当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY LETTERS期刊下所有文献 > Optimization of alpha-acylaminoketone ecdysone agonists for control of gene expression.

Optimization of alpha-acylaminoketone ecdysone agonists for control of gene expression.

Abstract：

:Fifteen new alpha-acylaminoketones were prepared by four different routes in an initial effort to optimize the potency of these compounds as ecdysone agonists. The compounds were assayed in mammalian cells expressing the ecdysone receptors from Bombyx mori (BmEcR) and Choristoneura fumiferana (CfEcR) for their ability to cause expression of a reporter gene downstream of an ecdysone response element. A new alpha-acylaminoketone was identified which had activity equal to that of the standard dibenzoylhydrazine ecdysone agonist GS()-E in the assay based on CfEcR.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tice CM,Hormann RE,Thompson CS,Friz JL,Cavanaugh CK,Saggers JA

doi

10.1016/s0960-894x(03)00315-9

subject

Has Abstract

pub_date

2003-06-02 00:00:00

pages

1883-6

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960894X03003159

journal_volume

13

pub_type

杂志文章

相关文献

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS文献大全
  • Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

    abstract：:A series of potent specific HIV-1 RT inhibitory compounds is described. The compounds are urea analogs of PETT (PhenylEthylThiazoleThiourea) derivatives and the series includes derivatives with an ethyl linker (1-6) and conformationally restricted analogs (7-13). The antiviral activity is determined both at the RT lev...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(98)00249-2

    authors： Sahlberg C,Noréen R,Engelhardt P,Högberg M,Kangasmetsä J,Vrang L,Zhang H

    更新日期：1998-06-16 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

  • Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.

    abstract：:A novel series of indole/indazole-aminopyrimidines was designed and synthesized with an aim to achieve optimal potency and selectivity for the c-Jun kinase family or JNKs. Structure guided design was used to optimize the series resulting in a significant potency improvement. The best compound (17) has IC50 of 3 nM for...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 信件

    doi：10.1016/j.bmcl.2013.04.029

    authors： Gong L,Han X,Silva T,Tan YC,Goyal B,Tivitmahaisoon P,Trejo A,Palmer W,Hogg H,Jahagir A,Alam M,Wagner P,Stein K,Filonova L,Loe B,Makra F,Rotstein D,Rapatova L,Dunn J,Zuo F,Dal Porto J,Wong B,Jin S,Chang A,T

    更新日期：2013-06-15 00:00:00

  • Tra1 as a screening target for transcriptional activation domain discovery.

    abstract：:There is tremendous interest in developing activator artificial transcription factors that functionally mimic endogenous transcriptional activators for use as mechanistic probes, as components of synthetic cell circuitry, and in transcription-targeted therapies. Here, we demonstrate that a phage display selection agai...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.05.045

    authors： Majmudar CY,Labut AE,Mapp AK

    更新日期：2009-07-15 00:00:00

  • Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.

    abstract：:Single enantiomer (SS) and (RR) 2-[(phenoxy)(phenyl)methyl]morpholine derivatives 5, 8-23 are inhibitors of monoamine reuptake. Target compounds were prepared using an enantioselective synthesis employing a highly specific enzyme-catalysed resolution of racemic n-butyl 4-benzylmorpholine-2-carboxylate (26) as the key ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2008.03.050

    authors： Fish PV,Deur C,Gan X,Greene K,Hoople D,Mackenny M,Para KS,Reeves K,Ryckmans T,Stiff C,Stobie A,Wakenhut F,Whitlock GA

    更新日期：2008-04-15 00:00:00

  • Discovery of thienopyrimidine-based FLT3 inhibitors from the structural modification of known IKKβ inhibitors.

    abstract：:Inactivation of the NF-κB signaling pathway by inhibition of IKKβ is a well-known approach to treat inflammatory diseases such as rheumatoid arthritis and cancer. Thienopyrimidine-based analogues were designed through modification of the known IKKβ inhibitor, SPC-839, and then biologically evaluated. The resulting ana...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.04.058

    authors： Park CH,Lee C,Yang JS,Joe BY,Chun K,Kim H,Kim HY,Kang JS,Lee JI,Kim MH,Han G

    更新日期：2014-06-15 00:00:00

  • A new strategy for the synthesis of crucigasterin A, and cytotoxic activity of this compound and its related analogues.

