Published in Bioorg Med Chem Lett on November 22, 2009
Synthesis and in vitro evaluation of N-alkyl-3-hydroxy-3-(2-imino-3-methyl-5-oxoimidazolidin-4-yl)indolin-2-one analogs as potential anticancer agents. Bioorg Med Chem Lett (2010) 1.05
Antiangiogenic properties of substituted (Z)-(±)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ol/one analogs and their derivatives. Bioorg Med Chem Lett (2010) 0.89
The novel chemical entity YTR107 inhibits recruitment of nucleophosmin to sites of DNA damage, suppressing repair of DNA double-strand breaks and enhancing radiosensitization. Clin Cancer Res (2011) 0.88
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Novel substituted (Z)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-one and (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ol derivatives as potent thermal sensitizing agents. Bioorg Med Chem Lett (2007) 3.14
NADPH oxidase activity is essential for Keap1/Nrf2-mediated induction of GCLC in response to 2-indol-3-yl-methylenequinuclidin-3-ols. Cancer Res (2003) 3.02
Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1). Bioorg Med Chem Lett (2009) 2.77
Inhibition of TGF-beta with neutralizing antibodies prevents radiation-induced acceleration of metastatic cancer progression. J Clin Invest (2007) 2.52
A novel mechanism of action and potential use for lobeline as a treatment for psychostimulant abuse. Biochem Pharmacol (2002) 2.51
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Identification of sensor cysteines in human Keap1 modified by the cancer chemopreventive agent sulforaphane. Chem Res Toxicol (2005) 2.22
Inhibition of mammalian target of rapamycin or apoptotic pathway induces autophagy and radiosensitizes PTEN null prostate cancer cells. Cancer Res (2006) 2.21
An orally bioavailable parthenolide analog selectively eradicates acute myelogenous leukemia stem and progenitor cells. Blood (2007) 2.14
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Increased expression of nuclear factor E2 p45-related factor 2 (NRF2) in head and neck squamous cell carcinomas. Head Neck (2006) 1.52
Lobelane inhibits methamphetamine-evoked dopamine release via inhibition of the vesicular monoamine transporter-2. J Pharmacol Exp Ther (2009) 1.49
Covalent modification at Cys151 dissociates the electrophile sensor Keap1 from the ubiquitin ligase CUL3. Chem Res Toxicol (2008) 1.47
N,N'-Alkane-diyl-bis-3-picoliniums as nicotinic receptor antagonists: inhibition of nicotine-evoked dopamine release and hyperactivity. J Pharmacol Exp Ther (2008) 1.44
Inflammatory chemokine receptors regulate CD8(+) T cell contraction and memory generation following infection. J Exp Med (2011) 1.40
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Lobelane analogues as novel ligands for the vesicular monoamine transporter-2. Bioorg Med Chem (2005) 1.38
Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents. Bioorg Med Chem Lett (2004) 1.36
The effects of a novel nicotinic receptor antagonist N,N-dodecane-1,12-diyl-bis-3-picolinium dibromide (bPiDDB) on acute and repeated nicotine-induced increases in extracellular dopamine in rat nucleus accumbens. Neuropharmacology (2006) 1.32
Novel chemical enhancers of heat shock increase thermal radiosensitization through a mitotic catastrophe pathway. Cancer Res (2007) 1.32
Molecular mechanism of human Nrf2 activation and degradation: role of sequential phosphorylation by protein kinase CK2. Free Radic Biol Med (2007) 1.31
Pyrrolidine analogues of lobelane: relationship of affinity for the dihydrotetrabenazine binding site with function of the vesicular monoamine transporter 2 (VMAT2). J Med Chem (2009) 1.30
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Smad3-ATF3 signaling mediates TGF-beta suppression of genes encoding Phase II detoxifying proteins. Free Radic Biol Med (2005) 1.25
Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras. Neuropharmacology (2008) 1.25
Targeting aberrant glutathione metabolism to eradicate human acute myelogenous leukemia cells. J Biol Chem (2013) 1.25
