当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.

Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.

Abstract：

:Insulin-like growth factor receptor (IGF-1R) is a growth factor receptor tyrosine kinase that acts as a critical mediator of cell proliferation and survival. Inhibitors of this receptor are believed to provide a new target in cancer therapy. We previously reported an isoquinolinedione series of IGF-1R inhibitors. Now we have identified a series of 3-cyanoquinoline compounds that are low nanomolar inhibitors of IGF-1R. The strategies, synthesis, and SAR behind the cyanoquinoline scaffold will be discussed.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Miller LM,Mayer SC,Berger DM,Boschelli DH,Boschelli F,Di L,Du X,Dutia M,Floyd MB,Johnson M,Kenny CH,Krishnamurthy G,Moy F,Petusky S,Tkach D,Torres N,Wu B,Xu W

doi

10.1016/j.bmcl.2008.11.037

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

62-6

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01390-5

journal_volume

19

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Design, synthesis, and evaluation of bisubstrate analog inhibitors of cholera toxin.

    abstract：:Bisubstrate analog inhibitors in which a nicotinamide mimic is attached to a series of structurally diversified guanidines (arginine mimics) were synthesized and evaluated for inhibition of cholera toxin. The mechanism-based bisubstrate inhibitors were up to 1400-fold more potent than the natural substrate NAD+ and 40...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.05.049

    authors： Zhang G

    更新日期：2008-07-01 00:00:00

  • Synthesis and SAR of azalide 3,6-ketal aromatic derivatives as potent Gram-positive and Gram-negative antibacterial agents.

    abstract：:3,6-Ketals of 15-membered azalide pseudoaglycones are a novel series of macrolide antibiotics. The aromatic derivatives of the azalide 3,6-ketals demonstrated potent antibacterial activities against both Gram-positive and Gram-negative bacteria. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00434-1

    authors： Cheng H,Dirlam JP,Ziegler CB,Lundy KM,Hayashi SF,Kamicker BJ,Dutra JK,Daniel KL,Santoro SL,George DM,Bertsche CD,Sakya SM,Suarez-Contreras M

    更新日期：2002-09-02 00:00:00

  • Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.

    abstract：:New N-(1,2-diphenylethyl)piperazines 6 are disclosed as dual serotonin and noradrenaline reuptake inhibitors (SNRI) which may have potential in treating stress urinary incontinence (SUI). In this Letter, we present new data for SNRI PF-526014 (4) including performance in a canine in vivo model of SUI, cardiovascular a...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.04.052

    authors： Fray MJ,Fish PV,Allan GA,Bish G,Clarke N,Eccles R,Harrison AC,Le Net JL,Phillips SC,Regan N,Sobry C,Stobie A,Wakenhut F,Westbrook D,Westbrook SL,Whitlock GA

    更新日期：2010-06-15 00:00:00

  • Using enzymatic amplification by aldolase for the optical detection of DNA by an artificial signal cascade.

    abstract：:A two-step reaction cascade is applied to the sequence-specific detection of single-stranded DNA, including analyte-triggered re-activation of apo-aldolase by its cofactor Zn(2+) and catalytic conversion of a chromophore. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.07.102

    authors： Graf N,Kassube S,Krämer R

    更新日期：2008-09-01 00:00:00

  • Optimization of the enzymatic synthesis of O-glycan core 2 structure by use of a genetic algorithm.

    abstract：:The enzymatic synthesis of Gal-beta 1,3[GlcNAc-beta 1,6]-GalNAc-alpha 1-OBn (core 2-Bn) using a multi-enzyme system consisting of a beta-galactosidase (EC 3.2.1.23) from bovine testes and a recombinant core 2 beta 1,6-GlcNAc transferase (C2GnT, EC 2.4.1.102) was empirically optimized by the use of a genetic algorithm....

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00087-2

    authors： Hoh C,Dudziak G,Liese A

    更新日期：2002-04-08 00:00:00

  • Slow generation of hydrogen sulfide from sulfane sulfurs and NADH models.

    abstract：:Here we report the model studies of the reactions between NADH models (using HEH and BNAH) and sulfane sulfurs (using polysulfides). Such reactions could lead to the oxidation of NADH models and the production of hydrogen sulfide (H2S). Kinetics of the reaction between BNAH and elemental sulfur S8 were determined in e...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.12.023

    authors： Peng B,Liu C,Li Z,Day JJ,Lu Y,Lefer DJ,Xian M

    更新日期：2017-02-01 00:00:00

  • Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.

