当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > InCl3 mediated heteroarylation of indoles and their derivatization via CH activation strategy: Discovery of 2-(1H-indol-3-yl)-quinoxaline derivatives as a new class of PDE4B selective inhibitors for arthritis and/or multiple sclerosis.

InCl3 mediated heteroarylation of indoles and their derivatization via CH activation strategy: Discovery of 2-(1H-indol-3-yl)-quinoxaline derivatives as a new class of PDE4B selective inhibitors for arthritis and/or multiple sclerosis.

Abstract：

:A new class of PDE4 inhibitors were designed and synthesized via the InCl3 mediated heteroarylation of indoles and their further derivatization through the Pd(II)-catalyzed CH activation strategy. This effort allowed us to discover a series of 2-(1H-indol-3-yl)-quinoxaline based inhibitors possessing PDE4B selectivity over PDE4D and PDE4C. One of these compounds i.e. 3b (PDE4B IC50 = 0.39 ± 0.13 μM with ∼27 and > 250 fold selectivity for PDE4B over PDE4D and C, respectively) showed effects in Zebrafish experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis when dosed at 3, 10 and 30 mg/kg intraperitoneally. Indeed, it halted the progression of the disease across all these doses tested. At an intraperitoneal dose of 30 mg/kg the compound 3b showed promising effects in adjuvant induced arthritic rats. The compound reduced paw volume, inflammation and pannus formation (in the knee joints) as well as pro-inflammatory gene expression/mRNA levels significantly in arthritic rats. Moreover, this compound was found to be selective towards PDE4 over other families of PDEs in vitro and safe when tested for its probable toxicity (e.g. teratogenicity, hepatotoxicity and cardiotoxicity) in Zebrafish.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Sunke R,Bankala R,Thirupataiah B,Ramarao EVVS,Kumar JS,Doss HM,Medishetti R,Kulkarni P,Kapavarapu RK,Rasool M,Mudgal J,Mathew JE,Shenoy GG,Parsa KVL,Pal M

doi

10.1016/j.ejmech.2019.04.020

subject

Has Abstract

pub_date

2019-07-15 00:00:00

pages

198-215

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30326-5

journal_volume

174

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Design, synthesis and in vitro evaluation of heterobivalent peptidic radioligands targeting both GRP- and VPAC1-Receptors concomitantly overexpressed on various malignancies - Is the concept feasible?

    abstract：:Radiolabeled heterobivalent peptidic ligands (HBPLs), being able to address different receptors, are highly interesting tumor imaging agents as they can offer multiple advantages over monovalent peptide receptor ligands. However, few examples of radiolabeled HBPLs have been described so far. One promising approach is ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.05.047

    authors： Lindner S,Fiedler L,Wängler B,Bartenstein P,Schirrmacher R,Wängler C

    更新日期：2018-07-15 00:00:00

  • Synthesis and biological evaluation of 2,3-diarylimidazo[1,2-a]pyridines as antileishmanial agents.

    abstract：:A novel series of 2,3-diarylimidazo[1,2-a]pyridines was synthesized and evaluated for their antileishmanial activities. Four derivatives exhibited good activity against the promastigote and intracellular amastigote stages of Leishmania major, coupled with a low cytotoxicity against the HeLa human cell line. The impact...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.10.048

    authors： Marhadour S,Marchand P,Pagniez F,Bazin MA,Picot C,Lozach O,Ruchaud S,Antoine M,Meijer L,Rachidi N,Le Pape P

    更新日期：2012-12-01 00:00:00

  • A novel orally active inhibitor of HLE.

    abstract：:Human leukocyte elastase (HLE) is a serine proteinase, capable of degrading a variety of structural matrix proteins. SSR69071 2-[(4-isopropyl-6-methoxy-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methoxy]-9-(2-piperidin-1-ylethoxy)-4H-pyrido[1,2-a]pyrimidin-4-one was selected as a novel orally active HLE inhibitor f...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(03)00046-1

    authors： Varga M,Kapui Z,Bátori S,Nagy LT,Vasvári-Debreczy L,Mikus E,Urbán-Szabó K,Arányi P

    更新日期：2003-04-01 00:00:00

  • Synthesis, spectral characterization and bio-analysis of some organotin(IV) complexes.

