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Items: 1 to 50 of 59

1.

Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.

Niculescu-Duvaz D, Niculescu-Duvaz I, Suijkerbuijk BM, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie L, Hedley D, Takle AK, Wilson DM, Pons JF, Coulter T, Kirk R, Cantarino N, Whittaker S, Marais R, Springer CJ.

Bioorg Med Chem. 2010 Sep 15;18(18):6934-52. doi: 10.1016/j.bmc.2010.06.031. Epub 2010 Jun 15.

2.

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
3.

BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.

Nourry A, Zambon A, Davies L, Niculescu-Duvaz I, Dijkstra HP, Ménard D, Gaulon C, Niculescu-Duvaz D, Suijkerbuijk BM, Friedlos F, Manne HA, Kirk R, Whittaker S, Marais R, Springer CJ.

J Med Chem. 2010 Mar 11;53(5):1964-78. doi: 10.1021/jm901509a.

PMID:
20148563
4.

Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.

Ménard D, Niculescu-Duvaz I, Dijkstra HP, Niculescu-Duvaz D, Suijkerbuijk BM, Zambon A, Nourry A, Roman E, Davies L, Manne HA, Friedlos F, Kirk R, Whittaker S, Gill A, Taylor RD, Marais R, Springer CJ.

J Med Chem. 2009 Jul 9;52(13):3881-91. doi: 10.1021/jm900242c.

PMID:
19473026
5.

Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).

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

J Med Chem. 2009 Apr 23;52(8):2255-64. doi: 10.1021/jm801509w. Erratum in: J Med Chem. 2009 Sep 24;52(18):5770.

PMID:
19323560
6.

A novel technique to monitor carboxypeptidase G2 expression in suicide gene therapy using 19F magnetic resonance spectroscopy.

Mancini L, Davies L, Friedlos F, Falck-Miniotis M, Dzik-Jurasz AS, Springer CJ, Leach MO, Payne GS.

NMR Biomed. 2009 Jun;22(5):561-6. doi: 10.1002/nbm.1375.

PMID:
19259950
7.

Attenuated Salmonella targets prodrug activating enzyme carboxypeptidase G2 to mouse melanoma and human breast and colon carcinomas for effective suicide gene therapy.

Friedlos F, Lehouritis P, Ogilvie L, Hedley D, Davies L, Bermudes D, King I, Martin J, Marais R, Springer CJ.

Clin Cancer Res. 2008 Jul 1;14(13):4259-66. doi: 10.1158/1078-0432.CCR-07-4800.

8.

Novel inhibitors of the v-raf murine sarcoma viral oncogene homologue B1 (BRAF) based on a 2,6-disubstituted pyrazine scaffold.

Niculescu-Duvaz I, Roman E, Whittaker SR, Friedlos F, Kirk R, Scanlon IJ, Davies LC, Niculescu-Duvaz D, Marais R, Springer CJ.

J Med Chem. 2008 Jun 12;51(11):3261-74. doi: 10.1021/jm070776b. Epub 2008 May 13.

PMID:
18473434
9.

Suicide gene therapy of human colon carcinoma xenografts using an armed oncolytic adenovirus expressing carboxypeptidase G2.

Schepelmann S, Ogilvie LM, Hedley D, Friedlos F, Martin J, Scanlon I, Chen P, Marais R, Springer CJ.

Cancer Res. 2007 May 15;67(10):4949-55.

10.

Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.

Niculescu-Duvaz I, Roman E, Whittaker SR, Friedlos F, Kirk R, Scanlon IJ, Davies LC, Niculescu-Duvaz D, Marais R, Springer CJ.

J Med Chem. 2006 Jan 12;49(1):407-16.

PMID:
16392826
11.

Activated B-RAF is an Hsp90 client protein that is targeted by the anticancer drug 17-allylamino-17-demethoxygeldanamycin.

da Rocha Dias S, Friedlos F, Light Y, Springer C, Workman P, Marais R.

Cancer Res. 2005 Dec 1;65(23):10686-91.

12.

Novel fluorinated prodrugs for activation by carboxypeptidase G2 showing good in vivo antitumor activity in gene-directed enzyme prodrug therapy.

Davies LC, Friedlos F, Hedley D, Martin J, Ogilvie LM, Scanlon IJ, Springer CJ.

J Med Chem. 2005 Aug 11;48(16):5321-8.

