F. Friedlos

发表

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

Richard D. Taylor, Esteban Roman, Steven Whittaker, 2009, Journal of medicinal chemistry.

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

F. Friedlos, M. Pera, J. Mills, 1987, Cancer research.

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

S. Whittaker, C. Springer, R. Marais, 2008, Journal of medicinal chemistry.

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

P. Workman, C. Springer, R. Marais, 2005, Cancer research.

Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds

David M. Wilson, S. Whittaker, Arnaud Nourry, 2010, Bioorganic & medicinal chemistry.

Mechanism of cytotoxicity of anticancer platinum drugs: evidence that cis-diamminedichloroplatinum(II) and cis-diammine-(1,1-cyclobutanedicarboxylato)platinum(II) differ only in the kinetics of their interaction with DNA.

D. Lydall, F. Friedlos, J. Roberts, 1986, Cancer research.

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

C. Springer, R. Marais, I. Niculescu-Duvaz, 2002, Cancer research.

Gene-directed enzyme prodrug therapy: quantitative bystander cytotoxicity and DNA damage induced by CB1954 in cells expressing bacterial nitroreductase

C. Springer, F. Friedlos, S. Court, 1998, Gene Therapy.

B-RAF is a therapeutic target in melanoma

C. Marshall, C. Springer, R. Marais, 2004, Oncogene.

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

F. Friedlos, R. Knox, M. Boland, 1993, Cancer and Metastasis Reviews.

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

C. Springer, R. Marais, Ping Chen, 2007, Cancer research.

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

C. Springer, R. Marais, F. Friedlos, 2005, Cancer research.

Methods to improve efficacy in suicide gene therapy approaches: targeting prodrug-activating enzymes carboxypeptidase G2 and nitroreductase to different subcellular compartments.

R. Marais, F. Friedlos, R. Spooner, 2004, Methods in molecular medicine.

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

F. Friedlos, R. Sherwood, G. Anlezark, 1992, Biochemical pharmacology.

The bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB1954)--I. Purification and properties of a nitroreductase enzyme from Escherichia coli--a potential enzyme for antibody-directed enzyme prodrug therapy (ADEPT).

F. Friedlos, R. Sherwood, G. Anlezark, 1992, Biochemical pharmacology.

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

C. Springer, R. Marais, F. Friedlos, 2001, International journal of cancer.

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

D. Kerr, I. McNeish, C. Springer, 1998, Advances in experimental medicine and biology.

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

W. Denny, W. Wilson, B. Palmer, 1995, Biochemical pharmacology.

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

L. Davies, F. Friedlos, R. Sherwood, 1995, Biochemical pharmacology.

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

P. Biggs, L. Davies, F. Friedlos, 1993, Biochemical pharmacology.

CB 1954 (2,4-dinitro-5-aziridinyl benzamide) becomes a DNA interstrand crosslinking agent in Walker tumour cells.

F. Friedlos, J. Roberts, R. Knox, 1986, Biochemical and biophysical research communications.

Bioactivation of CB 1954: reaction of the active 4-hydroxylamino derivative with thioesters to form the ultimate DNA-DNA interstrand crosslinking species.

F. Friedlos, J. Roberts, R. Knox, 1991, Biochemical pharmacology.

Identification of novel reduced pyridinium derivatives as synthetic co-factors for the enzyme DT diaphorase (NAD(P)H dehydrogenase (quinone), EC 1.6.99.2).

L. Davies, F. Friedlos, M. Jarman, 1992, Biochemical pharmacology.

The properties of total adducts and interstrand crosslinks in the DNA of cells treated with CB 1954. Exceptional frequency and stability of the crosslink.

F. Friedlos, J. Roberts, J. Quinn, 1992, Biochemical pharmacology.

Caffeine, aminoimidazolecarboxamide and dicoumarol, inhibitors of NAD(P)H dehydrogenase (quinone) (DT diaphorase), prevent both the cytotoxicity and DNA interstrand crosslinking produced by 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) in Walker cells.

F. Friedlos, J. Roberts, R. Knox, 1989, Biochemical pharmacology.

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

L. Mancini, M. Leach, C. Springer, 2009, NMR in biomedicine.

In suicide gene therapy, the site of subcellular localization of the activating enzyme is more important than the rate at which it activates prodrug

C. Springer, R. Marais, F. Friedlos, 2000, Cancer Gene Therapy.

Quantitative estimation of cisplatin-induced DNA interstrand cross-links and their repair in mammalian cells: relationship to toxicity.

F. Friedlos, J. Roberts, John J. Roberts, 1987, Pharmacology & therapeutics.

Inhibition by caffeine of post-replication repair in Chinese hamster cells treated with 7-bromomethylbenz(a)anthracene: enhancement of toxicity, chromosome damage and inhibition of ligation of newly-synthesized DNA.

F. Friedlos, J. Roberts, H. W. van den Berg, 1977, Chemico-biological interactions.

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

C. Springer, I. Niculescu-Duvaz, D. Niculescu-Duvaz, 1999, Anti-cancer drug design.

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

C. Springer, L. Davies, F. Friedlos, 2005, Journal of medicinal chemistry.

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

C. Springer, R. Marais, L. Davies, 2000, Human gene therapy.

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.

D. Kerr, J. Neoptolemos, C. Springer, 1997, Cancer gene therapy.

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

P. Workman, F. Friedlos, S. Chen, 1995, Molecular pharmacology.

Self-immolative anthracycline prodrugs for suicide gene therapy.