    abstract：:Five novel organotin(IV) derivatives have been synthesized by refluxing trimethyl, triethyl, tributyl, and triphenyl and tribenzyltin chloride with Schiff base derived from salicylaldehyde and adenine. These compounds were characterized by spectroscopic (IR, (1)H, (13)C, (119)Sn-NMR, (119m)Sn Mössbauer) techniques and...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.019

    authors： Rehman W,Baloch MK,Badshah A

    更新日期：2008-11-01 00:00:00

  • Novel antiacanthamoebic compounds belonging to quinazolinones.

    abstract：:We report one-pot synthesis of a series of new 3-aryl-8-methylquinazolin-4(3H)-ones (QNZ) and their antimicrobial activity against Acanthamoeba castellanii belonging to T4 genotype. A library of fifteen synthetic derivatives of QNZs was synthesized, and their structural elucidation was performed by using nuclear magne...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111575

    authors： Anwar A,Shahbaz MS,Saad SM,Kanwal,Khan KM,Siddiqui R,Khan NA

    更新日期：2019-11-15 00:00:00

  • Sesquiterpene lactones from Inula falconeri, a plant endemic to the Himalayas, as potential anti-inflammatory agents.

    abstract：:A phytochemical investigation of Inula falconeri, a plant endemic to the Himalayas, afforded 10 new sesquiterpenoids and 26 known sesquiterpene lactones, including those bearing guaiane, pseudoguaiane, xanthane, eudesmane, germacrane, rare secocaryophyllane, chromolaevane, and carabrane frameworks. The structures were...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.08.047

    authors： Cheng X,Zeng Q,Ren J,Qin J,Zhang S,Shen Y,Zhu J,Zhang F,Chang R,Zhu Y,Zhang W,Jin H

    更新日期：2011-11-01 00:00:00

  • 5-Substituted [1]pyrindine derivatives with antiproliferative activity.

    abstract：:We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cytotoxicity against tumor cells in the micromolar range but h...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.11.028

    authors： Kolb S,Goddard ML,Loukaci A,Mondésert O,Ducommun B,Braud E,Garbay C

    更新日期：2010-03-01 00:00:00

  • Synthesis, characterization and antimicrobial studies of some new quinoline incorporated benzimidazole derivatives.

    abstract：:Two new series of quinoline incorporated benzimidazole derivatives (4a-i and 8a-f) were synthesized from substituted aniline and isatin through multi-step reaction. 6-substituted-4-carboxyquinolines (3a,b and 7) were synthesized by multi component one pot reactions (via Doebner reaction and Pfitzinger reaction respect...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.05.027

    authors： Garudachari B,Satyanarayana MN,Thippeswamy B,Shivakumar CK,Shivananda KN,Hegde G,Isloor AM

    更新日期：2012-08-01 00:00:00

  • Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening.

    abstract：:Various 3-[4-(substituted phenyl)-1,3-thiazol-2-ylamino]-4-(substituted phenyl)-4,5-dihydro-1H-1,2,4-triazole-5-thiones (7a-t) were designed keeping in view the structural requirements suggested in the pharmacophore model for anticonvulsant activity. Thiazole and triazole moieties being anticonvulsants were clubbed to...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.12.062

    authors： Siddiqui N,Ahsan W

    更新日期：2010-04-01 00:00:00

  • Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry perspective.

    abstract：:As a dual-specificity protein kinase, monopolar spindle 1 (Mps1) is one of the main kinases involved in kinetochore localization and the spindle assembly checkpoint (SAC). Cancer cells often display chromosomal instability, which is a consequence of disfunction of cell cycle checkpoints partially. Mps1 is overexpresse...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2019.04.047

    authors： Wang S,Zhang M,Liang D,Sun W,Zhang C,Jiang M,Liu J,Li J,Li C,Yang X,Zhou X

    更新日期：2019-08-01 00:00:00

  • Design of antineoplastic agents based on the '2-phenylnaphthalene-type' structural pattern--synthesis and biological activity studies of 11H-indolo[3.2-c]quinoline derivatives.

