当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors.

Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors.

Abstract：

:The discovery of a novel series of 2-(4-pyridyl)thienopyridinone GSK-3β inhibitors is reported. X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular activity and predicted CNS penetration is also presented.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gentile G,Bernasconi G,Pozzan A,Merlo G,Marzorati P,Bamborough P,Bax B,Bridges A,Brough C,Carter P,Cutler G,Neu M,Takada M

doi

10.1016/j.bmcl.2011.06.050

subject

Has Abstract

pub_date

2011-08-15 00:00:00

pages

4823-7

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00833-X

journal_volume

21

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Synthesis and antiviral activity of novel D- and L-2'-azido-2',3'-dideoxyribofuranosyl-4'-thiopyrimidines and purines.

    abstract：:Novel D- and L-2'-azido-2',3'-dideoxyribofuranosyl-4'-thiopyrimidines and purines have been synthesized starting from L-xylose and D-xylose, respectively. Among synthesized compounds tested against several viruses such as HIV-1, HSV-1, HSV-2, and HCMV, D-beta-N6-methyladenine (ent-22a) and D-alpha-N6-methyladenine (en...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00006-3

    authors： Kim HO,Kim YH,Suh H,Jeong LS

    更新日期：2001-02-26 00:00:00

  • Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity.

    abstract：:A series of pyrrolo[3,2,1-ij]quinoline derivatives was synthesized, evaluated for their activity against the 5-HT2c and 5-HT2a, receptors and found to be agonists at 5-HT2c with selectivity over 5-HT2a. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00141-4

    authors： Isaac M,Slassi A,O'Brien A,Edwards L,MacLean N,Bueschkens D,Lee DK,McCallum K,De Lannoy I,Demchyshyn L,Kamboj R

    更新日期：2000-05-01 00:00:00

  • Synthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor.

    abstract：:Several efficient synthetic routes for 2-, 4-, and 6-aryl-1,2,4-triazine-3,5-diones were developed. Derivatives were synthesized and studied as gonadotropin-releasing hormone antagonists in an effort to understand structure-activity relationships of the monocyclic compounds. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.06.057

    authors： Pontillo J,Guo Z,Wu D,Struthers RS,Chen C

    更新日期：2005-10-01 00:00:00

  • Pyrrolovesamicols--synthesis, structure and VAChT binding of two 4-fluorobenzoyl regioisomers.

    abstract：:This Letter describes the synthesis of two regioisomers of a new class of vesamicol analogs as possible ligands for imaging the vesicular acetylcholine transporter in future PET studies. The two pyrrolovesamicols (±)-6a and (±)-6b were synthesized by nucleophilic ring opening reaction of a tetrahydroindole epoxide pre...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.01.127

    authors： Wenzel B,Li Y,Kraus W,Sorger D,Sabri O,Brust P,Steinbach J

    更新日期：2012-03-15 00:00:00

  • Glycan multivalency effects toward albumin enable N-glycan-dependent tumor targeting.

    abstract：:Multivalent interactions play an essential role in molecular recognition in living systems. These effects were employed to target tumor cells using albumin clusters bearing ∼10 molecules of asparagine-linked glycans (N-glycans). Noninvasive near-infrared fluorescence imaging clearly revealed A431 tumors implanted in B...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.03.046

    authors： Ogura A,Tahara T,Nozaki S,Onoe H,Kurbangalieva A,Watanabe Y,Tanaka K

    更新日期：2016-05-01 00:00:00

  • New conformationally locked bicyclic N,O-nucleoside analogues of antiviral drugs.

    abstract：:In order to obtain rigidity within the sugar moiety of nucleosides, the bicyclic pyrimidine derivatives of N,O-isoxazolidines were designed and synthesized by using 1,3-dipolar cycloaddition of Delta(1)-pyrrolidine-1-oxide and the appropriate vinyl-nucleobases. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.11.048

    authors： Procopio A,Alcaro S,De Nino A,Maiuolo L,Ortuso F,Sindona G

    更新日期：2005-02-01 00:00:00

  • Substituted 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones as novel anti-MRSA agents: synthesis, SAR, and in-vitro assessment.