C. Springer, R. Marais, I. Niculescu-Duvaz, 1999, Journal of medicinal chemistry.

The Role of Platinum-DNA Interactions in the Cellular Toxicity and Anti-Tumour Effects of Platinum Co-Ordination Compounds

J. J. Roberts, D. Lydall, F. Friedlos, 1988 .

Metabolism of NAD(P)H by blood components. Relevance to bioreductively activated prodrugs in a targeted enzyme therapy system.

F. Friedlos, R. Knox, 1992, Biochemical pharmacology.

A new cytotoxic, DNA interstrand crosslinking agent, 5-(aziridin-1-yl)-4-hydroxylamino-2-nitrobenzamide, is formed from 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) by a nitroreductase enzyme in Walker carcinoma cells.

F. Friedlos, J. Roberts, M. Jarman, 1988, Biochemical pharmacology.

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

W. Denny, B. Palmer, C. Springer, 1997, Journal of medicinal chemistry.

The nitroreductase enzyme in Walker cells that activates 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954) to 5-(aziridin-1-yl)-4-hydroxylamino-2-nitrobenzamide is a form of NAD(P)H dehydrogenase (quinone) (EC 1.6.99.2).

J. J. Roberts, C. Southan, F. Friedlos, 1988, Biochemical pharmacology.

Self-immolative nitrogen mustard prodrugs for suicide gene therapy.

C. Springer, R. Marais, I. Niculescu-Duvaz, 1998, Journal of medicinal chemistry.

The frequency of interstrand cross-links in DNA following reaction of cis-diamminedichloroplatinum(II) with cells in culture or DNA in vitro: stability of DNA cross-links and their repair.

F. Friedlos, J. Roberts, 1982, Chemico-biological interactions.

Quantitative aspects of the formation and loss of DNA interstrand crosslinks in Chinese hamster cells following treatment with cis-diamminedichloroplatinum(II) (cisplatin). I. Proportion of DNA-platinum reactions involved in DNA crosslinking.

F. Friedlos, J. Roberts, 1981, Biochimica et biophysica acta.

Differential toxicity of cis- and trans-diamminedichloroplatinum(II) toward mammalian cells: lack of influence of any difference in the rates of loss of their DNA-bound adducts.

F. Friedlos, J. Roberts, 1987, Cancer research.

The effect of monofunctional or difunctional platinum adducts and of various other associated DNA damage on the expression of transfected DNA in mammalian cell lines sensitive or resistant to difunctional agents.

D. Lydall, F. Friedlos, J. Roberts, 1987, Biochimica et biophysica acta.

The unique sensitivity of Walker rat tumour cells to difunctional agents is associated with a failure to recover from inhibition of DNA synthesis and increased chromosome damage.

C. Rawlings, D. Scott, F. Friedlos, 1986, Mutation research.

DNA Repair Characteristics of Walker Rat Carcinoma Cells Sensitive and Resistant to Cis-Diamminedichloroplatinum(II) (Cisplatin) and Difunctional Alkylating Agents

J. J. Roberts, C. Rawlings, F. Friedlos, 1984 .

DNA TEMPLATE BREAKAGE AND DECREASED EXCISION OF HYDROCARBON DERIVED ADDUCTS FROM CHINESE HAMSTER CELL DNA FOLLOWING CAFFEINE-INDUCED INHIBITION OF POST REPLICATION REPAIR

J. J. Roberts, F. Friedlos, E. Belka, 1978 .

Caffeine-inhibited DNA repair in 7-bromomethylbenz (a)-anthracene-treated Chinease hamster cells: formation of breaks in parental DNA and inhibition of ligation of nascent DNA as a mechanism for enhancement of lethality and chromosome damage.

F. Friedlos, J. Roberts, 1978, Mutation research.

Attenuated Salmonella Targets Prodrug Activating Enzyme Carboxypeptidase G2 to Mouse Melanoma and Human Breast and Colon Carcinomas for Effective Suicide Gene Therapy

Panos Lehouritis, Lawrence Davies, Richard Marais, 2008, Clinical Cancer Research.

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

C. Rawlings, D. Lydall, F. Friedlos, 1991, Mutation research.

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

J. Brueggen, J. Wood, C. Springer, 2003, British Journal of Cancer.

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

Richard D. Taylor, H. Dijkstra, S. Whittaker, 2009, Journal of medicinal chemistry.

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

F. Friedlos, A. Mauger, P. Burke, 1994, Journal of medicinal chemistry.

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

P. Biggs, F. Friedlos, R. Knox, 1992, Biochemical pharmacology.

Caffeine inhibits excision of 7-bromomethylbenz (a) anthracene-DNA adducts from exponentially growing but not from stationary phase Chinese hamster cells.

F. Friedlos, J. Roberts, 1978, Nucleic Acids Research.

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

P. Workman, J. Hartley, F. Friedlos, 1997, British Journal of Cancer.

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

H. Dijkstra, S. Whittaker, Arnaud Nourry, 2010, Journal of medicinal chemistry.

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

S. Whittaker, C. Springer, R. Marais, 2006, Journal of medicinal chemistry.

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.

H. Dijkstra, S. Whittaker, Arnaud Nourry, 2010, Journal of medicinal chemistry.

Significant differences in biological parameters between prodrugs cleavable by carboxypeptidase G2 that generate 3,5-difluoro-phenol and -aniline nitrogen mustards in gene-directed enzyme prodrug therapy systems.

C. Springer, R. Marais, I. Niculescu-Duvaz, 2004, Journal of medicinal chemistry.

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

C. Springer, R. Marais, I. Niculescu-Duvaz, 2003, Journal of medicinal chemistry.

Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds

David M. Wilson, S. Whittaker, Arnaud Nourry, 2010, Bioorganic & Medicinal Chemistry.