    abstract：:Designed as a new group of planar molecule containing the proposed 2-phenylnaphthalene-type structure, a number of 11H-indolo[3.2-c]quinoline derivatives were synthesized and evaluated biologically. Several compounds were found to possess cytotoxic activity against the growth of human promyelocytic leukemia cells (HL-...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(02)01420-4

    authors： He L,Chang HX,Chou TC,Savaraj N,Cheng CC

    更新日期：2003-01-01 00:00:00

  • Novel (E)-5-styryl-2,2'-bithiophene derivatives as ligands for β-amyloid plaques.

    abstract：:In continuation of our investigation on the bithiophene structure as potential β-amyloid probes, a series of (E)-5-styryl-2,2'-bithiophene (SBTP) derivatives was designed and synthesized. In vitro binding showed that all of them displayed high binding affinities to Aβ(1-42) aggregates (K(i)=0.10-41.05nM). Moreover, tw...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.04.015

    authors： Cui M,Li Z,Tang R,Jia H,Liu B

    更新日期：2011-07-01 00:00:00

  • Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues.

    abstract：:Four mexiletine analogues have been tested for their antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig heart tissues and to assess calcium antagonist activity, in comparison with the parent compound mexiletine. All analogues showed from moderate to high antiarrhythmic activity. In particular, ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.046

    authors： Roselli M,Carocci A,Budriesi R,Micucci M,Toma M,Di Cesare Mannelli L,Lovece A,Catalano A,Cavalluzzi MM,Bruno C,De Palma A,Contino M,Perrone MG,Colabufo NA,Chiarini A,Franchini C,Ghelardini C,Habtemariam S,Lentini G

    更新日期：2016-10-04 00:00:00

  • QSAR study on tetrahydroquinoline analogues as plasmodium protein farnesyltransferase inhibitors: a comparison of rationales of malarial and mammalian enzyme inhibitory activities for selectivity.

    abstract：:The quantitative structure-activity relationships of Plasmodium falciparum and Rat protein farnesyltransferase (PFT) inhibitory activities of 6-cyano-1-(3-methyl-3H-imidazoly-4-ylmethyl)-3-substituted-1,2,3,4-tetrahydroquinoline (THQ) analogues are investigated in order to explore the similarities/deviations between t...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.025

    authors： Gupta MK,Prabhakar YS

    更新日期：2008-12-01 00:00:00

  • Novel HIV-1 capsid-targeting small molecules of the PF74 binding site.

    abstract：:The PF74 binding site in HIV-1 capsid protein (CA) is a compelling antiviral drug target. Although PF74 confers mechanistically distinct antiviral phenotypes by competing against host factors for CA binding, it suffers from prohibitively low metabolic stability. Therefore, there has been increasing interest in designi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112626

    authors： Wang L,Casey MC,Vernekar SKV,Sahani RL,Kankanala J,Kirby KA,Du H,Hachiya A,Zhang H,Tedbury PR,Xie J,Sarafianos SG,Wang Z

    更新日期：2020-10-15 00:00:00

  • Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.

    abstract：:Accetohydroxyacid synthase (AHAS) is the first enzyme involved in the biosynthetic pathway of branched-chain amino acids. Earlier gene mutation of Candida albicans in a mouse model suggested that this enzyme is a promising target of antifungals. Recent studies have demonstrated that some commercial AHAS-inhibiting sul...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.11.005

    authors： Wu RJ,Ren T,Gao JY,Wang L,Yu Q,Yao Z,Song GQ,Ruan WB,Niu CW,Song FH,Zhang LX,Li M,Wang JG

    更新日期：2019-01-15 00:00:00

  • Novel 8-arylated purines as inhibitors of glycogen synthase kinase.

    abstract：:A series of 8-arylated purine derivatives bearing either an aniline or an alkyl amide at position 6 were found to inhibit glycogen synthase kinase-3, with good selectivity over ten kinases. Molecular modeling studies indicated that the most active compounds (8a and 8e), adopt a planar conformation, close to the shape ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.04.026

    authors： Ibrahim N,Mouawad L,Legraverend M

    更新日期：2010-08-01 00:00:00

  • Synthesis and pharmacological evaluation of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives as anti-inflammatory and analgesic agents.

