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Items: 1 to 50 of 89

1.

Differences in Signaling Patterns on PI3K Inhibition Reveal Context Specificity in KRAS-Mutant Cancers.

Stewart A, Coker EA, Pölsterl S, Georgiou A, Minchom AR, Carreira S, Cunningham D, O'Brien ME, Raynaud FI, de Bono JS, Al-Lazikani B, Banerji U.

Mol Cancer Ther. 2019 Aug;18(8):1396-1404. doi: 10.1158/1535-7163.MCT-18-0727. Epub 2019 Jul 1.

PMID:
31262731
2.

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.

Le Bihan YV, Lanigan RM, Atrash B, McLaughlin MG, Velupillai S, Malcolm AG, England KS, Ruda GF, Mok NY, Tumber A, Tomlin K, Saville H, Shehu E, McAndrew C, Carmichael L, Bennett JM, Jeganathan F, Eve P, Donovan A, Hayes A, Wood F, Raynaud FI, Fedorov O, Brennan PE, Burke R, van Montfort RLM, Rossanese OW, Blagg J, Bavetsias V.

Eur J Med Chem. 2019 Sep 1;177:316-337. doi: 10.1016/j.ejmech.2019.05.041. Epub 2019 May 17.

3.

Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species.

Wood FL, Shepherd S, Hayes A, Liu M, Grira K, Mok Y, Atrash B, Faisal A, Bavetsias V, Linardopoulos S, Blagg J, Raynaud FI.

Eur J Pharm Sci. 2019 Apr 3. pii: S0928-0987(19)30142-3. doi: 10.1016/j.ejps.2019.04.004. [Epub ahead of print]

4.

Effect of acute total sleep deprivation on plasma melatonin, cortisol and metabolite rhythms in females.

Honma A, Revell VL, Gunn PJ, Davies SK, Middleton B, Raynaud FI, Skene DJ.

Eur J Neurosci. 2019 Mar 30. doi: 10.1111/ejn.14411. [Epub ahead of print]

PMID:
30929284
5.

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 27;61(18):8226-8240. doi: 10.1021/acs.jmedchem.8b00690. Epub 2018 Sep 10.

6.

Vistusertib (dual m-TORC1/2 inhibitor) in combination with paclitaxel in patients with high-grade serous ovarian and squamous non-small-cell lung cancer.

Basu B, Krebs MG, Sundar R, Wilson RH, Spicer J, Jones R, Brada M, Talbot DC, Steele N, Ingles Garces AH, Brugger W, Harrington EA, Evans J, Hall E, Tovey H, de Oliveira FM, Carreira S, Swales K, Ruddle R, Raynaud FI, Purchase B, Dawes JC, Parmar M, Turner AJ, Tunariu N, Banerjee S, de Bono JS, Banerji U.

Ann Oncol. 2018 Sep 1;29(9):1918-1925. doi: 10.1093/annonc/mdy245.

7.

Erratum to: investigation of metabolites for estimating blood deposition time.

Lech K, Liu F, Davies SK, Ackermann K, Ang JE, Middleton B, Revell VL, Raynaud FI, Hoveijn I, Hut RA, Skene DJ, Kayser M.

Int J Legal Med. 2018 Jan;132(1):33. doi: 10.1007/s00414-017-1670-y. No abstract available.

PMID:
28840223
8.

Development and validation of a LC-MS/MS method for the quantification of the checkpoint kinase 1 inhibitor SRA737 in human plasma.

Zangarini M, Berry P, Sludden J, Raynaud FI, Banerji U, Jones P, Edwards D, Veal GJ.

Bioanalysis. 2017 Jul;9(13):1001-1010. doi: 10.4155/bio-2017-0043. Epub 2017 Jul 10.

PMID:
28692309
9.

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.

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.

Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution.

Hayes A, Mok NY, Liu M, Thai C, Henley AT, Atrash B, Lanigan RM, Sejberg J, Le Bihan YV, Bavetsias V, Blagg J, Raynaud FI.

Xenobiotica. 2017 Sep;47(9):771-777. doi: 10.1080/00498254.2016.1230245. Epub 2016 Oct 26.

12.

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.

13.

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.

14.

p53 Loss in MYC-Driven Neuroblastoma Leads to Metabolic Adaptations Supporting Radioresistance.

Yogev O, Barker K, Sikka A, Almeida GS, Hallsworth A, Smith LM, Jamin Y, Ruddle R, Koers A, Webber HT, Raynaud FI, Popov S, Jones C, Petrie K, Robinson SP, Keun HC, Chesler L.

Cancer Res. 2016 May 15;76(10):3025-35. doi: 10.1158/0008-5472.CAN-15-1939. Epub 2016 Mar 29.

15.

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.

16.

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.

17.

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.

18.

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.

19.

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
20.

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.

21.

8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.

Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J.

J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7.

22.

7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent.

