当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Anthranilic acid based CCK1 receptor antagonists: preliminary investigation on their second "touch point".

Anthranilic acid based CCK1 receptor antagonists: preliminary investigation on their second "touch point".

Abstract：

:In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group. Hence, the modification of the C-terminal pharmacophoric group of our lead VL-0395 can not only enhance the affinity of anthranilic acid derivatives but can modulate the selectivity for one CCK receptor subtype or afford mixed antagonists.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Varnavas A,Lassiani L,Valenta V,Mennuni L,Makovec F,Hadjipavlou-Litina D

doi

10.1016/j.ejmech.2005.01.002

subject

Has Abstract

pub_date

2005-06-01 00:00:00

pages

563-81

issue

6

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(05)00003-6

journal_volume

40

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Addition of thiols to o-quinone methide: new 2-hydroxy-3-phenylsulfanylmethyl[1,4]naphthoquinones and their activity against the human malaria parasite Plasmodium falciparum (3D7).

    abstract：:A series of 36 new phenylsulfanylmethyl[1,4]naphthoquinones (7-42) were synthesized by a three-component reaction that involves lawsone, the appropriate aldehyde and thiols with variable substitution patterns. These reactions involve the in situ generation of o-quinone methides (o-QM) via Knoevenagel condensation and ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.10.052

    authors： Sharma A,Santos IO,Gaur P,Ferreira VF,Garcia CR,da Rocha DR

    更新日期：2013-01-01 00:00:00

  • Design, synthesis and in vitro cell-free/cell-based biological evaluations of novel ERCC1-XPF inhibitors targeting DNA repair pathway.

    abstract：:The structure-specific ERCC1-XPF endonuclease is essential for repairing bulky DNA lesions and helix distortions induced by UV radiation, which forms cyclobutane pyrimidine dimers (CPDs), or chemicals that crosslink DNA strands such as cyclophosphamide and platinum-based chemotherapeutic agents. Inhibition of the ERCC...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112658

    authors： Elmenoufy AH,Gentile F,Jay D,Karimi-Busheri F,Yang X,Soueidan OM,Mani RS,Ciniero G,Tuszynski JA,Weinfeld M,West FG

    更新日期：2020-10-15 00:00:00

  • Para-sulfonatocalix[n]arene-based biomaterials: Recent progress in pharmaceutical and biological applications.

    abstract：:The history, properties, and characteristics of para-sulfonato-calixarenes are described. On the one hand, the inherent antibacterial and antifungal properties against microorganisms, and on the other hand non-toxicity of these supramolecules toward human organs are analyzed. The resulting biocompatibility of para-sul...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112121

    authors： Bahojb Noruzi E,Molaparast M,Zarei M,Shaabani B,Kariminezhad Z,Ebadi B,Shafiei-Irannejad V,Rahimi M,Pietrasik J

    更新日期：2020-03-15 00:00:00

  • Metal complexes of retinoid derivatives with antiproliferative activity: synthesis, characterization and DNA interaction studies.

    abstract：:9-cis-Retinal thiosemicarbazone and its Co(III), Ni(II) and Cu(II) complexes are synthesized and characterized. Central Co(III) atom is in an octahedral environment while Ni(II) and Cu(II) atoms are in a square planar environment. DNA binding constants and spectroscopic data show an intercalative behavior for the nick...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.12.019

    authors： Bisceglie F,Baldini M,Belicchi-Ferrari M,Buluggiu E,Careri M,Pelosi G,Pinelli S,Tarasconi P

    更新日期：2007-05-01 00:00:00

  • Benzofuran derivatives as anticancer inhibitors of mTOR signaling.

    abstract：:A series of 32 derivatives and isosteres of the mTOR inhibitor 2 were synthesized and compared for their cytotoxicity in radioresistant SQ20B cancer cell line. Several of these compounds, in particular 30b, were significantly more cytotoxic than 2. Importantly, 30b was shown to block both mTORC1 and Akt signaling, sug...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.05.014

    authors： Salomé C,Ribeiro N,Chavagnan T,Thuaud F,Serova M,de Gramont A,Faivre S,Raymond E,Désaubry L

