Published in Biochemistry on November 25, 2003
10-(4-Chloro-phen-yl)-9-(4-fluoro-phen-yl)-3,3,6,6-tetra-methyl-3,4,6,7,9,10-hexa-hydro-acridine-1,8(2H,5H)-dione. Acta Crystallogr Sect E Struct Rep Online (2008) 1.56
Modification at the C9 position of the marine natural product isoaaptamine and the impact on HIV-1, mycobacterial, and tumor cell activity. Bioorg Med Chem (2006) 0.93
Antiviral and anticancer optimization studies of the DNA-binding marine natural product aaptamine. Chem Biol Drug Des (2008) 0.84
DNA studies of newly synthesized heteroleptic platinum(II) complexes [Pt(bpy)(iip)](2+) and [Pt(bpy)(miip)](2.). J Biol Inorg Chem (2015) 0.78
Intracellular trafficking as a determinant of AS-DACA cytotoxicity in rhabdomyosarcoma cells. BMC Cell Biol (2011) 0.76
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
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
Mechanism of action and preclinical antitumor activity of the novel hypoxia-activated DNA cross-linking agent PR-104. Clin Cancer Res (2007) 1.60
A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J (2011) 1.57
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
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
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
Cell type-specific, topoisomerase II-dependent inhibition of hypoxia-inducible factor-1alpha protein accumulation by NSC 644221. Clin Cancer Res (2007) 1.17
Genotoxicity of non-covalent interactions: DNA intercalators. Mutat Res (2007) 1.16
Extending nature's leads: the anticancer agent ellipticine. Curr Med Chem Anticancer Agents (2004) 1.11
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
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
Synthesis of the ABC ring system of azaspiracid. 1. Effect of D ring truncation on bis-spirocyclization. Org Lett (2002) 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
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 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
Interactions between the etoposide derivative F14512 and human type II topoisomerases: implications for the C4 spermine moiety in promoting enzyme-mediated DNA cleavage. Biochemistry (2011) 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 of the ABC ring system of Azaspiracid. 2. A systematic study into the effect of C(16) and C(17) substitution on bis-spirocyclization. Org Lett (2002) 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
Drug interactions with Bacillus anthracis topoisomerase IV: biochemical basis for quinolone action and resistance. Biochemistry (2011) 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
Substituents on etoposide that interact with human topoisomerase IIalpha in the binary enzyme-drug complex: contributions to etoposide binding and activity. Biochemistry (2008) 0.99
Non-covalent ligand/DNA interactions: minor groove binding agents. Mutat Res (2007) 0.98
Short DNA sequences and bacterial DNA induce esophageal, gastric, and colorectal cancer cell invasion. APMIS (2012) 0.98
Topoisomerase II - drug interaction domains: identification of substituents on etoposide that interact with the enzyme. Biochemistry (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
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
4-Pyridylanilinothiazoles that selectively target von Hippel-Lindau deficient renal cell carcinoma cells by inducing autophagic cell death. J Med Chem (2010) 0.94
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
Epigenetic regulation of gene expression as an anticancer drug target. Curr Cancer Drug Targets (2011) 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
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
Quantitation of bystander effects in nitroreductase suicide gene therapy using three-dimensional cell cultures. Cancer Res (2002) 0.92
Amsacrine as a topoisomerase II poison: importance of drug-DNA interactions. Biochemistry (2012) 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
Inhibition of the pore-forming protein perforin by a series of aryl-substituted isobenzofuran-1(3H)-ones. Bioorg Med Chem (2011) 0.90
Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. J Med Chem (2010) 0.89
Transcription factors as targets for DNA-interacting drugs. Curr Med Chem (2003) 0.89
Validation of inhibitors of an ABC transporter required to transport lipopolysaccharide to the cell surface in Escherichia coli. Bioorg Med Chem (2013) 0.88
DNA and the chromosome - varied targets for chemotherapy. Cell Chromosome (2004) 0.88
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors. Bioorg Med Chem (2007) 0.87
3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. J Med Chem (2012) 0.87
Creation and screening of a multi-family bacterial oxidoreductase library to discover novel nitroreductases that efficiently activate the bioreductive prodrugs CB1954 and PR-104A. Biochem Pharmacol (2013) 0.87
Structure-activity relationships of 1,2,4-benzotriazine 1,4-dioxides as hypoxia-selective analogues of tirapazamine. J Med Chem (2003) 0.87
Antimalarial 9-anilinoacridine compounds directed at hematin. Antimicrob Agents Chemother (2003) 0.87
Pharmacokinetic/pharmacodynamic model-guided identification of hypoxia-selective 1,2,4-benzotriazine 1,4-dioxides with antitumor activity: the role of extravascular transport. J Med Chem (2007) 0.87
