Published in J Med Chem on June 03, 2004
Trypanocidal activity of aziridinyl nitrobenzamide prodrugs. Antimicrob Agents Chemother (2010) 1.11
Evaluating aziridinyl nitrobenzamide compounds as leishmanicidal prodrugs. Antimicrob Agents Chemother (2013) 0.77
Exploiting tumour hypoxia in cancer treatment. Nat Rev Cancer (2004) 7.91
Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality. Sci Transl Med (2011) 2.97
A molecule targeting VHL-deficient renal cell carcinoma that induces autophagy. Cancer Cell (2008) 2.38
The 2-nitroimidazole EF5 is a biomarker for oxidoreductases that activate the bioreductive prodrug CEN-209 under hypoxia. Clin Cancer Res (2011) 2.38
Role of marine biology in glacial-interglacial CO2 cycles. Science (2005) 2.11
Use of three-dimensional tissue cultures to model extravascular transport and predict in vivo activity of hypoxia-targeted anticancer drugs. J Natl Cancer Inst (2006) 1.79
Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J (2007) 1.74
Gemcitabine sensitization by checkpoint kinase 1 inhibition correlates with inhibition of a Rad51 DNA damage response in pancreatic cancer cells. Mol Cancer Ther (2009) 1.66
Vaccine-induced myeloid cell population dampens protective immunity to SIV. J Clin Invest (2014) 1.64
Mechanism of action and preclinical antitumor activity of the novel hypoxia-activated DNA cross-linking agent PR-104. Clin Cancer Res (2007) 1.60
Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302. Mol Cancer Ther (2011) 1.58
A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J (2011) 1.57
A mitochondria-targeted macrocyclic Mn(II) superoxide dismutase mimetic. Chem Biol (2012) 1.55
Covariant glacial-interglacial dust fluxes in the equatorial Pacific and Antarctica. Science (2008) 1.53
Thalidomide metabolites in mice and patients with multiple myeloma. Clin Cancer Res (2003) 1.43
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution. J Med Chem (2006) 1.39
Iron fertilization of the Subantarctic ocean during the last ice age. Science (2014) 1.36
A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res (2009) 1.26
Influence of substituent modifications on DNA binding energetics of acridine-based anticancer agents. Biochemistry (2003) 1.24
Pronounced hypoxia in models of murine and human leukemia: high efficacy of hypoxia-activated prodrug PR-104. PLoS One (2011) 1.23
Crystal structure of 9-amino-N-[2-(4-morpholinyl)ethyl]-4-acridinecarboxamide bound to d(CGTACG)2: implications for structure-activity relationships of acridinecarboxamide topoisomerase poisons. Nucleic Acids Res (2002) 1.23
The bioreductive prodrug PR-104A is activated under aerobic conditions by human aldo-keto reductase 1C3. Cancer Res (2010) 1.23
Cell type-specific, topoisomerase II-dependent inhibition of hypoxia-inducible factor-1alpha protein accumulation by NSC 644221. Clin Cancer Res (2007) 1.17
Increased productivity in the subantarctic ocean during Heinrich events. Nature (2005) 1.16
Genotoxicity of non-covalent interactions: DNA intercalators. Mutat Res (2007) 1.16
Synthesis and evaluation of nitroheterocyclic carbamate prodrugs for use with nitroreductase-mediated gene-directed enzyme prodrug therapy. J Med Chem (2003) 1.10
Multicellular resistance to tirapazamine is due to restricted extravascular transport: a pharmacokinetic/pharmacodynamic study in HT29 multicellular layer cultures. Cancer Res (2003) 1.08
Increases in c-Yes expression level and activity promote motility but not proliferation of human colorectal carcinoma cells. Neoplasia (2007) 1.07
Intermediates in the reduction of the antituberculosis drug PA-824, (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine, in aqueous solution. Org Biomol Chem (2008) 1.06
Studies on the nitroreductase prodrug-activating system. Crystal structures of complexes with the inhibitor dicoumarol and dinitrobenzamide prodrugs and of the enzyme active form. J Med Chem (2003) 1.05
Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). J Med Chem (2011) 1.05
Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). J Med Chem (2010) 1.04
IL-1 enhances expansion, effector function, tissue localization, and memory response of antigen-specific CD8 T cells. J Exp Med (2013) 1.03
A phase I trial of PR-104, a nitrogen mustard prodrug activated by both hypoxia and aldo-keto reductase 1C3, in patients with solid tumors. Cancer Chemother Pharmacol (2009) 1.03
Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis. Bioorg Med Chem (2008) 1.02
Activation of 3-amino-1,2,4-benzotriazine 1,4-dioxide antitumor agents to oxidizing species following their one-electron reduction. J Am Chem Soc (2003) 1.02