(Z)-3-(Benzo[b]thiophen-2-yl)-2-(3,4,5-trimethoxyphenyl)acrylonitrile and (E)-3-(benzo[b]thiophen-2-yl)-2-(3,4-dimethoxyphenyl)acrylonitrile. [corrected]. Acta Crystallogr C (2007) 1.23
Early CD4(+) T cell help prevents partial CD8(+) T cell exhaustion and promotes maintenance of Herpes Simplex Virus 1 latency. J Immunol (2009) 1.20
A NADPH oxidase-dependent redox signaling pathway mediates the selective radiosensitization effect of parthenolide in prostate cancer cells. Cancer Res (2010) 1.18
The pharmacological activity of nicotine and nornicotine on nAChRs subtypes: relevance to nicotine dependence and drug discovery. J Neurochem (2007) 1.18
Cysteine-based regulation of the CUL3 adaptor protein Keap1. Toxicol Appl Pharmacol (2009) 1.17
Molecular pathway for thymoquinone-induced cell-cycle arrest and apoptosis in neoplastic keratinocytes. Anticancer Drugs (2004) 1.17
bis-Azaaromatic quaternary ammonium analogues: ligands for alpha4beta2* and alpha7* subtypes of neuronal nicotinic receptors. Bioorg Med Chem Lett (2002) 1.17
Synthesis and evaluation of a series of benzothiophene acrylonitrile analogs as anticancer agents. Medchemcomm (2013) 1.17
Antileukemic activity of aminoparthenolide analogs. Bioorg Med Chem Lett (2008) 1.14
N-n-alkylnicotinium analogs, a novel class of nicotinic receptor antagonists: interaction with alpha4beta2* and alpha7* neuronal nicotinic receptors. J Pharmacol Exp Ther (2003) 1.13
(Z)-2-(1-Phenylsulfonyl-1H-indol-3-ylmethylene)-1-azabicyclo[2.2.2]octan-3-one and (Z)-(S)-2-(1-phenylsulfonyl-1H-indol-3-ylmethylene)-1-azabicyclo[2.2.2]octan-3-ol. Acta Crystallogr C (2004) 1.13
N-n-alkylpyridinium analogs, a novel class of nicotinic receptor antagonists: selective inhibition of nicotine-evoked [3H] dopamine overflow from superfused rat striatal slices. J Pharmacol Exp Ther (2003) 1.12
Immune control of HSV-1 latency. Viral Immunol (2005) 1.12
Synthesis and evaluation of a series of homologues of lobelane at the vesicular monoamine transporter-2. Bioorg Med Chem Lett (2008) 1.11
(Z)-3-(1H-Indol-3-yl)-2-(3-thienyl)acrylonitrile and (Z)-3-[1-(4-tert-butylbenzyl)-1H-indol-3-yl]-2-(3-thienyl)acrylonitrile. Acta Crystallogr C (2005) 1.11
Binding of tritiated sildenafil, tadalafil, or vardenafil to the phosphodiesterase-5 catalytic site displays potency, specificity, heterogeneity, and cGMP stimulation. Mol Pharmacol (2004) 1.11
(Z)-2-[(1-Phenylsulfonyl-1H-indol-3-yl)methylene]-1-azabicyclo[2.2.2]octan-3-one semicarbazone. Acta Crystallogr C (2007) 1.10
Novel N-1,2-dihydroxypropyl analogs of lobelane inhibit vesicular monoamine transporter-2 function and methamphetamine-evoked dopamine release. J Pharmacol Exp Ther (2011) 1.10
Nicotinic receptor-based therapeutics and candidates for smoking cessation. Biochem Pharmacol (2009) 1.09
A pilot study of plasma caffeine concentrations in a US sample of smoker and nonsmoker volunteers. Prog Neuropsychopharmacol Biol Psychiatry (2003) 1.09
Transdermal delivery of naltrexol and skin permeability lifetime after microneedle treatment in hairless guinea pigs. J Pharm Sci (2010) 1.09
The effect of a novel VMAT2 inhibitor, GZ-793A, on methamphetamine reward in rats. Psychopharmacology (Berl) (2011) 1.08
NRF2 deficiency reduces life span of mice administered thoracic irradiation. Free Radic Biol Med (2011) 1.07
Pharmacokinetics of the novel nicotinic receptor antagonist N,N'-dodecane-1,12-diyl-bis-3-picolinium dibromide in the rat. Drug Metab Dispos (2008) 1.07
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands. Bioorg Med Chem Lett (2005) 1.06
rac-2-(2-Amino-4-oxo-4,5-dihydro-1,3-thia-zol-5-yl)-2-hydroxy-indane-1,3-dione. Acta Crystallogr Sect E Struct Rep Online (2009) 1.06
Carrier-mediated transport of the quaternary ammonium neuronal nicotinic receptor antagonist n,n'-dodecylbispicolinium dibromide at the blood-brain barrier. J Pharmacol Exp Ther (2007) 1.06
N-n-alkylnicotinium analogs, a novel class of nicotinic receptor antagonist: inhibition of S(-)-nicotine-evoked [(3)H]dopamine overflow from superfused rat striatal slices. J Pharmacol Exp Ther (2002) 1.05