Bavetsias V, Pérez-Fuertes Y, McIntyre PJ, Atrash B, Kosmopoulou M, O'Fee L, Burke R, Sun C, Faisal A, Bush K, Avery S, Henley A, Raynaud FI, Linardopoulos S, Bayliss R, Blagg J.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4203-9. doi: 10.1016/j.bmcl.2015.08.003. Epub 2015 Aug 6.

23.

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.

24.

Combined MYC and P53 defects emerge at medulloblastoma relapse and define rapidly progressive, therapeutically targetable disease.

Hill RM, Kuijper S, Lindsey JC, Petrie K, Schwalbe EC, Barker K, Boult JK, Williamson D, Ahmad Z, Hallsworth A, Ryan SL, Poon E, Robinson SP, Ruddle R, Raynaud FI, Howell L, Kwok C, Joshi A, Nicholson SL, Crosier S, Ellison DW, Wharton SB, Robson K, Michalski A, Hargrave D, Jacques TS, Pizer B, Bailey S, Swartling FJ, Weiss WA, Chesler L, Clifford SC.

Cancer Cell. 2015 Jan 12;27(1):72-84. doi: 10.1016/j.ccell.2014.11.002. Epub 2014 Dec 18.

25.

First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors.

Sarker D, Ang JE, Baird R, Kristeleit R, Shah K, Moreno V, Clarke PA, Raynaud FI, Levy G, Ware JA, Mazina K, Lin R, Wu J, Fredrickson J, Spoerke JM, Lackner MR, Yan Y, Friedman LS, Kaye SB, Derynck MK, Workman P, de Bono JS.

Clin Cancer Res. 2015 Jan 1;21(1):77-86. doi: 10.1158/1078-0432.CCR-14-0947. Epub 2014 Nov 4.

26.

Effect of sleep deprivation on the human metabolome.

Davies SK, Ang JE, Revell VL, Holmes B, Mann A, Robertson FP, Cui N, Middleton B, Ackermann K, Kayser M, Thumser AE, Raynaud FI, Skene DJ.

Proc Natl Acad Sci U S A. 2014 Jul 22;111(29):10761-6. doi: 10.1073/pnas.1402663111. Epub 2014 Jul 7.

27.

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.

28.

Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells.

Bavetsias V, Faisal A, Crumpler S, Brown N, Kosmopoulou M, Joshi A, Atrash B, Pérez-Fuertes Y, Schmitt JA, Boxall KJ, Burke R, Sun C, Avery S, Bush K, Henley A, Raynaud FI, Workman P, Bayliss R, Linardopoulos S, Blagg J.

J Med Chem. 2013 Nov 27;56(22):9122-35. doi: 10.1021/jm401115g. Epub 2013 Nov 6.

29.

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design.

Couty S, Westwood IM, Kalusa A, Cano C, Travers J, Boxall K, Chow CL, Burns S, Schmitt J, Pickard L, Barillari C, McAndrew PC, Clarke PA, Linardopoulos S, Griffin RJ, Aherne GW, Raynaud FI, Workman P, Jones K, van Montfort RL.

Oncotarget. 2013 Oct;4(10):1647-61.

30.

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.

31.

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.

32.

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.

33.

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.

34.

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.

35.

Dependence of Wilms tumor cells on signaling through insulin-like growth factor 1 in an orthotopic xenograft model targetable by specific receptor inhibition.

Bielen A, Box G, Perryman L, Bjerke L, Popov S, Jamin Y, Jury A, Valenti M, Brandon Ade H, Martins V, Romanet V, Jeay S, Raynaud FI, Hofmann F, Robinson SP, Eccles SA, Jones C.

Proc Natl Acad Sci U S A. 2012 May 15;109(20):E1267-76. doi: 10.1073/pnas.1105034109. Epub 2012 Apr 23.

36.

Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns.

Moore AS, Faisal A, Gonzalez de Castro D, Bavetsias V, Sun C, Atrash B, Valenti M, de Haven Brandon A, Avery S, Mair D, Mirabella F, Swansbury J, Pearson AD, Workman P, Blagg J, Raynaud FI, Eccles SA, Linardopoulos S.

Leukemia. 2012 Jul;26(7):1462-70. doi: 10.1038/leu.2012.52. Epub 2012 Feb 22.

37.

Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.

Reader JC, Matthews TP, Klair S, Cheung KM, Scanlon J, Proisy N, Addison G, Ellard J, Piton N, Taylor S, Cherry M, Fisher M, Boxall K, Burns S, Walton MI, Westwood IM, Hayes A, Eve P, Valenti M, de Haven Brandon A, Box G, van Montfort RL, Williams DH, Aherne GW, Raynaud FI, Eccles SA, Garrett MD, Collins I.

J Med Chem. 2011 Dec 22;54(24):8328-42. doi: 10.1021/jm2007326. Epub 2011 Nov 23.

38.

Discovering and developing PI3 kinase inhibitors for cancer: rapid progress through academic-biotech-pharma interactions.

Raynaud FI, Workman P.

Mol Cancer Ther. 2011 Nov;10(11):2017-8. doi: 10.1158/1535-7163.MCT-11-0739. No abstract available.

