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Items: 40

1.

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.

2.

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]

3.

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.

Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, Fedorov O, Raynaud F, Donovan A, Blagg J, Bavetsias V, Oppermann U, Bountra C, Kawamura A, Brennan PE.

Angew Chem Int Ed Engl. 2019 Jan 8;58(2):515-519. doi: 10.1002/anie.201810179. Epub 2018 Dec 7.

4.

Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition.

Fearon D, Westwood IM, van Montfort RLM, Bayliss R, Jones K, Bavetsias V.

Bioorg Med Chem. 2018 Jul 15;26(11):3021-3029. doi: 10.1016/j.bmc.2018.04.033. Epub 2018 Apr 17.

5.

Assessing histone demethylase inhibitors in cells: lessons learned.

Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S.

Epigenetics Chromatin. 2017 Mar 1;10:9. doi: 10.1186/s13072-017-0116-6. eCollection 2017.

6.

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.

7.

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.

8.

Aurora Kinase Inhibitors: Current Status and Outlook.

Bavetsias V, Linardopoulos S.

Front Oncol. 2015 Dec 21;5:278. doi: 10.3389/fonc.2015.00278. eCollection 2015. Review.

9.

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.

10.

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.

11.

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.

12.

Regioselective C2-arylation of imidazo[4,5-b]pyridines.

Macdonald J, Oldfield V, Bavetsias V, Blagg J.

Org Biomol Chem. 2013 Apr 14;11(14):2335-47. doi: 10.1039/c3ob27477b.

PMID:
23429655
13.

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.

14.

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.

15.

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.

16.

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

Bouloc N, Large JM, Kosmopoulou M, Sun C, Faisal A, Matteucci M, Reynisson J, Brown N, Atrash B, Blagg J, McDonald E, Linardopoulos S, Bayliss R, Bavetsias V.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):5988-93. doi: 10.1016/j.bmcl.2010.08.091. Epub 2010 Aug 21.

PMID:
20833547
17.

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
18.

Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design.

Dodson CA, Kosmopoulou M, Richards MW, Atrash B, Bavetsias V, Blagg J, Bayliss R.

Biochem J. 2010 Mar 15;427(1):19-28. doi: 10.1042/BJ20091530. Erratum in: Biochem J. 2010;427(3):551.

PMID:
20067443
19.

Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).

Gorsuch S, Bavetsias V, Rowlands MG, Aherne GW, Workman P, Jarman M, McDonald E.

Bioorg Med Chem. 2009 Jan 15;17(2):467-74. doi: 10.1016/j.bmc.2008.11.079. Epub 2008 Dec 7.

PMID:
19101154
20.

ClTi(OiPr)3-promoted reductive amination on the solid phase: combinatorial synthesis of a biaryl-based sulfonamide library.

Gutierrez CD, Bavetsias V, McDonald E.

J Comb Chem. 2008 Mar-Apr;10(2):280-4. doi: 10.1021/cc700132f. Epub 2008 Jan 12.

PMID:
18189368
21.

Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity.

Chan F, Sun C, Perumal M, Nguyen QD, Bavetsias V, McDonald E, Martins V, Wilsher NE, Raynaud FI, Valenti M, Eccles S, Te Poele R, Workman P, Aboagye EO, Linardopoulos S.

Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3147-57.

22.

Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.

Bavetsias V, Sun C, Bouloc N, Reynisson J, Workman P, Linardopoulos S, McDonald E.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6567-71. Epub 2007 Oct 22.

PMID:
17933533
23.

Targeting the alpha-folate receptor with cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase.

Henderson EA, Bavetsias V, Theti DS, Wilson SC, Clauss R, Jackman AL.

Bioorg Med Chem. 2006 Jul 15;14(14):5020-42. Epub 2006 Mar 22.

PMID:
16554160
24.

BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors.

Gibbs DD, Theti DS, Wood N, Green M, Raynaud F, Valenti M, Forster MD, Mitchell F, Bavetsias V, Henderson E, Jackman AL.

Cancer Res. 2005 Dec 15;65(24):11721-8.