    abstract：:In search for a new antibacterial agent with improved antimicrobial spectrum and potency, we designed and synthesized a series of novel 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones 7a-h by convergent synthesis approach. All the synthesized compounds were assayed for their in-vitro antibacteri...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.07.007

    authors： Diwakar SD,Bhagwat SS,Shingare MS,Gill CH

    更新日期：2008-08-15 00:00:00

  • Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).

    abstract：:An HTS screening campaign identified a series of low molecular weight phenols that showed excellent selectivity (>100-fold) for HDAC1/HDAC2 over other Class I and Class II HDACs. Evolution and optimization of this HTS hit series provided HDAC1-selective (SHI-1) compounds with excellent anti-proliferative activity and ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.02.012

    authors： Wilson KJ,Witter DJ,Grimm JB,Siliphaivanh P,Otte KM,Kral AM,Fleming JC,Harsch A,Hamill JE,Cruz JC,Chenard M,Szewczak AA,Middleton RE,Hughes BL,Dahlberg WK,Secrist JP,Miller TA

    更新日期：2008-03-15 00:00:00

  • Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.

    abstract：:A series of diphenyl ethers was prepared and evaluated for androgen receptor antagonist activity in human androgen receptor binding and cellular functional assays. Analogs with potent in vitro activities were evaluated for topical in vivo efficacy in the Golden Syrian Hamster ear model. Several compounds showed reduct...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.02.104

    authors： Mitchell LH,Hu LY,Nguyen M,Fakhoury S,Smith Y,Iula D,Kostlan C,Carroll M,Dettling D,Du D,Pocalyko D,Wade K,Lefker B

    更新日期：2009-04-15 00:00:00

  • Chemoenzymatic deacylation of ramoplanin.

    abstract：:The chemoenzymatic deacylation of ramoplanin A2 is described for the first time: ramoplanin A2 was Boc-protected and hydrogenated to Boc-protected tetrahydroramoplanin, which was subsequently deacylated using an acylase from Actinoplanes utahensis NRRL 12052. The chemoenzymatic process proceeded with 80% overall yield...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.06.046

    authors： Gandolfi R,Marinelli F,Ragg E,Romano D,Molinari F

    更新日期：2012-08-15 00:00:00

  • Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors.

    abstract：:A series of 9-aminoalkanamido-1-azabenzanthrones derviatives (3a-i Ar-NHCO(CH(2))(n)NR(1)R(2)) and their quaternary methiodide salts (4a-g Ar-NHCO(CH(2))(n)N(+)(CH(3))R(1)R(2)I(-)) were designed and synthesized as acetylcholinesterase (AChE) or butyrylcholinesterase (BuChE) inhibitors. The synthetic compounds exhibite...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.04.015

    authors： Tang H,Ning FX,Wei YB,Huang SL,Huang ZS,Chan AS,Gu LQ

    更新日期：2007-07-01 00:00:00

  • An atom economic synthesis and antitubercular evaluation of novel spiro-cyclohexanones.

    abstract：:The 1,3-dipolar cycloaddition of azomethine ylides derived from acenaphthenequinone and alpha-amino acids viz. sarcosine, phenylglycine, 1,3-thiazolane-4-carboxylic acid and proline to a series of 2,6-bis[(E)-arylmethylidene]cyclohexanones afforded novel spiro-heterocycles chemo-, regio- and stereoselectively in quant...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.05.018

    authors： Ranjith Kumar R,Perumal S,Manju SC,Bhatt P,Yogeeswari P,Sriram D

    更新日期：2009-07-01 00:00:00

  • Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability.

    abstract：:A series of phosphate and ester-based prodrugs of anilinopyrazinone 1 (BMS-665053) containing either a methylene or an (acyloxy)alkoxy linker was prepared and evaluated in rat pharmacokinetic studies with the goal of improving the oral bioavailability of the parent (1). The prodrugs, in general, had improved aqueous s...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2017.02.015

    authors： Hartz RA,Vrudhula VM,Ahuja VT,Grace JE,Lodge NJ,Bronson JJ,Macor JE

    更新日期：2017-03-15 00:00:00

  • Structure-activity relationships for analogues of the phenazine-based dual topoisomerase I/II inhibitor XR11576.

    abstract：:As part of a programme to identify further analogues of the dual topo I/II inhibitor XR11576, we describe here the syntheses and SAR studies of various 'minimal' and 3,4-benzofused phenazine chromophores of the phenazine template of XR11576. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00770-3

    authors： Wang S,Miller W,Milton J,Vicker N,Stewart A,Charlton P,Mistry P,Hardick D,Denny WA

