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Items: 14

1.

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.

2.

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.

3.

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.

4.

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.

5.

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.

6.

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.

7.

The Bcl-2/Bcl-XL family inhibitor ABT-737 sensitizes ovarian cancer cells to carboplatin.

Witham J, Valenti MR, De-Haven-Brandon AK, Vidot S, Eccles SA, Kaye SB, Richardson A.

Clin Cancer Res. 2007 Dec 1;13(23):7191-8.

8.

Application of meso scale technology for the measurement of phosphoproteins in human tumor xenografts.

Gowan SM, Hardcastle A, Hallsworth AE, Valenti MR, Hunter LJ, de Haven Brandon AK, Garrett MD, Raynaud F, Workman P, Aherne W, Eccles SA.

Assay Drug Dev Technol. 2007 Jun;5(3):391-401.

PMID:
17638539
9.
10.

Novel trans platinum complexes: comparative in vitro and in vivo activity against platinum-sensitive and resistant murine tumours.

Goddard PM, Orr RM, Valenti MR, Barnard CF, Murrer BA, Kelland LR, Harrap KR.

Anticancer Res. 1996 Jan-Feb;16(1):33-8.

PMID:
8615631
11.

Schedule dependency of orally administered bis-acetato-ammine-dichloro-cyclohexylamine-platinum(IV) (JM216) in vivo.

McKeage MJ, Kelland LR, Boxall FE, Valenti MR, Jones M, Goddard PM, Gwynne J, Harrap KR.

Cancer Res. 1994 Aug 1;54(15):4118-22.

12.

Selective potentiation of platinum drug cytotoxicity in cisplatin-sensitive and -resistant human ovarian carcinoma cell lines by amphotericin B.

Sharp SY, Mistry P, Valenti MR, Bryant AP, Kelland LR.

Cancer Chemother Pharmacol. 1994;35(2):137-43.

PMID:
7987990
14.

The 5-HT3 antagonist, BRL 43694, does not compromise the efficacy of cisplatin in tumour-bearing mice.

Goddard PM, Jones M, Pollard LA, Valenti MR, Harrap KR.

Cancer Chemother Pharmacol. 1990;25(5):377-9.

PMID:
2155065

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