25.

Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.

Collins I, Caldwell J, Fonseca T, Donald A, Bavetsias V, Hunter LJ, Garrett MD, Rowlands MG, Aherne GW, Davies TG, Berdini V, Woodhead SJ, Davis D, Seavers LC, Wyatt PG, Workman P, McDonald E.

Bioorg Med Chem. 2006 Feb 15;14(4):1255-73. Epub 2005 Oct 24.

PMID:
16249095
26.

Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity.

Stimson L, Rowlands MG, Newbatt YM, Smith NF, Raynaud FI, Rogers P, Bavetsias V, Gorsuch S, Jarman M, Bannister A, Kouzarides T, McDonald E, Workman P, Aherne GW.

Mol Cancer Ther. 2005 Oct;4(10):1521-32.

27.

Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation.

Sorrentino R, Libertini S, Pallante PL, Troncone G, Palombini L, Bavetsias V, Spalletti-Cernia D, Laccetti P, Linardopoulos S, Chieffi P, Fusco A, Portella G.

J Clin Endocrinol Metab. 2005 Feb;90(2):928-35. Epub 2004 Nov 23.

PMID:
15562011
29.
30.

The design and synthesis of water-soluble analogues of CB30865, a quinazolin-4-one-based antitumor agent.

Bavetsias V, Skelton LA, Yafai F, Mitchell F, Wilson SC, Allan B, Jackman AL.

J Med Chem. 2002 Aug 15;45(17):3692-702.

PMID:
12166942
31.

Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS).

Bavetsias V, Marriott JH, Theti DS, Melin JC, Wilson SC, Jackman AL.

Bioorg Med Chem Lett. 2001 Dec 3;11(23):3015-7.

PMID:
11714600
32.

Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).

Bavetsias V, Marriott JH, Melin C, Kimbell R, Matusiak ZS, Boyle FT, Jackman AL.

J Med Chem. 2000 May 18;43(10):1910-26.

PMID:
10821704
33.

Nonpolyglutamatable antifolates as inhibitors of thymidylate synthase (TS) and potential antitumour agents.

Bavetsias V, Jackman AL.

Curr Med Chem. 1998 Aug;5(4):265-88. Review.

PMID:
9668195
34.
35.

Prodrugs of thymidylate synthase inhibitors: potential for antibody directed enzyme prodrug therapy (ADEPT).

Springer CJ, Bavetsias V, Jackman AL, Boyle FT, Marshall D, Pedley RB, Bisset GM.

Anticancer Drug Des. 1996 Dec;11(8):625-36.

PMID:
9022750
36.
37.

Quinazoline-based thymidylate synthase inhibitors: relationship between structural modifications and polyglutamation.

Jackman AL, Kimbell R, Brown M, Brunton L, Bisset GM, Bavetsias V, Marsham P, Hughes LR, Boyle FT.

Anticancer Drug Des. 1995 Oct;10(7):573-89.

PMID:
7495480
38.

The synthesis and thymidylate synthase inhibitory activity of L-gamma-L-linked dipeptide and L-gamma-amide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).

Bisset GM, Bavetsias V, Thornton TJ, Pawelczak K, Calvert AH, Hughes LR, Jackman AL.

J Med Chem. 1994 Sep 30;37(20):3294-302.

PMID:
7932557
39.

Quinazoline antifolates inhibiting thymidylate synthase: synthesis of gamma-linked peptide and amide analogues of 2-desamino-2-methyl-N10-propargyl- 5,8-dideazafolic acid (ICI 198583).

Bavetsias V, Jackman AL, Thornton TJ, Pawelczak K, Boyle FT, Bisset GM.

Adv Exp Med Biol. 1993;338:593-6. No abstract available.

PMID:
8304188
40.

Gamma-linked dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8- dideazafolate as antitumour agents.

Jackman AL, Bisset GM, Jodrell DI, Gibson W, Kimbell R, Bavetsias V, Calvert AH, Harrap KR, Stephens TC, Smith MN, et al.

Adv Exp Med Biol. 1993;338:579-84.

PMID:
8304184

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