    abstract：:The synthesis and evaluation of tetrasubstituted aminopyridines, bearing novel azaindazole hinge binders, as potent AKT inhibitors are described. Compound 14c was identified as a potent AKT inhibitor that demonstrated reduced CYP450 inhibition and an improved developability profile compared to those of previously desc...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.11.061

    authors： Lin H,Yamashita DS,Xie R,Zeng J,Wang W,Leber J,Safonov IG,Verma S,Li M,Lafrance L,Venslavsky J,Takata D,Luengo JI,Kahana JA,Zhang S,Robell KA,Levy D,Kumar R,Choudhry AE,Schaber M,Lai Z,Brown BS,Donovan BT,Mi

    更新日期：2010-01-15 00:00:00

  • Synthesis and evaluation of N-alkyl-9-aminoacridines with antibacterial activity.

    abstract：:A series of 9-alkylaminoacridines were synthesized and evaluated for activity against two strains of methicillin-resistant and one strain of methicillin-sensitive Staphylococcus aureus. Results are presented that show a clear structure activity relationship between the N-alkyl chain length and antibacterial activity w...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.05.037

    authors： Benoit AR,Schiaffo C,Salomon CE,Goodell JR,Hiasa H,Ferguson DM

    更新日期：2014-07-15 00:00:00

  • Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE).

    abstract：:Pyridone-based peptidomimetic inhibitors of recombinant human Interleukin-1 beta-converting enzyme (ICE, caspase-1) with an aminomethylene ketone activating group in the P1' position are described. Several analogues with sub-nanomolar Ki's versus ICE and improved aqueous solubility are reported. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(98)00136-x

    authors： Semple G,Ashworth DM,Batt AR,Baxter AJ,Benzies DW,Elliot LH,Evans DM,Franklin RJ,Hudson P,Jenkins PD,Pitt GR,Rooker DP,Yamamoto S,Isomura Y

    更新日期：1998-04-21 00:00:00

  • Generation of novel radiolabeled opiates through site-selective iodination.

    abstract：:Tritiated opioid radioligands have proven valuable in exploring opioid binding sites. However, tritium has many limitations. Its low specific activity and limited counting efficiency makes it difficult to examine low abundant, high affinity sites and its disposal is problematic due to the need to use organic scintilla...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.05.008

    authors： Majumdar S,Burgman M,Haselton N,Grinnell S,Ocampo J,Pasternak AR,Pasternak GW

    更新日期：2011-07-01 00:00:00

  • Design, synthesis, and evaluation of indole compounds as novel inhibitors targeting Gp41.

    abstract：:A series of indole ring containing compounds were designed based on the structure of the gp41 complex in the region of the hydrophobic pocket. These compounds were synthesized using a Suzuki Coupling reaction, and evaluated using a fluorescence binding assay and cell-cell fusion assay. The observed inhibition constant...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.01.111

    authors： Zhou G,Wu D,Hermel E,Balogh E,Gochin M

    更新日期：2010-03-01 00:00:00

  • Synthesis and photophysical properties of new SNARF derivatives as dual emission pH sensors.

    abstract：:We report the synthesis and properties of two new seminaphthorhodafluor (SNARF) derivatives, SNARF-F and SNARF-Cl. Both these derivatives exhibit typical red shifts of absorption and fluorescence, and higher cell permeability as compared to traditional SNARF, while the pH-dependent dual-emission characteristics are we...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.01.105

    authors： Nakata E,Nazumi Y,Yukimachi Y,Uto Y,Maezawa H,Hashimoto T,Okamoto Y,Hori H

    更新日期：2011-03-15 00:00:00

  • Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization.

    abstract：:Starting from our previously identified novel c-Met kinase inhibitors bearing 1H-imidazo[4,5-h][1,6]naphthyridin-2(3H)-one scaffold, a global structural exploration was conducted to furnish an optimal binding motif for further development, directed by the enzyme inhibitory mechanism. First round SAR study picked two i...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.11.070

    authors： An XD,Liu H,Xu ZL,Jin Y,Peng X,Yao YM,Geng M,Long YQ

    更新日期：2015-02-01 00:00:00

  • Anion inhibition studies of a β-carbonic anhydrase from Clostridium perfringens.

    abstract：:A β-carbonic anhydrases (CAs, EC 4.2.1.1) was recently cloned, purified and characterized kinetically in the pathogen Clostridium perfringens. We report here the first inhibition study of this enzyme (CpeCA). CpeCA was poorly inhibited by iodide and bromide, and was inhibited with KIs in the range of 1-10mM by a range...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.10.037

    authors： Vullo D,Sai Kumar RS,Scozzafava A,Capasso C,Ferry JG,Supuran CT

    更新日期：2013-12-15 00:00:00

  • Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.