    abstract：:Stereoselective total synthesis of bioactive marine natural product crucigasterin A has been accomplished from commercially available and inexpensive L-(-)-malic acid as a starting material. Julia olefination and chelation controlled Grignard additions are the key steps involved in the present synthesis. Cytotoxic pro...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.07.007

    authors： Kumar JN,Reddy PR,Das B,Kumar CG,Sujitha P

    更新日期：2013-09-15 00:00:00

  • Design, synthesis and enzymatic evaluation of 3-O-substituted aryl β-D-galactopyranosides as inhibitors of Trypanosoma cruzi trans-sialidase.

    abstract：:The trans-sialidase of Trypanosoma cruzi (TcTS) is a surface enzyme that modifies the parasite glycocalyx covering it with sialic acid. This process is essential to adhesion and invasion mechanisms in life cycle of the protozoan in the human host, making TcTS a very attractive molecular target for drug design. Using t...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2014.07.088

    authors： Silva BL,S Filho JD,Andrade P,Carvalho I,Alves RJ

    更新日期：2014-09-15 00:00:00

  • Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4).

    abstract：:ADX88178 (1) has been recently developed as a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4). The aim of this study was to develop [(11)C]1 as a novel positron emission tomography ligand and to evaluate its binding ability for mGluR4. Using stannyl precursor 3, [(11)C]1 was efficie...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.12.008

    authors： Fujinaga M,Yamasaki T,Nengaki N,Ogawa M,Kumata K,Shimoda Y,Yui J,Xie L,Zhang Y,Kawamura K,Zhang MR

    更新日期：2016-01-15 00:00:00

  • Synthesis of novel benzothiazole amides: Evaluation of PPAR activity and anti-proliferative effects in paraganglioma, pancreatic and colorectal cancer cell lines.

    abstract：:The reduced activation of PPARs has a positive impact on cancer cell growth and viability in multiple preclinical tumor models, suggesting a new therapeutic potential for PPAR antagonists. In the present study, the benzothiazole amides 2a-g were synthesized and their activities on PPARs were investigated. Transactivat...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.06.020

    authors： Ammazzalorso A,De Lellis L,Florio R,Laghezza A,De Filippis B,Fantacuzzi M,Giampietro L,Maccallini C,Tortorella P,Veschi S,Loiodice F,Cama A,Amoroso R

    更新日期：2019-08-15 00:00:00

  • Substituted tetrahydro-beta-carbolines as potential agents for the treatment of human papillomavirus infection.

    abstract：:The identification and optimization of a series of substituted tetrahydro-beta-carbolines with potent activity against human papillomavirus is described. Structure-activity studies focused on the substitution pattern and chirality of the beta-carboline ring system are discussed. Optimization of these parameters led to...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.10.123

    authors： Miller JF,Turner EM,Sherrill RG,Gudmundsson K,Spaltenstein A,Sethna P,Brown KW,Harvey R,Romines KR,Golden P

    更新日期：2010-01-01 00:00:00

  • Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers.

    abstract：:The synthesis and structure-activity relationship (SAR) study of a novel series of N-type calcium channel blockers are described. L-Cysteine derivative 2a was found to be a potent and selective N-type calcium channel blocker with IC(50) 0.63 microM on IMR-32 assay. Compound 2a showed analgesic efficacy in the rat form...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00414-0

    authors： Seko T,Kato M,Kohno H,Ono S,Hashimura K,Takimizu H,Nakai K,Maegawa H,Katsube N,Toda M

    更新日期：2001-08-20 00:00:00

  • Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors.

    abstract：:Post-translational modulation of eIF4E through phosphorylation by Mnks is highly integral to the pathogenesis of different cancers. Therefore, inhibition of Mnks offers a strategy for cancer treatment. Herein, a series of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives is presented as Mnk in...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.07.043

    authors： Abdelaziz AM,Basnet SKC,Islam S,Li M,Tadesse S,Albrecht H,Gerber C,Yu M,Wang S

    更新日期：2019-09-15 00:00:00

  • Combined tachykinin receptor antagonist: synthesis and stereochemical structure-activity relationships of novel morpholine analogues.

    abstract：:We report herein the synthesis and stereochemical structure-activity relationships of novel morpholine analogues 12 and 13 with regards to NK1, NK2 and NK3 tachykinin receptor binding affinity. An essential requirement for more potent binding affinities was controlled by absolute configuration. (S,R)-12 and (S,R)-13 e...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(00)00324-3

    authors： Nishi T,Ishibashi K,Takemoto T,Nakajima K,Fukazawa T,Iio Y,Itoh K,Mukaiyama O,Yamaguchi T

    更新日期：2000-08-07 00:00:00

  • Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.

