jmedchem.5b01685. Epub 2016 Jan 21.

25.

PAK4 promotes kinase-independent stabilization of RhoU to modulate cell adhesion.

Dart AE, Box GM, Court W, Gale ME, Brown JP, Pinder SE, Eccles SA, Wells CM.

J Cell Biol. 2015 Nov 23;211(4):863-79. doi: 10.1083/jcb.201501072.

26.

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D, Schwarz D, Schneider K, Stubbs M, Ewan K, Fraser E, TePoele R, Court W, Box G, Valenti M, de Haven Brandon A, Gowan S, Rohdich F, Raynaud F, Schneider R, Poeschke O, Blaukat A, Workman P, Schiemann K, Eccles SA, Wienke D, Blagg J.

Nat Chem Biol. 2015 Dec;11(12):973-980. doi: 10.1038/nchembio.1952. Epub 2015 Oct 26.

27.

The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.

Walton MI, Eve PD, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Boxall KJ, Tall M, Swales K, Matthews TP, McHardy T, Lainchbury M, Osborne J, Hunter JE, Perkins ND, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Collins I, Garrett MD.

Oncotarget. 2016 Jan 19;7(3):2329-42. doi: 10.18632/oncotarget.4919.

28.

Three-dimensional (3D) tumor spheroid invasion assay.

Vinci M, Box C, Eccles SA.

J Vis Exp. 2015 May 1;(99):e52686. doi: 10.3791/52686.

29.

Endothelial Angiogenesis and Barrier Function in Response to Thrombin Require Ca2+ Influx through the Na+/Ca2+ Exchanger.

Andrikopoulos P, Kieswich J, Harwood SM, Baba A, Matsuda T, Barbeau O, Jones K, Eccles SA, Yaqoob MM.

J Biol Chem. 2015 Jul 24;290(30):18412-28. doi: 10.1074/jbc.M114.628156. Epub 2015 May 15.

30.

Acquired resistance to EGFR tyrosine kinase inhibitors alters the metabolism of human head and neck squamous carcinoma cells and xenograft tumours.

Beloueche-Babari M, Box C, Arunan V, Parkes HG, Valenti M, De Haven Brandon A, Jackson LE, Eccles SA, Leach MO.

Br J Cancer. 2015 Mar 31;112(7):1206-14. doi: 10.1038/bjc.2015.86.

31.

Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.

Mallinger A, Crumpler S, Pichowicz M, Waalboer D, Stubbs M, Adeniji-Popoola O, Wood B, Smith E, Thai C, Henley AT, Georgi K, Court W, Hobbs S, Box G, Ortiz-Ruiz MJ, Valenti M, De Haven Brandon A, TePoele R, Leuthner B, Workman P, Aherne W, Poeschke O, Dale T, Wienke D, Esdar C, Rohdich F, Raynaud F, Clarke PA, Eccles SA, Stieber F, Schiemann K, Blagg J.

J Med Chem. 2015 Feb 26;58(4):1717-35. doi: 10.1021/jm501436m. Epub 2015 Feb 13.

32.

Exploring the biomechanical properties of brain malignancies and their pathologic determinants in vivo with magnetic resonance elastography.

Jamin Y, Boult JKR, Li J, Popov S, Garteiser P, Ulloa JL, Cummings C, Box G, Eccles SA, Jones C, Waterton JC, Bamber JC, Sinkus R, Robinson SP.

Cancer Res. 2015 Apr 1;75(7):1216-1224. doi: 10.1158/0008-5472.CAN-14-1997. Epub 2015 Feb 11.

33.

Cancer-associated fibroblasts induce high mobility group box 1 and contribute to resistance to doxorubicin in breast cancer cells.

Amornsupak K, Insawang T, Thuwajit P, O-Charoenrat P, Eccles SA, Thuwajit C.

BMC Cancer. 2014 Dec 15;14:955. doi: 10.1186/1471-2407-14-955.

34.

HIF-1α-independent hypoxia-induced rapid PTK6 stabilization is associated with increased motility and invasion.