A roadmap for drug discovery and its translation to small molecule agents in clinical development for tuberculosis treatment. Tuberculosis (Edinb) (2008) 1.02
Diflavin oxidoreductases activate the bioreductive prodrug PR-104A under hypoxia. Mol Pharmacol (2011) 1.02
Identification of human reductases that activate the dinitrobenzamide mustard prodrug PR-104A: a role for NADPH:cytochrome P450 oxidoreductase under hypoxia. Biochem Pharmacol (2007) 1.01
Substituted 9-aminoacridine-4-carboxamides tethered to platinum(II)diamine complexes: chemistry, cytotoxicity and DNA sequence selectivity. J Inorg Biochem (2010) 1.01
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors. J Med Chem (2006) 1.00
Marked potentiation of the antitumour activity of chemotherapeutic drugs by the antivascular agent 5,6-dimethylxanthenone-4-acetic acid (DMXAA). Cancer Chemother Pharmacol (2002) 0.99
DNA cross-links in human tumor cells exposed to the prodrug PR-104A: relationships to hypoxia, bioreductive metabolism, and cytotoxicity. Cancer Res (2009) 0.99
Non-covalent ligand/DNA interactions: minor groove binding agents. Mutat Res (2007) 0.98
Beta-testing of PI3-kinase inhibitors: is beta better? Cancer Discov (2012) 0.97
Structure-activity relationships for pyrido-, imidazo-, pyrazolo-, pyrazino-, and pyrrolophenazinecarboxamides as topoisomerase-targeted anticancer agents. J Med Chem (2002) 0.97
Pharmacokinetic/pharmacodynamic modeling identifies SN30000 and SN29751 as tirapazamine analogues with improved tissue penetration and hypoxic cell killing in tumors. Clin Cancer Res (2010) 0.96
Homologous recombination is the principal pathway for the repair of DNA damage induced by tirapazamine in mammalian cells. Cancer Res (2008) 0.96
18F-EF5 PET imaging as an early response biomarker for the hypoxia-activated prodrug SN30000 combined with radiation treatment in a non-small cell lung cancer xenograft model. J Nucl Med (2013) 0.95
Reactivity of ubiquinone and ubiquinol with superoxide and the hydroperoxyl radical: implications for in vivo antioxidant activity. Free Radic Biol Med (2008) 0.95
Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1. Bioorg Med Chem Lett (2005) 0.95
A combined pharmacokinetic model for the hypoxia-targeted prodrug PR-104A in humans, dogs, rats and mice predicts species differences in clearance and toxicity. Cancer Chemother Pharmacol (2010) 0.94
4-Pyridylanilinothiazoles that selectively target von Hippel-Lindau deficient renal cell carcinoma cells by inducing autophagic cell death. J Med Chem (2010) 0.94
Oxygen dependence and extravascular transport of hypoxia-activated prodrugs: comparison of the dinitrobenzamide mustard PR-104A and tirapazamine. Int J Radiat Oncol Biol Phys (2007) 0.93
Epigenetic regulation of gene expression as an anticancer drug target. Curr Cancer Drug Targets (2011) 0.93
Spin trapping of radicals other than the *OH radical upon reduction of the anticancer agent tirapazamine by cytochrome P450 reductase. J Am Chem Soc (2009) 0.93
Design, synthesis, and in vitro evaluation of dipeptide-based antibody minor groove binder conjugates. J Med Chem (2005) 0.93
Hypoxia-selective 3-alkyl 1,2,4-benzotriazine 1,4-dioxides: the influence of hydrogen bond donors on extravascular transport and antitumor activity. J Med Chem (2007) 0.92
Quantitation of bystander effects in nitroreductase suicide gene therapy using three-dimensional cell cultures. Cancer Res (2002) 0.92
Metabolism of thalidomide in liver microsomes of mice, rabbits, and humans. J Pharmacol Exp Ther (2004) 0.92
Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3. Eur J Med Chem (2013) 0.92
Reactions of superoxide with myeloperoxidase. Biochemistry (2007) 0.90
Mycobacterium bovis BCG vaccination induces memory CD4+ T cells characterized by effector biomarker expression and anti-mycobacterial activity. Vaccine (2007) 0.90
Amsacrine as a topoisomerase II poison: importance of drug-DNA interactions. Biochemistry (2012) 0.90
A phase I trial of PR-104, a pre-prodrug of the bioreductive prodrug PR-104A, given weekly to solid tumour patients. BMC Cancer (2011) 0.90
Roles of DNA repair and reductase activity in the cytotoxicity of the hypoxia-activated dinitrobenzamide mustard PR-104A. Mol Cancer Ther (2009) 0.90
Inhibition of the pore-forming protein perforin by a series of aryl-substituted isobenzofuran-1(3H)-ones. Bioorg Med Chem (2011) 0.90
Exploration of a series of 5-arylidene-2-thioxoimidazolidin-4-ones as inhibitors of the cytolytic protein perforin. J Med Chem (2013) 0.90