    更新日期：2002-02-11 00:00:00

  • 1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.

    abstract：:The synthesis of a series of novel 1-[(benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles is described. The compounds were tested for human placental aromatase inhibition in vitro, using [1beta-3H]-androstenedione as the substrate for the aromatase enzyme, the percentage inhibition and IC50 data is included. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00328-5

    authors： Vinh TK,Ahmadi M,Delgado PO,Perez SF,Walters HM,Smith HJ,Nicholls PJ,Simons C

    更新日期：1999-07-19 00:00:00

  • 3-Methoxycarbonyl-5-nitrophenyl boronic acid: high affinity diol recognition at neutral pH.

    abstract：:Several boronic acids were screened for their ability to bind to diols. 3-methoxycarbonyl-5-nitrophenyl boronic acid bound to both a catechol dye as well as fructose with a comparable affinity to that of an ortho-methylamino substituted boronic acid. This work suggests a greater role for appropriately functionalized e...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2003.10.017

    authors： Mulla HR,Agard NJ,Basu A

    更新日期：2004-01-05 00:00:00

  • Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.

    abstract：:The discovery, synthesis, potential binding mode, and in vitro kinase profile of several pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines as potent kinase inhibitors are discussed. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.05.100

    authors： Alberti MJ,Auten EP,Lackey KE,McDonald OB,Wood ER,Preugschat F,Cutler GJ,Kane-Carson L,Liu W,Jung DK

    更新日期：2005-08-15 00:00:00

  • New highly selective inhibitors of class II fructose-1,6-bisphosphate aldolases.

    abstract：:Phosphoglycolo amidoxime and phosphoglycolo hydrazide, two new derivatives of phosphoglycolic acid, were synthesised and successfully tested as selective competitive inhibitors of class II FBP-aldolases. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.03.040

    authors： Fonvielle M,Weber P,Dabkowska K,Therisod M

    更新日期：2004-06-07 00:00:00

  • Synthesis of novel multivalent fluorescent inhibitors with high affinity to prostate cancer and their biological evaluation.

    abstract：:Prostate-specific membrane antigen (PSMA) is an important biological target for therapy and diagnosis of prostate cancer. In this study, novel multivalent PSMA inhibitors with glutamate-urea-lysine structures were designed to improve inhibition characteristics. Precursors of the novel inhibitors were prepared from glu...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2018.01.047

    authors： Kwon YD,Chung HJ,Lee SJ,Lee SH,Jeong BH,Kim HK

    更新日期：2018-02-15 00:00:00

  • Introduction of a nitroxide group on position 2 of 9-phenoxyacridine: easy access to spin labelled DNA-binding conjugates.

    abstract：:In the search for spin labelled intercalators of general use to construct DNA-binding conjugates, 6-chloro-2-[(1-oxyl-2,2,5,5-tetramethyl- pyrrolin-3-yl)methyloxy]-9-phenoxy-acridine 5, has been prepared. This key-intermediate reacts with amines to give the corresponding labelled 9-amino substituted acridines. Compara...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(98)00089-4

    authors： Belmont P,Chapelle C,Demeunynck M,Michon J,Michon P,Lhomme J

    更新日期：1998-03-17 00:00:00

  • Neamphamide B, new cyclic depsipeptide, as an anti-dormant mycobacterial substance from a Japanese marine sponge of Neamphius sp.

    abstract：:A new cyclic depsipeptide, designated neamphamide B (1), was isolated from a marine sponge of Neamphius sp. collected at Okinawa, Japan in 1993 as an anti-mycobacterial substance against active and dormant bacilli. The planar structure of neamphamide B (1) was determined on the basis of spectroscopic analysis, and ste...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2012.05.071

    authors： Yamano Y,Arai M,Kobayashi M

    更新日期：2012-07-15 00:00:00

  • Submonomer synthesis of azapeptide ligands of the Insulin Receptor Tyrosine Kinase domain.

    abstract：:Azapeptide ligands of the Insulin Receptor Tyrosine Kinase (IRTK) were developed by solid-phase submonomer azapeptide synthesis in sufficient isolated yields (36-55%) and purities >95% for structure-activity relationship studies. The azapeptides adopted folded geometries with some proportion of random coil according t...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.07.046

    authors： Kurian LA,Silva TA,Sabatino D

    更新日期：2014-09-01 00:00:00

  • Copper dipicolinates as peptidomimetic ligands for the Src SH2 domain.