    更新日期：2014-06-23 00:00:00

  • An overview on crystal structures of InhA protein: Apo-form, in complex with its natural ligands and inhibitors.

    abstract：:The enoyl-ACP reductase InhA from the mycobacterial fatty acid biosynthesis pathway has become a target of interest for the development of new anti-tubercular drugs. This protein has been identified as essential for the survival of Mycobacterium tuberculosis, the causative agent of tuberculosis, and as the main target...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2018.01.047

    authors： Chollet A,Maveyraud L,Lherbet C,Bernardes-Génisson V

    更新日期：2018-02-25 00:00:00

  • Synthesis, cytotoxicity and apoptosis of naphthalimide polyamine conjugates as antitumor agents.

    abstract：:Several naphthalimide polyamine conjugates were synthesized and evaluated for in vitro cytotoxicity against human leukemia K562, murine melanoma B16, Chinese hamster ovary CHO cell lines. Both triamine moieties and the length of spacers were crucial in elevating the potency of 1,8-naphthalimide. The typical compounds ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.02.044

    authors： Tian ZY,Xie SQ,Du YW,Ma YF,Zhao J,Gao WY,Wang CJ

    更新日期：2009-01-01 00:00:00

  • Efficient identification of novel anti-glioma lead compounds by machine learning models.

    abstract：:Glioblastoma multiforme (GBM) is the most devastating and widespread primary central nervous system tumor. Pharmacological treatment of this malignance is limited by the selective permeability of the blood-brain barrier (BBB) and relies on a single drug, temozolomide (TMZ), thus making the discovery of new compounds c...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111981

    authors： Neves BJ,Agnes JP,Gomes MDN,Henriques Donza MR,Gonçalves RM,Delgobo M,Ribeiro de Souza Neto L,Senger MR,Silva-Junior FP,Ferreira SB,Zanotto-Filho A,Andrade CH

    更新日期：2020-03-01 00:00:00

  • Green synthesis and antimicrobial evaluation of some new trifluoromethyl-substituted hexahydropyrimidines by grinding.

    abstract：:A series of trifluoromethyl-substituted hexahydropyrimidine derivatives were efficiently synthesized in excellent yields via one-pot three-component reaction of aromatic aldehydes, ethyl trifluoroacetoacetate and thiourea(urea) in presence of p-toluenesulfonic acid under solvent-free conditions at room temperature by ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.09.036

    authors： Zohdi HF,Rateb NM,Elnagdy SM

    更新日期：2011-11-01 00:00:00

  • Discovery of tertiary amide derivatives incorporating benzothiazole moiety as anti-gastric cancer agents in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway.

    abstract：:On the basis and continuation of our previous studies on anti-tubulin and anti-gastric cancer agents, novel tertiary amide derivatives incorporating benzothiazole moiety were synthesized and the antiproliferative activity was studied in vitro. Preliminary structure activity relationships (SARs) were explored according...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112618

    authors： Song J,Gao QL,Wu BW,Zhu T,Cui XX,Jin CJ,Wang SY,Wang SH,Fu DJ,Liu HM,Zhang SY,Zhang YB,Li YC

    更新日期：2020-10-01 00:00:00

  • Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease.

    abstract：:New benzofuranylthiazole derivatives containing the aryl-urea moiety were synthesized and evaluated in vitro as dual acetylcholinesterase (AChE)-butyrylcholinesterase (BuChE) inhibitors. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized com...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.07.005

    authors： Kurt BZ,Gazioglu I,Basile L,Sonmez F,Ginex T,Kucukislamoglu M,Guccione S

    更新日期：2015-09-18 00:00:00

  • Structure-activity analysis of CJ-15,801 analogues that interact with Plasmodium falciparum pantothenate kinase and inhibit parasite proliferation.

