当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis, molecular docking and biological evaluation of novel phthaloyl derivatives of 3-amino-3-aryl propionic acids as inhibitors of Trypanosoma cruzi trans-sialidase.

Synthesis, molecular docking and biological evaluation of novel phthaloyl derivatives of 3-amino-3-aryl propionic acids as inhibitors of Trypanosoma cruzi trans-sialidase.

Abstract：

:In the last two decades, trans-sialidase of Trypanosoma cruzi (TcTS) has been an important pharmacological target for developing new anti-Chagas agents. In a continuous effort to discover new potential TcTS inhibitors, 3-amino-3-arylpropionic acid derivatives (series A) and novel phthaloyl derivatives (series B, C and D) were synthesized and molecular docking, TcTS enzyme inhibition and determination of trypanocidal activity were carried out. From four series obtained, compound D-11 had the highest binding affinity value (-11.1 kcal/mol) compared to reference DANA (-7.8 kcal/mol), a natural ligand for TS enzyme. Furthermore, the 3D and 2D interactions analysis of compound D-11 showed a hydrogen bond, π-π stacking, π-anion, hydrophobic and Van der Waals forces with all important amino acid residues (Arg35, Arg245, Arg314, Tyr119, Trp312, Tyr342, Glu230 and Asp59) on the active site of TcTS. Additionally, D-11 showed the highest TcTS enzyme inhibition (86.9% ± 5) by high-performance ion exchange chromatography (HPAEC). Finally, D-11 showed better trypanocidal activity than the reference drugs nifurtimox and benznidazole with an equal % lysis (63 ± 4 and 65 ± 2 at 10 μg/mL) and LC50 value (52.70 ± 2.70 μM and 46.19 ± 2.36 μM) on NINOA and INC-5 strains, respectively. Therefore, D-11 is a small-molecule with potent TcTS inhibition and a strong trypanocidal effect that could help in the development of new anti-Chagas agents.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Kashif M,Chacón-Vargas KF,López-Cedillo JC,Nogueda-Torres B,Paz-González AD,Ramírez-Moreno E,Agusti R,Uhrig ML,Reyes-Arellano A,Peralta-Cruz J,Ashfaq M,Rivera G

doi

10.1016/j.ejmech.2018.07.005

subject

Has Abstract

pub_date

2018-08-05 00:00:00

pages

252-268

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)30561-0

journal_volume

156

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • New amphiphilic neamine conjugates bearing a metal binding motif active against MDR E. aerogenes Gram-negative bacteria.

    abstract：:Structure of bacterial envelope is one of the major factors contributing to Gram negative bacterial resistance. To develop new agents that target the bacterial membranes, we synthesized, by analogy with our previous peptide conjugates, new amphiphilic 3',4',6-trinaphthylmethylene neamines functionalized at position 5 ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.10.054

    authors： Allam A,Maigre L,Alves de Sousa R,Dumont E,Vergalli J,Pagès JM,Artaud I

    更新日期：2017-02-15 00:00:00

  • Synthesis and antimicrobial activities of a new series of 4-S-[4(1)-amino-5(1)-oxo-6(1)-substituted benzyl-4(1),5(1)-dihydro-1(1),2(1),4(1)-triazin-3-yl]mercaptoacetyl-3-arylsydnones.

    abstract：:The synthesis of some 4-S-(4(1)-amino-5(1)-oxo-6(1)-substituted benzyl-4(1),5(1)-dihydro-1(1),2(1),4(1)-triazin-3-yl)mercaptoacetyl-3-arylsydnones by the reaction of 3-aryl-4-bromoacetylsydnones with 6-substituted-4-amino-3-mercapto-1,2,4-triazin-5-ones is described. The IR, (1)H NMR, mass spectra and elemental analys...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.02.003

    authors： Hegde JC,Girisha KS,Adhikari A,Kalluraya B

    更新日期：2008-12-01 00:00:00

  • Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases.

    abstract：:In this work we describe a new family of dibenzo[1,4,5]thiadiazepines (2-12) that showed an interesting in vitro biological profile, namely neuroprotective and antioxidant properties, as well as blockade of cytosolic calcium entry. They showed no cytotoxic effects and the majority were predicted as CNS-permeable compo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.04.075

    authors： González-Muñoz GC,Arce MP,Pérez C,Romero A,Villarroya M,López MG,Conde S,Rodríguez-Franco MI

    更新日期：2014-06-23 00:00:00

  • Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.

    abstract：:Structure-based drug design was utilized to develop novel, 1-hydroxy-2-naphthoate-based small-molecule inhibitors of Mcl-1. Ligand design was driven by exploiting a salt bridge with R263 and interactions with the p2 pocket of the protein. Significantly, target molecules were accessed in just two synthetic steps, sugge...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.02.006

    authors： Lanning ME,Yu W,Yap JL,Chauhan J,Chen L,Whiting E,Pidugu LS,Atkinson T,Bailey H,Li W,Roth BM,Hynicka L,Chesko K,Toth EA,Shapiro P,MacKerell AD Jr,Wilder PT,Fletcher S