Modeling multiple species of nicotine and deschloroepibatidine interacting with alpha4beta2 nicotinic acetylcholine receptor: from microscopic binding to phenomenological binding affinity. J Am Chem Soc (2005) 1.05
Microwave assisted synthesis and in vitro cytotoxicities of substituted (Z)-2-amino-5-(1-benzyl-1H-indol-3-yl)methylene-1-methyl-1H-imidazol-4(5H)-ones against human tumor cell lines. Bioorg Med Chem Lett (2009) 1.05
Synthesis and in vitro evaluation of N-alkyl-3-hydroxy-3-(2-imino-3-methyl-5-oxoimidazolidin-4-yl)indolin-2-one analogs as potential anticancer agents. Bioorg Med Chem Lett (2010) 1.05
(Z)-4-[3-(2,5-Dioxoimidazolidin-4-ylidenemeth-yl)-1H-indol-1-ylmeth-yl]benzonitrile. Acta Crystallogr Sect E Struct Rep Online (2008) 1.04
3-(2-Amino-1-methyl-4-oxo-4,5-dihydro-1H-imidazol-5-yl)-5-fluoro-3-hydr-oxy-1-methyl-indolin-2-one methanol hemisolvate. Acta Crystallogr Sect E Struct Rep Online (2009) 1.04
Transdermal delivery of naltrexone and its active metabolite 6-beta-naltrexol in human skin in vitro and guinea pigs in vivo. J Pharm Sci (2005) 1.03
The radiosensitization effect of parthenolide in prostate cancer cells is mediated by nuclear factor-kappaB inhibition and enhanced by the presence of PTEN. Mol Cancer Ther (2007) 1.03
Enhancement of transdermal delivery of 6-beta-naltrexol via a codrug linked to hydroxybupropion. J Control Release (2006) 1.03
Active transport of high-affinity choline and nicotine analogs into the central nervous system by the blood-brain barrier choline transporter. J Pharmacol Exp Ther (2003) 1.02
Effects of norketamine enantiomers in rodent models of persistent pain. Pharmacol Biochem Behav (2008) 1.02
Redox-sensitive interaction between KIAA0132 and Nrf2 mediates indomethacin-induced expression of gamma-glutamylcysteine synthetase. Free Radic Biol Med (2002) 1.02
Selenium deficiency activates mouse liver Nrf2-ARE but vitamin E deficiency does not. Free Radic Biol Med (2008) 1.01
Activating transcription factor 3 is a novel repressor of the nuclear factor erythroid-derived 2-related factor 2 (Nrf2)-regulated stress pathway. Cancer Res (2008) 1.01
Flux across [corrected] microneedle-treated skin is increased by increasing charge of naltrexone and naltrexol in vitro. Pharm Res (2008) 1.01
Tris-azaaromatic quaternary ammonium salts: Novel templates as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release. Bioorg Med Chem Lett (2007) 1.00
In vitro permeation of a pegylated naltrexone prodrug across microneedle-treated skin. J Control Release (2010) 1.00
Mecamylamine, dihydro-beta-erythroidine, and dextromethorphan block conditioned responding evoked by the conditional stimulus effects of nicotine. Pharmacol Biochem Behav (2009) 1.00
Inhibition of signal transducer and activator of transcription 3 activity results in down-regulation of Survivin following irradiation. Mol Cancer Ther (2006) 1.00
The novel pyrrolidine nor-lobelane analog UKCP-110 [cis-2,5-di-(2-phenethyl)-pyrrolidine hydrochloride] inhibits VMAT2 function, methamphetamine-evoked dopamine release, and methamphetamine self-administration in rats. J Pharmacol Exp Ther (2010) 1.00
Targeting reward-relevant nicotinic receptors in the discovery of novel pharmacotherapeutic agents to treat tobacco dependence. Nebr Symp Motiv (2009) 1.00
Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain. Bioorg Med Chem Lett (2011) 0.99
(Z)-2-(1H-Indol-3-ylmethylene)-1-azabicyclo[2.2.2]octan-3-one. Acta Crystallogr C (2003) 0.99
Synthesis and antitubercular activity of a series of hydrazone and nitrovinyl analogs derived from heterocyclic aldehydes. J Enzyme Inhib Med Chem (2009) 0.99
NADPH oxidase and Nrf2 regulate gastric aspiration-induced inflammation and acute lung injury. J Immunol (2013) 0.98
Human skin permeation of branched-chain 3-0-alkyl ester and carbonate prodrugs of naltrexone. Pharm Res (2005) 0.98
In vivo evaluation of 3-O-alkyl ester transdermal prodrugs of naltrexone in hairless guinea pigs. J Control Release (2005) 0.98