    abstract：:Survival of the human malaria parasite Plasmodium falciparum is dependent on pantothenate (vitamin B5), a precursor of the fundamental enzyme cofactor coenzyme A. CJ-15,801, an enamide analogue of pantothenate isolated from the fungus Seimatosporium sp. CL28611, was previously shown to inhibit P. falciparum proliferat...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.08.050

    authors： Spry C,Sewell AL,Hering Y,Villa MVJ,Weber J,Hobson SJ,Harnor SJ,Gul S,Marquez R,Saliba KJ

    更新日期：2018-01-01 00:00:00

  • Synthesis, molecular modeling and biological evaluation of 2-(benzylthio)-5-aryloxadiazole derivatives as anti-tumor agents.

    abstract：:A series of 2-(benzylthio)-5-aryloxadiazole derivatives have been designed and synthesized, and their biological activities are also evaluated for EGFR inhibitory activity. Fourteen compounds among the twenty compounds are reported for the first time. Their chemical structures are characterized by (1)H NMR, MS, and el...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.11.015

    authors： Liu K,Lu X,Zhang HJ,Sun J,Zhu HL

    更新日期：2012-01-01 00:00:00

  • Synthesis, antiarrhythmic and anticoagulant activities of novel thiazolo derivatives from methyl 2-(thiazol-2-ylcarbamoyl)acetate.

    abstract：:A series of novel thiazolo derivatives were synthesized by initial condensation of methyl 2-(thiazol-2-ylcarbamoyl)acetate with phenyl isothiocyanate and further reactions using different organic reagents. The structures of newly synthesized compounds were confirmed by IR, 1H NMR, EIMS spectral data and elemental anal...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.05.004

    authors： Amr Ael-G,Sabrry NM,Abdalla MM,Abdel-Wahab BF

    更新日期：2009-02-01 00:00:00

  • Novel benzopsoralen analogues: synthesis, biological activity and molecular docking studies.

    abstract：:New benzopsoralen analogues were synthesized and their inhibitory effect on the growth of tumourtumour cell lines (MDA MB231 and TCC-SUP) was evaluated. The in vitro antitumour activity of the new benzopsoralen analogues was discussed in terms of structure-activity relationship. Molecular docking studies with human-CY...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.09.066

    authors： Francisco CS,Rodrigues LR,Cerqueira NM,Oliveira-Campos AM,Esteves AP

    更新日期：2014-11-24 00:00:00

  • Exploration of (S)-3-aminopyrrolidine as a potentially interesting scaffold for discovery of novel Abl and PI3K dual inhibitors.

    abstract：:Based on the literature-reported compensatory effect of PI3K on Abl inhibition and the improved preclinical effect of drug combination of Abl and PI3K inhibitors, a series of compounds bearing novel scaffold of (S)-3-aminopyrrolidine was identified as Abl and PI3K dual inhibitors through support vector machine screeni...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.020

    authors： Zhang C,Tan C,Zu X,Zhai X,Liu F,Chu B,Ma X,Chen Y,Gong P,Jiang Y

    更新日期：2011-04-01 00:00:00

  • Dideoxy fluoro-ketopyranosyl nucleosides as potent antiviral agents: synthesis and biological evaluation of 2,3- and 3,4-dideoxy-3-fluoro-4- and -2-keto-beta-d-glucopyranosyl derivatives of N(4)-benzoyl cytosine.

    abstract：:The synthesis of the dideoxy fluoro ketopyranonucleoside analogues, 1-(2,3-dideoxy-3-fluoro-6-O-trityl-beta-d-glycero-hexopyranosyl-4-ulose)-N(4)-benzoyl cytosine (7a), 1-(3,4-dideoxy-3-fluoro-6-O-trityl-beta-d-glycero-hexopyranosyl-2-ulose)-N(4)-benzoyl cytosine (13a) and their detritylated analogues 8a and 14a, resp...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.01.020

    authors： Manta S,Tsoukala E,Tzioumaki N,Goropevsek A,Pamulapati RT,Cencic A,Balzarini J,Komiotis D

    更新日期：2009-06-01 00:00:00

  • Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.