    abstract：:A series of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives have been synthesized. The structures of these compounds were established by IR, 1H NMR, 13C NMR, Mass spectral data and elemental analyses. Compounds were evaluated for their anti-inflammatory and analgesic activity as well as gastri...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.01.067

    authors： Gaba M,Singh D,Singh S,Sharma V,Gaba P

    更新日期：2010-06-01 00:00:00

  • Synthesis of novel bioactive derivatives of 3-(4-chlorophenyl)-2-hydrazino-5,6,7,8-tetrahydrobenzo(b)thieno[2,3-d]pyrimidine-4(3H)-ones.

    abstract：:A series of triazolo[4,3-a]tetrahydrobenzo(b)thieno[3,2-e]pyrimidine-5(4H)-ones (12a-n) were synthesized and evaluated for CNS depressant, skeletal muscle relaxant and anticonvulsant activities by photoactometer, Rotarod and pentylenetetrazole induced the convulsions method respectively in Swiss albino mice. Diazepam ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.05.027

    authors： Gupta SV,Baheti K,Bora R,Dekhane D,Chhabría M,Shingare M,Pawar S,Shishoo CJ,Thore SN

    更新日期：2009-11-01 00:00:00

  • Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease.

    abstract：:Designing drugs with a specific multi-target profile is a promising approach against multifactorial illnesses as Alzheimer's disease. In this work, new indazole ethers that possess dual activity as both cannabinoid agonists CB2 and inhibitors of BuChE have been designed by computational methods. On the basis of this k...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.11.026

    authors： González-Naranjo P,Pérez-Macias N,Campillo NE,Pérez C,Arán VJ,Girón R,Sánchez-Robles E,Martín MI,Gómez-Cañas M,García-Arencibia M,Fernández-Ruiz J,Páez JA

    更新日期：2014-02-12 00:00:00

  • Alpha (α-) and beta (β-carboranyl-C-deoxyribosides: syntheses, structures and biological evaluation.

    abstract：:The syntheses of the unprotected neutral closo-carboranyl-C-deoxyriboses, starting from anomeric mixture of 1-ethynyldeoxyriboses, and their corresponding open-cage nido-derivatives have been described. The structures of both the α- and β-anomers were confirmed by single-crystal X-ray diffraction. While limited water ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.06.005

    authors： Šnajdr I,Janoušek Z,Takagaki M,Císařová I,Hosmane NS,Kotora M

    更新日期：2014-08-18 00:00:00

  • Peptidyl 3-substituted 1-hydroxyureas as isosteric analogues of succinylhydroxamate MMP inhibitors.

    abstract：:To evaluate N-hydroxyurea as zinc binding group in the design of MMP inhibitors, two peptidyl 1-hydroxyureas were prepared by N-hydroxycarbamoylation of the diastereomeric dipeptides H-Leu-Phe-NHMe and H-D-Leu-Phe-NHMe. Peptidyl 1-hydroxyureas were more potent than the parent peptides, but dramatically weaker (4-5 ord...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.07.002

    authors： Campestre C,Tortorella P,Agamennone M,Preziuso S,Biasone A,Nuti E,Rossello A,Gallina C

    更新日期：2008-05-01 00:00:00

  • New bis(hydroxymethyl) alkanoate curcuminoid derivatives exhibit activity against triple-negative breast cancer in vitro and in vivo.

    abstract：:Novel bis(hydroxymethyl) alkanoate curcuminoid derivatives were designed, synthesized and screened for in vitro antiproliferative and in vivo antitumor activity. Selected new compound 9a and curcumin were further evaluated for inhibitory activity against ER+/PR+ breast cancer (MCF-7, T47D), HER 2+ breast cancer (SKBR3...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.03.006

    authors： Hsieh MT,Chang LC,Hung HY,Lin HY,Shih MH,Tsai CH,Kuo SC,Lee KH

    更新日期：2017-05-05 00:00:00

  • Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives.

    abstract：:Some novel pyrimidine-5-carbonitrile derivatives bearing various substituent have been synthesized. The structures of target compounds were confirmed by elemental analysis and spectral data. Some selected members of the newly synthesized compounds were investigated for their cytotoxic potency against certain human tum...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.05.028

    authors： Fargualy AM,Habib NS,Ismail KA,Hassan AM,Sarg MT

    更新日期：2013-08-01 00:00:00

  • Synthesis and biological evaluation of novel structural hybrids of benzofuroxan derivatives and fluoroquinolones.