    abstract：:The introduction of copper chelates into peptide mimetics creates the Src SH2 binding ligands and paramagnetic complexes suitable for EPR studies of peptide protein interactions. The dipicolinic acid was attached to SH2 domain targeting fragments by two different linkers. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2004.06.018

    authors： Schmidt B,Jiricek J,Titz A,Ye G,Parang K

    更新日期：2004-08-16 00:00:00

  • Design and evaluation of novel oxadiazole derivatives as potential prostate cancer agents.

    abstract：:Various 1,3,4-oxadiazole derivatives have been synthesized and their antiproliferative properties have been studied. The in vitro screening was performed against androgen dependent (LNCaP) and androgen independent (PC-3) prostate cancer cell lines. Most of the compounds showed promising activity. Among them, compounds...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.04.058

    authors： Mochona B,Qi X,Euynni S,Sikazwi D,Mateeva N,Soliman KF

    更新日期：2016-06-15 00:00:00

  • 4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1 agents.

    abstract：:A series of 4,4-disubstituted cyclohexylamine based CCR5 antagonists has been designed and synthesized. Their antiviral structure-activity relationship has been extensively explored. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.07.074

    authors： Duan M,Aquino C,Dorsey GF Jr,Ferris R,Kazmierski WM

    更新日期：2009-09-01 00:00:00

  • Hydroxyl radicals scavenging activity of N-substituted chitosan and quaternized chitosan.

    abstract：:N-substituted chitosan and quaternized chitosan were synthesized and their antioxidant activity against hydroxyl radicals was assessed, respectively. Compared with the antioxidant activity of chitosan, the results indicated that the two kinds of chitosan derivatives had different scavenging ability on hydroxyl radical...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.09.009

    authors： Guo Z,Liu H,Chen X,Ji X,Li P

    更新日期：2006-12-15 00:00:00

  • Evaluation of nitroalkenes as nitric oxide donors.

    abstract：:Chemiluminescence experiments demonstrate that simple nitroalkenes release low levels of nitric oxide. UV and EPR measurements suggest but cannot confirm direct NO release from nitroalkenes. Given the biological activity of nitrated unsaturated fatty acids, these results suggest the possible metabolic conversion of ni...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2007.01.016

    authors： Gorczynski MJ,Huang J,Lee H,King SB

    更新日期：2007-04-01 00:00:00

  • Discovery of anabaenopeptin 679 from freshwater algal bloom material: Insights into the structure-activity relationship of anabaenopeptin protease inhibitors.

    abstract：:Cyanobacteria possess a unique capacity for the production of structurally novel secondary metabolites compared to the biosynthetic abilities of other environmental prokaryotes such as bacteria of the genus Streptomyces. Two different strategies to explore cyanobacteria-derived natural products have been explored prev...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2016.09.008

    authors： Harms H,Kurita KL,Pan L,Wahome PG,He H,Kinghorn AD,Carter GT,Linington RG

    更新日期：2016-10-15 00:00:00

  • Discovery of pyrrolidine-based β-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.

    abstract：:We have developed a novel series of pyrrolidine derived BACE-1 inhibitors. The potency of the weak initial lead structure was enhanced using library-based SAR methods. The series was then further advanced by rational design while maintaining a minimal ligand binding efficiency threshold. Ultimately, the co-crystal str...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.11.024

    authors： Stachel SJ,Steele TG,Petrocchi A,Haugabook SJ,McGaughey G,Katharine Holloway M,Allison T,Munshi S,Zuck P,Colussi D,Tugasheva K,Wolfe A,Graham SL,Vacca JP

    更新日期：2012-01-01 00:00:00

  • Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists.

    abstract：:A series of novel 1,3-benzodiazapine based D1 antagonists was designed according to the understanding of pharmacophore models derived from SCH 23390 (1b), a potent and selective D1 antagonist. The new design features an achiral cyclic-amidine that maintains desired basicity. Solid phase synthesis was developed for SAR...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.07.012

    authors： Zhu Z,Sun ZY,Ye Y,McKittrick B,Greenlee W,Czarniecki M,Fawzi A,Zhang H,Lachowicz JE

    更新日期：2009-09-01 00:00:00