    abstract：:The synthesis of some novel Ospemifene derived analogs and their evaluation as anti-breast cancer agents against MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) human breast cancer cell lines are described. Few of these analogs for instance, compounds 6, 7 and 8 are shown to be more effective than recent Selective Es...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.08.050

    authors： Kaur G,Mahajan MP,Pandey MK,Singh P,Ramisetti SR,Sharma AK

    更新日期：2014-10-30 00:00:00

  • Novel series of 6-(2-substitutedacetamido)-4-anilinoquinazolines as EGFR-ERK signal transduction inhibitors in MCF-7 breast cancer cells.

    abstract：:Epidermal growth factor receptor (EGFR) signaling pathway has been previously investigated for its significant role in the progression of different types of malignant tumors, where development of small molecules targeting EGFR is well known strategy for design of antitumor agents. Herein, we report the design and synt...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.06.024

    authors： Ismail RSM,Abou-Seri SM,Eldehna WM,Ismail NSM,Elgazwi SM,Ghabbour HA,Ahmed MS,Halaweish FT,Abou El Ella DA

    更新日期：2018-07-15 00:00:00

  • Diverse chemical space of indoleamine-2,3-dioxygenase 1 (Ido1) inhibitors.

    abstract：:Indoleamine-2,3-dioxygenase 1 (IDO1) catalyses the first and rate limiting step of kynurenine pathway accounting for the major contributor of L-Tryptophan degradation. The Kynurenine metabolites are identified as essential cofactors, antagonists, neurotoxins, immunomodulators, antioxidants as well as carcinogens. The ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.113071

    authors： Singh R,Salunke DB

    更新日期：2021-02-05 00:00:00

  • Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines.

    abstract：:With the aim of overcoming gefitinib resistance, a series of novel quinazoline derivatives bearing an adamantyl group on the aniline ring were synthesized as potent epidermal growth factor receptor (EGFR) inhibitors. Most of these analogues are comparable to gefitinib in their ability to inhibit non-small cell lung ca...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.01.045

    authors： Yu H,Li Y,Ge Y,Song Z,Wang C,Huang S,Jin Y,Han X,Zhen Y,Liu K,Zhou Y,Ma X

    更新日期：2016-03-03 00:00:00

  • Synthesis and structure guided evaluation of estrogen agonist and antagonist activities of some new tetrazolyl indole derivatives.

    abstract：:Several regioisomeric tetrazolyl indole derivatives with structurally modified alkyl substituents at the tetracyclic indole nitrogen containing N-ethyl amino tetrazole moiety have been synthesized and screened for their ER binding affinity, agonist (estrogenic), antagonist (antiestrogenic) and anti-implantation activi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.10.035

    authors： Singh US,Shankar R,Yadav GP,Kharkwal G,Dwivedi A,Keshri G,Singh MM,Moulik PR,Hajela K

    更新日期：2008-10-01 00:00:00

  • Cytotoxic-antineoplastic activity of hydroquinone derivatives.

    abstract：:Several myrcenylhydroquinone derivatives have been evaluated for their cytotoxic activity against three neoplastic cell line cultures and compared with the activity previously observed on other neoplastic systems. Also a new series of this type of compounds has been prepared and the compounds synthesised have been eva...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(01)01329-0

    authors： Molinari A,Oliva A,Reinoso P,del Corral JM,Castro MA,Gordaliza M,Gupta MP,Solís P,San Feliciano A

    更新日期：2002-02-01 00:00:00

  • [1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A3 adenosine receptor subtype.

    abstract：:[1,2,4]Triazolo[1,5-c]pyrimidine is a promising platform to develop adenosine receptor antagonists. Here, we tried to investigate the effect of the substituent at the 8 position of [1,2,4]triazolo[1,5-c]pyrimidine derivatives on affinity and selectivity at the human A3 adenosine receptor subtype. In particular, we hav...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.08.042

    authors： Federico S,Margiotta E,Salmaso V,Pastorin G,Kachler S,Klotz KN,Moro S,Spalluto G