    abstract：:A series of novel hybrids based on benzofuroxan derivatives and fluoroquinolones (4a-d-6a-d) have been synthesized. Unexpectedly, the reactions have resulted in salt products formation during the hydrolysis of benzofuroxans by water molecules being present in the solvent instead of usual substitution products. All the...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.03.086

    authors： Chugunova E,Akylbekov N,Bulatova A,Gavrilov N,Voloshina A,Kulik N,Zobov V,Dobrynin A,Syakaev V,Burilov A

    更新日期：2016-06-30 00:00:00

  • Rational design, synthesis and QSAR study of vasorelaxant active 3-pyridinecarbonitriles incorporating 1H-benzimidazol-2-yl function.

    abstract：:A variety of 2-alkoxy-4-aryl-6-(1H-benzimidazol-2-yl)-3-pyridinecarbonitriles 4a-r were prepared via either regioselective reaction of 3-aryl-1-(1H-benzimidazol-2-yl)-2-propen-1-ones 3 with malononitrile or ylidenemalononitriles 6 with 2-acetyl-1H-benzimidazoles 1 in the presence of sodium alkoxide in the correspondin...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.01.042

    authors： Nofal ZM,Srour AM,El-Eraky WI,Saleh DO,Girgis AS

    更新日期：2013-05-01 00:00:00

  • Novel pyrazolopyridine derivatives as potential angiogenesis inhibitors: Synthesis, biological evaluation and transcriptome-based mechanistic analysis.

    abstract：:Modified purine derivatives exemplified by pyrazolopyrimidines have emerged as highly selective inhibitors of several angiogenic receptor tyrosine kinases. Herein, we designed and synthesized a new series of substituted pyrazolopyridines and explored their ability to influence crucial pro-angiogenic attributes of endo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.035

    authors： Michailidou M,Giannouli V,Kotsikoris V,Papadodima O,Kontogianni G,Kostakis IK,Lougiakis N,Chatziioannou A,Kolisis FN,Marakos P,Pouli N,Loutrari H

    更新日期：2016-10-04 00:00:00

  • Salicylanilides as inhibitors of the protein tyrosine kinase epidermal growth factor receptor.

    abstract：:A pharmacophore model for ATP-competitive inhibitors interacting with the active site of the EGFR protein tyrosine kinase and a putative binding mode of 4-anilinoquinazoline suggest that a salicylic acid function could serve as the pharmacophore replacement of a pyrimidine ring. Superpositions by CAMM of salicylanilid...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2003.09.010

    authors： Liechti C,Séquin U,Bold G,Furet P,Meyer T,Traxler P

    更新日期：2004-01-01 00:00:00

  • Dual potent ALK and ROS1 inhibitors combating drug-resistant mutants: Synthesis and biological evaluation of aminopyridine-containing diarylaminopyrimidine derivatives.

    abstract：:To identify ALK and ROS1 dual inhibitors conferring resistance to ALK secondary mutations, especially 'gatekeeper' L1196 M and the most predominant ceritinib-resistant G1202R mutations, a series of novel 2,4-diarylaminopyrimidine analogues were designed and synthesized by incorporating 2-alkoxy-6-alicyclic aminopyridi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.09.012

    authors： Guo M,Zuo D,Zhang J,Xing L,Gou W,Jiang F,Jiang N,Zhang D,Zhai X

    更新日期：2018-10-05 00:00:00

  • 1,2,3-Triazolyl ester of Ketorolac: A "Click Chemistry"-based highly potent PAK1-blocking cancer-killer.

    abstract：:An old anti-inflammatory/analgesic drug called Toradol is a racemic form of Ketorolac (50% R-form and 50% S-form) that blocks the oncogenic RAC-PAK1-COX-2 (cyclooxygenase-2) signaling, through the direct inhibition of RAC by the R-form and of COX-2 by the S-form, eventually down-regulating the production of prostaglan...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.11.038

    authors： Nguyen BCQ,Takahashi H,Uto Y,Shahinozzaman MD,Tawata S,Maruta H

    更新日期：2017-01-27 00:00:00