Pires IM, Blokland NJ, Broos AW, Poujade FA, Senra JM, Eccles SA, Span PN, Harvey AJ, Hammond EM.

Cancer Biol Ther. 2014 Oct;15(10):1350-7. doi: 10.4161/cbt.29822. Epub 2014 Jul 14.

35.

Preclinical evaluation of imaging biomarkers for prostate cancer bone metastasis and response to cabozantinib.

Graham TJ, Box G, Tunariu N, Crespo M, Spinks TJ, Miranda S, Attard G, de Bono J, Eccles SA, Davies FE, Robinson SP.

J Natl Cancer Inst. 2014 Apr;106(4):dju033. doi: 10.1093/jnci/dju033. Epub 2014 Mar 14.

PMID:
24634505
36.

Critical research gaps and translational priorities for the successful prevention and treatment of breast cancer.

Eccles SA, Aboagye EO, Ali S, Anderson AS, Armes J, Berditchevski F, Blaydes JP, Brennan K, Brown NJ, Bryant HE, Bundred NJ, Burchell JM, Campbell AM, Carroll JS, Clarke RB, Coles CE, Cook GJ, Cox A, Curtin NJ, Dekker LV, Silva Idos S, Duffy SW, Easton DF, Eccles DM, Edwards DR, Edwards J, Evans D, Fenlon DF, Flanagan JM, Foster C, Gallagher WM, Garcia-Closas M, Gee JM, Gescher AJ, Goh V, Groves AM, Harvey AJ, Harvie M, Hennessy BT, Hiscox S, Holen I, Howell SJ, Howell A, Hubbard G, Hulbert-Williams N, Hunter MS, Jasani B, Jones LJ, Key TJ, Kirwan CC, Kong A, Kunkler IH, Langdon SP, Leach MO, Mann DJ, Marshall JF, Martin L, Martin SG, Macdougall JE, Miles DW, Miller WR, Morris JR, Moss SM, Mullan P, Natrajan R, O'Connor JP, O'Connor R, Palmieri C, Pharoah PD, Rakha EA, Reed E, Robinson SP, Sahai E, Saxton JM, Schmid P, Smalley MJ, Speirs V, Stein R, Stingl J, Streuli CH, Tutt AN, Velikova G, Walker RA, Watson CJ, Williams KJ, Young LS, Thompson AM.

Breast Cancer Res. 2013 Oct 1;15(5):R92. doi: 10.1186/bcr3493. Review.

37.

Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).

Naud S, Westwood IM, Faisal A, Sheldrake P, Bavetsias V, Atrash B, Cheung KM, Liu M, Hayes A, Schmitt J, Wood A, Choi V, Boxall K, Mak G, Gurden M, Valenti M, de Haven Brandon A, Henley A, Baker R, McAndrew C, Matijssen B, Burke R, Hoelder S, Eccles SA, Raynaud FI, Linardopoulos S, van Montfort RL, Blagg J.

J Med Chem. 2013 Dec 27;56(24):10045-65. doi: 10.1021/jm401395s. Epub 2013 Dec 2.

38.

Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX.

Powers MV, Valenti M, Miranda S, Maloney A, Eccles SA, Thomas G, Clarke PA, Workman P.

Oncotarget. 2013 Nov;4(11):1963-75.

39.

Dual blockade of the PI3K/AKT/mTOR (AZD8055) and RAS/MEK/ERK (AZD6244) pathways synergistically inhibits rhabdomyosarcoma cell growth in vitro and in vivo.

Renshaw J, Taylor KR, Bishop R, Valenti M, De Haven Brandon A, Gowan S, Eccles SA, Ruddle RR, Johnson LD, Raynaud FI, Selfe JL, Thway K, Pietsch T, Pearson AD, Shipley J.

Clin Cancer Res. 2013 Nov 1;19(21):5940-51. doi: 10.1158/1078-0432.CCR-13-0850. Epub 2013 Aug 5.

40.