    abstract：:Bioisosteric substitution of the thiourea (3, 5, 7, 9) and urea (10) moiety of PETT compounds with sulfamide (1), cyanoguanidine (2, 4) and guanidine (6, 8) functionalities, and replacement of the phenethyl group with benzoylethyl group (compounds 11-20) have been studied. Synthesis and antiviral activities are descri...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00675-7

    authors： Högberg M,Engelhardt P,Vrang L,Zhang H

    更新日期：2000-02-07 00:00:00

  • Mariannamides A and B, new cyclic octapeptides isolated from Mariannaea elegans NBRC102301.

    abstract：:Two new cyclic octapeptides, mariannamides A (1) and B (2), have been isolated from Mariannaea elegans NBRC102301, a Pinus densiflora-derived filamentous fungus. Their structures were elucidated to be cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l-Val1-l-Ile2) and cyclo-(l-Leu1-l-Pro1-l-Pro2-l-Leu2-l-Ile1-l-Pro3-l...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2019.126946

    authors： Ishiuchi K,Hirose D,Kondo T,Watanabe K,Terasaka K,Makino T

    更新日期：2020-02-15 00:00:00

  • Lead optimization of an acylhydrazone scaffold possessing antiviral activity against Lassa virus.

    abstract：:Previously we reported the optimization of antiviral scaffolds containing benzimidazole and related heterocycles possessing activity against a variety of arenaviruses. These series of compounds were discovered through an HTS campaign of a 400,000 small molecule library using lentivirus-based pseudotypes incorporated w...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2013.08.103

    authors： Burgeson JR,Gharaibeh DN,Moore AL,Larson RA,Amberg SM,Bolken TC,Hruby DE,Dai D

    更新日期：2013-11-01 00:00:00

  • First hydroxamate inhibitors for carboxypeptidase A. N-acyl-N-hydroxy-beta-phenylalanines.

    abstract：:A series of N-acyl-N-hydroxy-beta-Phe were designed, synthesized, and shown to have potent inhibitory activity for carboxypeptidase A (CPA). They are the first examples of CPA inhibitors having a hydroxamate functionality. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(99)00055-4

    authors： Kim DH,Jin Y

    更新日期：1999-03-08 00:00:00

  • Synthetic analogs of daidzein, having more potent osteoblast stimulating effect.

    abstract：:A series of didzein derivatives were synthesized and assessed for stimulation of osteoblast differentiation using primary cultures of rat calvarial osteoblasts. Data suggested that three synthetic analogs, 1c, 3a and 3c were several folds more potent than daidzein in stimulating differentiation and mineralization of o...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.12.008

    authors： Yadav DK,Gautam AK,Kureel J,Srivastava K,Sahai M,Singh D,Chattopadhyay N,Maurya R

    更新日期：2011-01-15 00:00:00

  • Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.

    abstract：:A series of bivalent hydroxy ether butorphan ligands were prepared and their binding affinities at the opioid receptors determined. Addition of a hydroxy group to a hydrocarbon chain can potentiate binding affinity up to 27- and 86-fold at the mu and kappa opioid receptors, respectively. Two bivalent ligands with sub-...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.01.101

    authors： Fulton BS,Knapp BL,Bidlack JM,Neumeyer JL

    更新日期：2010-03-01 00:00:00

  • Efficient synthesis and biological evaluation of some 2,4-diamino-furo[2,3-d]pyrimidine derivatives.

    abstract：:The carbodiimides 2, obtained from aza-Wittig reactions of iminophosphorane 1 with aromatic isocyanates, reacted with ammonia to give ethyl 3,4-dihydro-6-methyl-4-oxo-2-arylamino-furo[2,3-d]pyrimidine-5-carboxylate 3. Further reaction of 3 with POCl(3) and various amines generated ethyl 4-alkylamino-2-arylamino-6-meth...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.08.122

    authors： Hu YG,Wang Y,Du SM,Chen XB,Ding MW

    更新日期：2010-11-01 00:00:00

  • Diamino-C,N-diarylpyridine positional isomers as inhibitors of lysophosphatidic acid acyltransferase-beta.

    abstract：:2,6-Diamino-4,N-diarylpyridines were identified as potent, isoform selective inhibitors of the enzymatic activity of lysophosphatidic acid acyltransferase-beta (LPAAT-beta). ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2005.07.055

    authors： Hong F,Hollenback D,Singer JW,Klein P

    更新日期：2005-11-01 00:00:00

  • Highly potent inhibitors of TNF-alpha production. Part 1: Discovery of chemical leads.

    abstract：:The discovery of 2-acylamino-2-phenylethyl disodium phosphates and as structurally novel inhibitors of TNF-alpha production is reported. Structure-activity relationships (SARs) are also discussed. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(02)00036-7

    authors： Matsui T,Kondo T,Nishita Y,Itadani S,Nakatani S,Omawari N,Sakai M,Nakazawa S,Ogata A,Ohno H,Obata T,Nakai H,Toda M