PMID:
16078849
13.

Systemic gene-directed enzyme prodrug therapy of hepatocellular carcinoma using a targeted adenovirus armed with carboxypeptidase G2.

Schepelmann S, Hallenbeck P, Ogilvie LM, Hedley D, Friedlos F, Martin J, Scanlon I, Hay C, Hawkins LK, Marais R, Springer CJ.

Cancer Res. 2005 Jun 15;65(12):5003-8.

14.

B-RAF is a therapeutic target in melanoma.

Karasarides M, Chiloeches A, Hayward R, Niculescu-Duvaz D, Scanlon I, Friedlos F, Ogilvie L, Hedley D, Martin J, Marshall CJ, Springer CJ, Marais R.

Oncogene. 2004 Aug 19;23(37):6292-8.

PMID:
15208680
15.
16.
17.

A novel vascular endothelial growth factor-directed therapy that selectively activates cytotoxic prodrugs.

Spooner RA, Friedlos F, Maycroft K, Stribbling SM, Roussel J, Brueggen J, Stolz B, O'Reilly T, Wood J, Matter A, Marais R, Springer CJ.

Br J Cancer. 2003 May 19;88(10):1622-30.

18.

Self-immolative nitrogen mustards prodrugs cleavable by carboxypeptidase G2 (CPG2) showing large cytotoxicity differentials in GDEPT.

Niculescu-Duvaz D, Niculescu-Duvaz I, Friedlos F, Martin J, Lehouritis P, Marais R, Springer CJ.

J Med Chem. 2003 Apr 24;46(9):1690-705.

PMID:
12699387
19.

Three new prodrugs for suicide gene therapy using carboxypeptidase G2 elicit bystander efficacy in two xenograft models.

Friedlos F, Davies L, Scanlon I, Ogilvie LM, Martin J, Stribbling SM, Spooner RA, Niculescu-Duvaz I, Marais R, Springer CJ.

Cancer Res. 2002 Mar 15;62(6):1724-9.

20.

Appropriate subcellular localisation of prodrug-activating enzymes has important consequences for suicide gene therapy.

Spooner RA, Maycroft KA, Paterson H, Friedlos F, Springer CJ, Marais R.

Int J Cancer. 2001 Jul 1;93(1):123-30.

21.
22.

Prodrugs for antibody- and gene-directed enzyme prodrug therapies (ADEPT and GDEPT).

Niculescu-Duvaz I, Friedlos F, Niculescu-Duvaz D, Davies L, Springer CJ.

Anticancer Drug Des. 1999 Dec;14(6):517-38. Review.

PMID:
10834273
23.

Regressions of established breast carcinoma xenografts by carboxypeptidase G2 suicide gene therapy and the prodrug CMDA are due to a bystander effect.

Stribbling SM, Friedlos F, Martin J, Davies L, Spooner RA, Marais R, Springer CJ.

Hum Gene Ther. 2000 Jan 20;11(2):285-92.

PMID:
10680842
24.

Self-immolative anthracycline prodrugs for suicide gene therapy.

Niculescu-Duvaz I, Niculescu-Duvaz D, Friedlos F, Spooner R, Martin J, Marais R, Springer CJ.

J Med Chem. 1999 Jul 1;42(13):2485-9.

PMID:
10395490
25.

Sensitisation of human ovarian cancer cells to killing by the prodrug CB1954 following retroviral or adenoviral transfer of the E. coli nitroreductase gene.

Searle PF, Weedon SJ, McNeish IA, Gilligan MG, Ford MJ, Friedlos F, Springer CJ, Young LS, Kerr DJ.

Adv Exp Med Biol. 1998;451:107-13. No abstract available.

PMID:
10026858
26.

Self-immolative nitrogen mustard prodrugs for suicide gene therapy.

Niculescu-Duvaz D, Niculescu-Duvaz I, Friedlos F, Martin J, Spooner R, Davies L, Marais R, Springer CJ.

J Med Chem. 1998 Dec 17;41(26):5297-309.

PMID:
9857097
28.

Sensitization of colorectal and pancreatic cancer cell lines to the prodrug 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB1954) by retroviral transduction and expression of the E. coli nitroreductase gene.