Kurt Hellmann D. M., D. Phil. Oxon 1922–2013.

Eccles SA.

Clin Exp Metastasis. 2013 Jun;30(5):553-4. No abstract available.

PMID:
23844428
41.

A cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells.

Miranda E, Nordgren IK, Male AL, Lawrence CE, Hoakwie F, Cuda F, Court W, Fox KR, Townsend PA, Packham GK, Eccles SA, Tavassoli A.

J Am Chem Soc. 2013 Jul 17;135(28):10418-25. doi: 10.1021/ja402993u. Epub 2013 Jul 9.

42.

A novel serum protein signature associated with resistance to epidermal growth factor receptor tyrosine kinase inhibitors in head and neck squamous cell carcinoma.

Box C, Mendiola M, Gowan S, Box GM, Valenti M, Brandon Ade H, Al-Lazikani B, Rogers SJ, Wilkins A, Harrington KJ, Eccles SA.

Eur J Cancer. 2013 Jul;49(11):2512-21. doi: 10.1016/j.ejca.2013.03.011. Epub 2013 Apr 10.

PMID:
23582742
43.

Tumor spheroid-based migration assays for evaluation of therapeutic agents.

Vinci M, Box C, Zimmermann M, Eccles SA.

Methods Mol Biol. 2013;986:253-66. doi: 10.1007/978-1-62703-311-4_16.

PMID:
23436417
44.

Two-dimensional vs. three-dimensional in vitro tumor migration and invasion assays.

Zimmermann M, Box C, Eccles SA.

Methods Mol Biol. 2013;986:227-52. doi: 10.1007/978-1-62703-311-4_15.

PMID:
23436416
45.

Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.

Lainchbury M, Matthews TP, McHardy T, Boxall KJ, Walton MI, Eve PD, Hayes A, Valenti MR, de Haven Brandon AK, Box G, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Garrett MD, Collins I.

J Med Chem. 2012 Nov 26;55(22):10229-40. doi: 10.1021/jm3012933. Epub 2012 Oct 19.

46.

Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.

Bavetsias V, Crumpler S, Sun C, Avery S, Atrash B, Faisal A, Moore AS, Kosmopoulou M, Brown N, Sheldrake PW, Bush K, Henley A, Box G, Valenti M, de Haven Brandon A, Raynaud FI, Workman P, Eccles SA, Bayliss R, Linardopoulos S, Blagg J.

J Med Chem. 2012 Oct 25;55(20):8721-34. doi: 10.1021/jm300952s. Epub 2012 Oct 8.

47.

CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs.

Walton MI, Eve PD, Hayes A, Valenti MR, De Haven Brandon AK, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, Chesler L, Raynaud FI, Eccles SA, Collins I, Garrett MD.

Clin Cancer Res. 2012 Oct 15;18(20):5650-61. doi: 10.1158/1078-0432.CCR-12-1322. Epub 2012 Aug 28.

48.

Erratum to: Kurt Hellmann D.M., D.Phil. Oxon. A happy 90th birthday!

Eccles SA, Steiner RK.

Clin Exp Metastasis. 2015 Jun;32(5):517-20. doi: 10.1007/s10585-012-9513-1. No abstract available.

PMID:
22872374
49.

The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma.

Berry T, Luther W, Bhatnagar N, Jamin Y, Poon E, Sanda T, Pei D, Sharma B, Vetharoy WR, Hallsworth A, Ahmad Z, Barker K, Moreau L, Webber H, Wang W, Liu Q, Perez-Atayde A, Rodig S, Cheung NK, Raynaud F, Hallberg B, Robinson SP, Gray NS, Pearson AD, Eccles SA, Chesler L, George RE.

Cancer Cell. 2012 Jul 10;22(1):117-30. doi: 10.1016/j.ccr.2012.06.001.

50.

AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity.

Yap TA, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD.

Clin Cancer Res. 2012 Jul 15;18(14):3912-23. doi: 10.1158/1078-0432.CCR-11-3313. Epub 2012 Jul 10.

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