    abstract：:Identification of a number of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes is described. In the rat microdialysis assay, this series of compounds showed pronounced enhancement of brain acetylcholine release after oral administration. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00457-1

    authors： Wang Y,Chackalamannil S,Hu Z,Clader JW,Greenlee W,Billard W,Binch H,Crosby G,Ruperto V,Duffy RA,McQuade R,Lachowicz JE

    更新日期：2000-10-16 00:00:00

  • Enantioselective synthesis of (R)-(+)- and (S)-(-)-higenamine and their analogues with effects on platelet aggregation and experimental animal model of disseminated intravascular coagulation.

    abstract：:Optically active tetrahydroisoquinoline alkaloids, (R)-(+)-higenamine (1R) and (S)-(-)-higenamine (1 S), and their optically active 1-naphthylmethyl analogues (2 and 3), were synthesized by enantioselective hydrogenation of the corresponding dihydroisoquinoline intermediates 7 as a key step. The evaluation of the plat...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.05.094

    authors： Pyo MK,Lee DH,Kim DH,Lee JH,Moon JC,Chang KC,Yun-Choi HS

    更新日期：2008-07-15 00:00:00

  • Synthesis of 2-methyl-1,4-naphthoquinones with higher gamma-glutamyl carboxylase activity than MK-4 both in vitro and in vivo.

    abstract：:Vitamin K is the collective term for compounds that share a 2-methyl-1,4-naphthoquinone ring, but differ in the side-chain at the 3-position. We synthesized novel 2-methyl-1,4-naphthoquinone derivatives with different side chain length at the 3-position. Derivatives with C-14 and C-16 tails showed the highest in vitro...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.11.073

    authors： Vermeer C,van 't Hoofd C,Knapen MHJ,Xanthoulea S

    更新日期：2017-01-15 00:00:00

  • Novel halogenated nitrobenzylthioinosine analogs as es nucleoside transporter inhibitors.

    abstract：:Nucleoside transporter inhibitors have potential therapeutic applications as anticancer, antiviral, cardioprotective, and neuroprotective agents. We have synthesized and flow cytometrically evaluated the binding affinity of a series of novel halogenated nitrobenzylthioinosine analogs at the human es nucleoside transpo...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.02.016

    authors： Gupte A,Buolamwini JK

    更新日期：2004-05-03 00:00:00

  • Eta4-pyrone iron(0)carbonyl complexes as effective CO-releasing molecules (CO-RMs).

    abstract：:The CO-releasing properties of iron(0)tricarbonyl complexes bearing a 2-pyrone ligand have been evaluated. In this report, we demonstrate that the intrinsic stability of the (eta4-2-pyrone)Fe(CO)3 complex influences the extent and rate of CO release, which is affected by the presence of a halogen substituent on the 2-...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.10.085

    authors： Fairlamb IJ,Duhme-Klair AK,Lynam JM,Moulton BE,O'Brien CT,Sawle P,Hammad J,Motterlini R

    更新日期：2006-02-15 00:00:00

  • Discovery and synthesis of tetrahydropyrimidinedione-4-carboxamides as endothelial lipase inhibitors.

    abstract：:Endothelial lipase (EL) inhibitors have been shown to elevate HDL-C levels in pre-clinical murine models and have potential benefit in prevention and treatment of cardiovascular diseases. Modification of the 1-ethyl-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one (DHP) lead, 1, led to the discovery of a series of potent tetrahy...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.10.022

    authors： Hu CH,Wang TC,Qiao JX,Haque L,Chen AYA,Taylor DS,Ying X,Onorato JM,Galella M,Shen H,Huang CS,Toussaint N,Li YX,Abell L,Adam LP,Gordon D,Wexler RR,Finlay HJ

    更新日期：2018-12-15 00:00:00

  • Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.

    abstract：:A selection of 76 nitroheterocycles and related compounds from our in-house compound library was screened in vitro against the parasite Trypanosoma brucei rhodesiense, causative agent of human African trypanosomiasis (HAT). The unspecific cytotoxicity of the compounds was also evaluated against rat myoblast L6-cells t...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.06.004

    authors： Arán VJ,Kaiser M,Dardonville C

    更新日期：2012-07-15 00:00:00

  • Design, synthesis and anti-TMV activities of novel chromone derivatives containing dithioacetal moiety.

    abstract：:Thirty-five novel chromone derivatives containing dithioacetal moiety were designed, synthesized, and their anti-TMV activities were evaluated through half-leaf method. The results showed compound c23 illustrates highly curative, protective and inactivating activities against TMV at 500 mg/L, with the values of 68.8%,...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.126945

    authors： Li M,Zan N,Huang M,Jiang D,Hu D,Song B

    更新日期：2020-03-01 00:00:00

  • Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.