Green NK, Youngs DJ, Neoptolemos JP, Friedlos F, Knox RJ, Springer CJ, Anlezark GM, Michael NP, Melton RG, Ford MJ, Young LS, Kerr DJ, Searle PF.

Cancer Gene Ther. 1997 Jul-Aug;4(4):229-38.

PMID:
9253508
29.

Mustard prodrugs for activation by Escherichia coli nitroreductase in gene-directed enzyme prodrug therapy.

Friedlos F, Denny WA, Palmer BD, Springer CJ.

J Med Chem. 1997 Apr 11;40(8):1270-5.

PMID:
9111301
30.

Involvement of DT-diaphorase (EC 1.6.99.2) in the DNA cross-linking and sequence selectivity of the bioreductive anti-tumour agent EO9.

Bailey SM, Wyatt MD, Friedlos F, Hartley JA, Knox RJ, Lewis AD, Workman P.

Br J Cancer. 1997;76(12):1596-603.

31.

Bioactivation of dinitrobenzamide mustards by an E. coli B nitroreductase.

Anlezark GM, Melton RG, Sherwood RF, Wilson WR, Denny WA, Palmer BD, Knox RJ, Friedlos F, Williams A.

Biochem Pharmacol. 1995 Aug 25;50(5):609-18.

PMID:
7669063
32.

Virtual cofactors for an Escherichia coli nitroreductase enzyme: relevance to reductively activated prodrugs in antibody directed enzyme prodrug therapy (ADEPT).

Knox RJ, Friedlos F, Jarman M, Davies LC, Goddard P, Anlezark GM, Melton RG, Sherwood RF.

Biochem Pharmacol. 1995 May 26;49(11):1641-7.

PMID:
7786305
33.

Catalytic properties of NAD(P)H:quinone acceptor oxidoreductase: study involving mouse, rat, human, and mouse-rat chimeric enzymes.

Chen S, Knox R, Lewis AD, Friedlos F, Workman P, Deng PS, Fung M, Ebenstein D, Wu K, Tsai TM.

Mol Pharmacol. 1995 May;47(5):934-9.

PMID:
7746280
34.

Self-immolative prodrugs: candidates for antibody-directed enzyme prodrug therapy in conjunction with a nitroreductase enzyme.

Mauger AB, Burke PJ, Somani HH, Friedlos F, Knox RJ.

J Med Chem. 1994 Oct 14;37(21):3452-8.

PMID:
7932574
35.

Identification, synthesis and properties of 5-(aziridin-1-yl)-2-nitro-4-nitrosobenzamide, a novel DNA crosslinking agent derived from CB1954.

Knox RJ, Friedlos F, Biggs PJ, Flitter WD, Gaskell M, Goddard P, Davies L, Jarman M.

Biochem Pharmacol. 1993 Sep 1;46(5):797-803.

PMID:
8373433
36.

The bioactivation of CB 1954 and its use as a prodrug in antibody-directed enzyme prodrug therapy (ADEPT).

Knox RJ, Friedlos F, Boland MP.

Cancer Metastasis Rev. 1993 Jun;12(2):195-212. Review.

PMID:
8375021
37.

The bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB1954)--II. A comparison of an Escherichia coli nitroreductase and Walker DT diaphorase.

Knox RJ, Friedlos F, Sherwood RF, Melton RG, Anlezark GM.

Biochem Pharmacol. 1992 Dec 15;44(12):2297-301.

PMID:
1472095
39.

Potentiation of CB 1954 cytotoxicity by reduced pyridine nucleotides in human tumour cells by stimulation of DT diaphorase activity.

Friedlos F, Biggs PJ, Abrahamson JA, Knox RJ.

Biochem Pharmacol. 1992 Nov 3;44(9):1739-43.

PMID:
1449531
40.
41.
42.
43.

The Walker 256 carcinoma: a cell type inherently sensitive only to those difunctional agents that can form DNA interstrand crosslinks.

Knox RJ, Lydall DA, Friedlos F, Basham C, Rawlings CJ, Roberts JJ.

Mutat Res. 1991 Nov;255(3):227-40.

PMID:
1719394
44.
48.

Inherent sensitivity of cultured human embryonal carcinoma cells to adducts of cis-diamminedichloroplatinum(II) on DNA.

Pera MF, Friedlos F, Mills J, Roberts JJ.

Cancer Res. 1987 Dec 15;47(24 Pt 1):6810-3.

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