39.

Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.

Wilson SC, Atrash B, Barlow C, Eccles S, Fischer PM, Hayes A, Kelland L, Jackson W, Jarman M, Mirza A, Moreno J, Nutley BP, Raynaud FI, Sheldrake P, Walton M, Westwood R, Whittaker S, Workman P, McDonald E.

Bioorg Med Chem. 2011 Nov 15;19(22):6949-65. doi: 10.1016/j.bmc.2011.08.051. Epub 2011 Aug 31.

PMID:
21982796
40.

Targeting the Hsp90 molecular chaperone with novel macrolactams. Synthesis, structural, binding, and cellular studies.

Day JE, Sharp SY, Rowlands MG, Aherne W, Hayes A, Raynaud FI, Lewis W, Roe SM, Prodromou C, Pearl LH, Workman P, Moody CJ.

ACS Chem Biol. 2011 Dec 16;6(12):1339-47. doi: 10.1021/cb200196e. Epub 2011 Oct 4.

PMID:
21932796
41.

The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo.

Faisal A, Vaughan L, Bavetsias V, Sun C, Atrash B, Avery S, Jamin Y, Robinson SP, Workman P, Blagg J, Raynaud FI, Eccles SA, Chesler L, Linardopoulos S.

Mol Cancer Ther. 2011 Nov;10(11):2115-23. doi: 10.1158/1535-7163.MCT-11-0333. Epub 2011 Sep 1.

42.

Enhanced efficacy of IGF1R inhibition in pediatric glioblastoma by combinatorial targeting of PDGFRα/β.

Bielen A, Perryman L, Box GM, Valenti M, de Haven Brandon A, Martins V, Jury A, Popov S, Gowan S, Jeay S, Raynaud FI, Hofmann F, Hargrave D, Eccles SA, Jones C.

Mol Cancer Ther. 2011 Aug;10(8):1407-18. doi: 10.1158/1535-7163.MCT-11-0205. Epub 2011 Jun 9.

43.

Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors.

Shuttleworth SJ, Silva FA, Cecil AR, Tomassi CD, Hill TJ, Raynaud FI, Clarke PA, Workman P.

Curr Med Chem. 2011;18(18):2686-714. Review.

44.

Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.

Large JM, Torr JE, Raynaud FI, Clarke PA, Hayes A, Stefano Fd, Urban F, Shuttleworth SJ, Saghir N, Sheldrake P, Workman P, McDonald E.

Bioorg Med Chem. 2011 Jan 15;19(2):836-51. doi: 10.1016/j.bmc.2010.12.006. Epub 2010 Dec 9.

PMID:
21216151
45.

Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.

Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD.

Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29.

46.

Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.

Caldwell JJ, Welsh EJ, Matijssen C, Anderson VE, Antoni L, Boxall K, Urban F, Hayes A, Raynaud FI, Rigoreau LJ, Raynham T, Aherne GW, Pearl LH, Oliver AW, Garrett MD, Collins I.

J Med Chem. 2011 Jan 27;54(2):580-90. doi: 10.1021/jm101150b. Epub 2010 Dec 27.

PMID:
21186793
47.

Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.

Donald AD, Clark VL, Patel S, Day FA, Rowlands MG, Wibata J, Stimson L, Hardcastle A, Eccles SA, McNamara D, Needham LA, Raynaud FI, Aherne W, Moffat DF.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6657-60. doi: 10.1016/j.bmcl.2010.09.016. Epub 2010 Sep 21.

PMID:
20884208
48.

Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.

Bavetsias V, Large JM, Sun C, Bouloc N, Kosmopoulou M, Matteucci M, Wilsher NE, Martins V, Reynisson J, Atrash B, Faisal A, Urban F, Valenti M, de Haven Brandon A, Box G, Raynaud FI, Workman P, Eccles SA, Bayliss R, Blagg J, Linardopoulos S, McDonald E.

J Med Chem. 2010 Jul 22;53(14):5213-28. doi: 10.1021/jm100262j.

PMID:
20565112
49.

The phosphoinositide 3-kinase inhibitor PI-103 downregulates choline kinase alpha leading to phosphocholine and total choline decrease detected by magnetic resonance spectroscopy.

Al-Saffar NM, Jackson LE, Raynaud FI, Clarke PA, Ramírez de Molina A, Lacal JC, Workman P, Leach MO.

Cancer Res. 2010 Jul 1;70(13):5507-17. doi: 10.1158/0008-5472.CAN-09-4476. Epub 2010 Jun 15.

50.

Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.

Suijkerbuijk BM, Niculescu-Duvaz I, Gaulon C, Dijkstra HP, Niculescu-Duvaz D, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie LM, Hedley D, Lopes F, Preece NP, Moreno-Farre J, Raynaud FI, Kirk R, Whittaker S, Marais R, Springer CJ.

J Med Chem. 2010 Apr 8;53(7):2741-56. doi: 10.1021/jm900607f.

PMID:
20199087

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