    更新日期：2018-09-05 00:00:00

  • Synthesis, evaluation against Leishmania amazonensis and cytotoxicity assays in macrophages of sixteen new congeners Morita-Baylis-Hillman adducts.

    abstract：:We report the design, synthesis, in vitro evaluation against Leishmania amazonensis (IC(50)), cytotoxicity assays in macrophages (CC(50)), and selectivity index (SICC(50)/IC(50)) of sixteen new congeners aromatic Morita-Baylis-Hillman adducts 1-16. The 1-16 were prepared in good to excellent yields (58%-97%) from the ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.06.036

    authors： Silva FP,de Assis PA,Junior CG,de Andrade NG,da Cunha SM,Oliveira MR,Vasconcellos ML

    更新日期：2011-09-01 00:00:00

  • Phenylpropiophenone derivatives as potential anticancer agents: synthesis, biological evaluation and quantitative structure-activity relationship study.

    abstract：:Series of twelve chalcone and propafenone derivatives has been synthesized and evaluated for anticancer activities against HeLa, Fem-X, PC-3, MCF-7, LS174 and K562 cell lines. The 2D-QSAR and 3D-QSAR studies were performed for all compounds with cytotoxic activities against each cancer cell line. Partial least squares...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.02.013

    authors： Ivković BM,Nikolic K,Ilić BB,Žižak ŽS,Novaković RB,Čudina OA,Vladimirov SM

    更新日期：2013-05-01 00:00:00

  • β-Ionone and its analogs as promising anticancer agents.

    abstract：:β-Ionone is an end-ring analog of β-carotenoids which widely distributed in fruit and vegetables. Recent studies have demonstrated anti-proliferative, anti-metastatic and apoptosis induction properties of β-ionone in vitro and in vivo. Also, the studies have focused on investigating the β-ionone action on different ty...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2016.07.037

    authors： Ansari M,Emami S

    更新日期：2016-11-10 00:00:00

  • Design, synthesis and antiviral activity of novel quinazolinones.

    abstract：:HIV-1 integrase (IN) is a validated therapeutic target for antiviral drug design. However, the emergence of viral strains resistant to clinically studied IN inhibitors demands the discovery of novel inhibitors that are structurally as well as mechanistically different. Herein, a series of quinazolinones were designed ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.04.010

    authors： Wang Z,Wang M,Yao X,Li Y,Tan J,Wang L,Qiao W,Geng Y,Liu Y,Wang Q

    更新日期：2012-07-01 00:00:00

  • Potent naphthoquinones against antimony-sensitive and -resistant Leishmania parasites: synthesis of novel α- and nor-α-lapachone-based 1,2,3-triazoles by copper-catalyzed azide-alkyne cycloaddition.

    abstract：:Continuing our screening program for novel anti-parasite compounds, we synthesized seven 1,4-naphthoquinones coupled to 1,2,3-triazoles, five nor-β-lapachone-based 1,2,3-triazoles and ten α-lapachone-based 1,2,3-triazoles. These and other naphthoquinonoid compounds were evaluated for their activity against promastigot...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.02.038

    authors： Guimarães TT,Pinto Mdo C,Lanza JS,Melo MN,do Monte-Neto RL,de Melo IM,Diogo EB,Ferreira VF,Camara CA,Valença WO,de Oliveira RN,Frézard F,da Silva EN Jr

    更新日期：2013-05-01 00:00:00

  • Structural variations of piritrexim, a lipophilic inhibitor of human dihydrofolate reductase: synthesis, antitumor activity and molecular modeling investigations.

    abstract：:Piritrexim (PTX) (1), a lipophilic inhibitor of the human dihydrofolate reductase, has been evaluated as an anticancer agent. The synthesis of four structural variations (2-5) of PTX is reported. The PTX analogues 2-5 were obtained by reaction of suitable C3-building blocks with pyrimidine-2,4,6-triamine (14) or with ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2004.09.001

    authors： Zink M,Lanig H,Troschütz R

    更新日期：2004-12-01 00:00:00