Selective treatment of hypoxic tumor cells in vivo: phosphate pre-prodrugs of nitro analogues of the duocarmycins. Angew Chem Int Ed Engl (2011) 0.87
Radical properties governing the hypoxia-selective cytotoxicity of antitumor 3-amino-1,2,4-benzotriazine 1,4-dioxides. Org Biomol Chem (2005) 0.86
4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase. J Med Chem (2007) 0.86
Oxidation of 2-deoxyribose by benzotriazinyl radicals of antitumor 3-amino-1,2,4-benzotriazine 1,4-dioxides. J Am Chem Soc (2004) 0.86
Characterization of radicals formed following enzymatic reduction of 3-substituted analogues of the hypoxia-selective cytotoxin 3-amino-1,2,4-benzotriazine 1,4-dioxide (tirapazamine). J Am Chem Soc (2010) 0.85
Structure of 9-amino-[N-(2-dimethylamino)propyl]acridine-4-carboxamide bound to d(CGTACG)(2): a comparison of structures of d(CGTACG)(2) complexed with intercalatorsin the presence of cobalt. Acta Crystallogr D Biol Crystallogr (2004) 0.85
Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases. Eur J Med Chem (2007) 0.84
α₁-Adrenoceptor and serotonin 5-HT(1A) receptor affinity of homobivalent 4-aminoquinoline compounds: an investigation of the effect of linker length. Biochem Pharmacol (2013) 0.84
Antiviral and anticancer optimization studies of the DNA-binding marine natural product aaptamine. Chem Biol Drug Des (2008) 0.84
Formulation and pharmacokinetics of lipid nanoparticles of a chemically sensitive nitrogen mustard derivative: Chlorambucil. Int J Pharm (2008) 0.84
Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening. Bioorg Med Chem Lett (2009) 0.84
Influence of the amino substituents in the interaction of ethidium bromide with DNA. Biophys J (2004) 0.84
Inhibition of the cellular function of perforin by 1-amino-2,4-dicyanopyrido[1,2-a]benzimidazoles. Bioorg Med Chem (2011) 0.83
Phosphatidylinositol 3-kinase inhibitor (PIK75) containing surface functionalized nanoemulsion for enhanced drug delivery, cytotoxicity and pro-apoptotic activity in ovarian cancer cells. Pharm Res (2012) 0.83
Phosphoinositide-3-kinases (PI3Ks): combined comparative modeling and 3D-QSAR to rationalize the inhibition of p110alpha. J Chem Inf Model (2008) 0.83
Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins. J Med Chem (2008) 0.83
Effects of anticancer drugs on transcription factor-DNA interactions. Expert Opin Ther Targets (2005) 0.82
Structural characterisation of bisintercalation in higher-order DNA at a junction-like quadruplex. J Mol Biol (2002) 0.82
Potentiation of the cytotoxicity of the anticancer agent tirapazamine by benzotriazine N-oxides: the role of redox equilibria. J Am Chem Soc (2006) 0.82
DNA-targeted 1,2,4-benzotriazine 1,4-dioxides: potent analogues of the hypoxia-selective cytotoxin tirapazamine. J Med Chem (2004) 0.82
Structure-activity relationships for analogues of the phenazine-based dual topoisomerase I/II inhibitor XR11576. Bioorg Med Chem Lett (2002) 0.82
Synthesis and in vitro evaluation of analogues of avocado-produced toxin (+)-(R)-persin in human breast cancer cells. Bioorg Med Chem (2011) 0.82
Synthesis and cytotoxic activity of carboxamide derivatives of benzo[b][1,6]naphthyridin-(5H)ones. Bioorg Med Chem (2005) 0.82
Dihydrofuro[3,4-c]pyridinones as inhibitors of the cytolytic effects of the pore-forming glycoprotein perforin. J Med Chem (2008) 0.81
Effect of nitroreduction on the alkylating reactivity and cytotoxicity of the 2,4-dinitrobenzamide-5-aziridine CB 1954 and the corresponding nitrogen mustard SN 23862: distinct mechanisms of bioreductive activation. Chem Res Toxicol (2003) 0.81
Combined neutron and X-ray diffraction studies of DNA in crystals and solutions. Acta Crystallogr D Biol Crystallogr (2010) 0.81
Synthesis and cytotoxic activity of N-[(alkylamino)alkyl]carboxamide derivatives of 7-oxo-7H-benz[de]anthracene, 7-oxo-7H-naphtho[1,2,3-de]quinoline, and 7-oxo-7H-benzo[e]perimidine. Bioorg Med Chem (2005) 0.80
Development of PIK-75 nanosuspension formulation with enhanced delivery efficiency and cytotoxicity for targeted anti-cancer therapy. Int J Pharm (2013) 0.80
Unsymmetrical DNA cross-linking agents: combination of the CBI and PBD pharmacophores. J Med Chem (2003) 0.80
Structure-activity relationships for 4-anilinoquinoline derivatives as inhibitors of the DNA methyltransferase enzyme DNMT1. Bioorg Med Chem (2013) 0.80
Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR. Bioorg Med Chem (2011) 0.80
Effect of wet milling process on the solid state of indomethacin and simvastatin. Int J Pharm (2009) 0.80
Novel angular benzophenazines: dual topoisomerase I and topoisomerase II inhibitors as potential anticancer agents. J Med Chem (2002) 0.80
Interactions of actinomycin D with human telomeric G-quadruplex DNA. Biochemistry (2009) 0.80
In vitro and in vivo characterization of XR11576, a novel, orally active, dual inhibitor of topoisomerase I and II. Anticancer Drugs (2002) 0.80
The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents. Bioorg Med Chem Lett (2007) 0.79
Repurposing the chemical scaffold of the anti-arthritic drug Lobenzarit to target tryptophan biosynthesis in Mycobacterium tuberculosis. Chembiochem (2014) 0.78