    更新日期：2002-03-25 00:00:00

  • Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of N,N'-bis[2-oxo-2H-benzopyran]-3-carboxamides.

    abstract：:A novel series of N,N'-bis[2-oxo-2H-1-benzopyran]-3-carboxamide derivatives have been synthesized and investigated for the ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO). Some of the synthesized compounds show good selective inhibitory activity against the MAO-A isoform. Both the MA...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2006.04.026

    authors： Chimenti F,Secci D,Bolasco A,Chimenti P,Granese A,Carradori S,Befani O,Turini P,Alcaro S,Ortuso F

    更新日期：2006-08-01 00:00:00

  • The synthesis of beta-peptides containing guanidino groups.

    abstract：:The synthesis of the beta-peptide 1 by the postsynthetic modification of the corresponding amino-containing peptide 3 is described. The potential of 1 to act as a template for the ligation of complementary negatively-charged peptides is discussed. ...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/s0960-894x(01)00027-0

    authors： Wen K,Han H,Hoffman TZ,Janda KD,Orgel LE

    更新日期：2001-03-12 00:00:00

  • Design and efficient synthesis of novel arylthiourea derivatives as potent hepatitis C virus inhibitors.

    abstract：:A novel class of arylthiourea HCV inhibitors bearing various functionalities, such as cyclic urea, cyclic thiourea, urea, and thiourea, on the alkyl linker were designed and synthesized. Herein we report the synthesis and structure-activity relationships (SARs) of this novel class of arylthiourea derivatives that show...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.09.037

    authors： Kang IJ,Wang LW,Hsu SJ,Lee CC,Lee YC,Wu YS,Yueh A,Wang JC,Hsu TA,Chao YS,Chern JH

    更新日期：2009-11-01 00:00:00

  • Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity.

    abstract：:Pre-clinical investigation of some aryl-piperidinyl ether histamine H3 receptor antagonists revealed a strong hERG binding. To overcome this issue, we have developed a QSAR model specially dedicated to H3 receptor ligands. This model was designed to be directly applicable in medicinal chemistry with no need of molecul...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2011.07.006

    authors： Levoin N,Labeeuw O,Calmels T,Poupardin-Olivier O,Berrebi-Bertrand I,Lecomte JM,Schwartz JC,Capet M

    更新日期：2011-09-15 00:00:00

  • Crystal structure of the most catalytically effective carbonic anhydrase enzyme known, SazCA from the thermophilic bacterium Sulfurihydrogenibium azorense.

    abstract：:Two thermostable α-carbonic anhydrases (α-CAs) isolated from thermophilic Sulfurihydrogenibium spp., namely SspCA (from S. yellowstonensis) and SazCA (from S. azorense), were shown in a previous work to possess interesting complementary properties. SspCA was shown to have an exceptional thermal stability, whereas SazC...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2015.02.068

    authors： De Simone G,Monti SM,Alterio V,Buonanno M,De Luca V,Rossi M,Carginale V,Supuran CT,Capasso C,Di Fiore A

    更新日期：2015-05-01 00:00:00

  • Montmorillonite K-10 catalyzed cyclization of N-ethoxycarbonyl-N'-arylguanidines: access to pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole derivatives.

    abstract：:Two new heterocycles, pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole, were prepared in three steps from 3-aminocarbazole and 3-aminoindole, respectively. The key Friedel-Crafts intramolecular cyclization was realized under microwave irradiation using montmorillonite K-10 clay as a catalyst. The pyrimido[4,5-c]carb...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2010.05.028

    authors： Debray J,Zeghida W,Baldeyrou B,Mahieu C,Lansiaux A,Demeunynck M

    更新日期：2010-07-15 00:00:00

  • Novel C-seco-taxoids possessing high potency against paclitaxel-resistant cancer cell lines overexpressing class III beta-tubulin.

    abstract：:Novel C-seco-taxoids were synthesized from 10-deacetylbaccatin III and their potencies evaluated against drug-sensitive and drug-resistant cancer cell lines. The drug-resistant cell lines include ovarian cancer cell lines resistant to cisplatin, topotecan, adriamycin and paclitaxel overexpressing class III beta-tubuli...

    journal_title：Bioorganic & medicinal chemistry letters

    pub_type： 杂志文章

    doi：10.1016/j.bmcl.2009.04.070

    authors： Pepe A,Sun L,Zanardi I,Wu X,Ferlini C,Fontana G,Bombardelli E,Ojima I

    更新日期：2009-06-15 00:00:00