    abstract：:A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were found to have potent activity in vitro and in vivo. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.06.034

    authors： Xiao HY,Balog A,Attar RM,Fairfax D,Fleming LB,Holst CL,Martin GS,Rossiter LM,Chen J,Cvjic ME,Dell-John J,Geng J,Gottardis MM,Han WC,Nation A,Obermeier M,Rizzo CA,Schweizer L,Spires T Jr,Shan W,Gavai A,Salvati ME

    更新日期：2010-08-01 00:00:00

  • A neural network based prediction of octanol-water partition coefficients using atomic5 fragmental descriptors.

    abstract：:An artificial neural network based approach using Atomic5 fragmental descriptors has been developed to predict the octanol-water partition coefficient (logP). We used a pre-selected set of organic molecules from PHYSPROP database as training and test sets for a feedforward neural network. Results demonstrate the super...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.12.024

    authors： Molnár L,Keseru GM,Papp A,Gulyás Z,Darvas F

    更新日期：2004-02-23 00:00:00

  • Synthesis and cytotoxic activity of a glucuronylated prodrug of nornitrogen mustard.

    abstract：:A new glucuronylated prodrug of nornitrogen mustard, incorporating the same spacer group as the doxorubicin prodrug HMR 1826, has been prepared. Upon exposure to E. coli beta-glucuronidase, fast hydrolysis occurs but a lower cytotoxicity against LoVo cancer cells is observed compared to the nornitrogen mustard alone. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00353-x

    authors： Papot S,Combaud D,Bosslet K,Gerken M,Czech J,Gesson JP

    更新日期：2000-08-21 00:00:00

  • Discovery of a potent and selective series of pyrazole bacterial methionyl-tRNA synthetase inhibitors.

    abstract：:Starting with a micromolar lead identified from high-throughput screening, a series of pyrazoles were discovered with significantly improved potency on bacterial methionyl-tRNA synthetase and selectivity over human methionyl-tRNA synthetase. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(03)00298-1

    authors： Finn J,Mattia K,Morytko M,Ram S,Yang Y,Wu X,Mak E,Gallant P,Keith D

    更新日期：2003-07-07 00:00:00

  • Functional expression and characterization of EryA, the erythritol kinase of Brucella abortus, and enzymatic synthesis of L-erythritol-4-phosphate.

    abstract：:The eryA gene of the bacterial pathogen Brucella abortus has been functionally expressed in Escherichia coli. The resultant EryA was shown to catalyze the ATP-dependent conversion of erythritol to L-erythritol-4-phosphate (L-E4P). The steady state kinetic parameters of this reaction were determined and the enzyme was ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)01032-6

    authors： Lillo AM,Tetzlaff CN,Sangari FJ,Cane DE

    更新日期：2003-02-24 00:00:00

  • Fluorescent diphenylphosphonate-based probes for detection of serine protease activity during inflammation.

    abstract：:Activity-based probes are small molecules that covalently bind to the active site of a protease in an activity-dependent manner. We synthesized and characterized two fluorescent activity-based probes that target serine proteases with trypsin-like or elastase-like activity. We assessed the selectivity and potency of th...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.11.064

    authors： Edgington-Mitchell LE,Barlow N,Aurelio L,Samha A,Szabo M,Graham B,Bunnett N

    更新日期：2017-01-15 00:00:00

  • Novel bis-, tris-, and tetrakis-tertiary amino analogs as antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release.

    abstract：:A series of tertiary amine analogs derived from lead azaaromatic quaternary ammonium salts has been designed and synthesized. The preliminary structure-activity relationships of these new analogs suggest that such tertiary amine analogs, which potently inhibit nicotine-evoked dopamine release from rat striatum, repres...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.11.070

    authors： Zhang Z,Zheng G,Pivavarchyk M,Deaciuc AG,Dwoskin LP,Crooks PA

    更新日期：2011-01-01 00:00:00

  • Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.

    abstract：:Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically crafted to achieve interactions with both the flap and with the S2' p...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.04.050

    authors： Cumming JN,Le TX,Babu S,Carroll C,Chen X,Favreau L,Gaspari P,Guo T,Hobbs DW,Huang Y,Iserloh U,Kennedy ME,Kuvelkar R,Li G,Lowrie J,McHugh NA,Ozgur L,Pan J,Parker EM,Saionz K,Stamford AW,Strickland C,Tadesse D,

    更新日期：2008-06-01 00:00:00