    更新日期：2016-05-04 00:00:00

  • African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase.

    abstract：:African trypanosomiasis is a parasitic disease affecting 5000 humans and millions of livestock animals in sub-Saharan Africa every year. Current treatments are limited, difficult to administer and often toxic causing long term injury or death in many patients. Trypanosome alternative oxidase is a parasite specific enz...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.09.067

    authors： West RA,O'Doherty OG,Askwith T,Atack J,Beswick P,Laverick J,Paradowski M,Pennicott LE,Rao SPS,Williams G,Ward SE

    更新日期：2017-12-01 00:00:00

  • Synthesis and in vitro Trichomonacidal activities of some new dialkylperoxides and 1,2,4-trioxanes.

    abstract：:Two series of three trioxanes and 18 disubstituted peroxides were synthesised and evaluated for their in vitro trichomonacidal activity against Trichomonas vaginalis. The most active compound, 2-methylprop-2-yl 2-methoxyeth-1-yl peroxide exhibited an IC(50) value of 1.0+/-0.2 microM whereas other dialkyl peroxides had...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(01)01278-8

    authors： Camuzat-Dedenis B,Provot O,Cointeaux L,Peyrou V,Berrien JF,Bories C,Loiseau PM,Mayrargue J

    更新日期：2001-10-01 00:00:00

  • New and efficient approach for synthesis of novel bioactive [1,3,4]thiadiazoles incorporated with 1,3-thiazole moiety.

    abstract：:A series of novel 1,3,4-thiadiazoles incorporated with thiazole moiety was synthesized by reaction of 5-acetyl-2-benzoylimino-3-phenyl-1,3,4-thiadiazole thiosemicarbazone 2 with each of N-phenyl 2-oxo-propanehydrazonoyl chloride 3 and ethyl (N-aryl-hydrazono) chloroacetate 5 in dioxane in basic medium. Also, another s...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.05.009

    authors： Farghaly TA,Abdallah MA,Masaret GS,Muhammad ZA

    更新日期：2015-06-05 00:00:00

  • Structure-activity relationship studies of acridones as potential antipsoriatic agents. 2. Synthesis and antiproliferative activity of 10-substituted hydroxy-10H-acridin-9-ones against human keratinocyte growth.

    abstract：:A series of 10-substituted hydroxy-10H-acridin-9-ones were synthesized and studied as potential antipsoriatic agents. The antiproliferative activity of the novel derivatives, which can be considered as aza-analogues of the antipsoriatic drug anthralin, was determined using the human keratinocyte cell line HaCaT. Struc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.08.059

    authors： Putic A,Stecher L,Prinz H,Müller K

    更新日期：2010-11-01 00:00:00

  • Rhodium(II) acetate-catalyzed stereoselective synthesis, SAR and anti-HIV activity of novel oxindoles bearing cyclopropane ring.

    abstract：:Novel oxindole derivatives bearing substituted cyclopropane ring have been designed on the basis of docking studies with HIV-1 RT using the software DS 2.5 and synthesized as probable NNRTIs against HIV-1 using rhodium(II) acetate-catalyzed stereoselective cyclopropanation reaction. The cyclopropane isomer, having tra...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.037

    authors： Kumari G,Nutan,Modi M,Gupta SK,Singh RK

    更新日期：2011-04-01 00:00:00

  • Homology modeling in tandem with 3D-QSAR analyses: a computational approach to depict the agonist binding site of the human CB2 receptor.

    abstract：:CB2 receptor belongs to the large family of G-protein coupled receptors (GPCRs) controlling a wide variety of signal transduction. The recent crystallographic determination of human β2 adrenoreceptor and its high sequence similarity with human CB2 receptor (hCB2) prompted us to compute a theoretical model of hCB2 base...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.07.023

    authors： Cichero E,Ligresti A,Allarà M,di Marzo V,Lazzati Z,D'Ursi P,Marabotti A,Milanesi L,Spallarossa A,Ranise A,Fossa P

    更新日期：2011-09-01 00:00:00

  • Explorations into modeling human oral bioavailability.

    abstract：:Explorations into modeling human oral bioavailability started with a whole dataset of 772 drug compounds. First, training set and test set were chosen based on Kohonen's self-organizing Neural Network (KohNN). Then, a quantitative model of the whole dataset was built using multiple linear regression (MLR) analysis. Th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.05.017

    authors： Wang Z,Yan A,Yuan Q,Gasteiger J

    更新日期：2008-11-01 00:00:00

  • Antifungal peptides at membrane interaction.

    abstract：:Many drugs are available for the treatment of systemic or superficial mycoses, but only a limited number of them are effective antifungal drugs, devoid of toxic and undesirable side effects. Furthermore, resistance development and fungistatic rather than fungicidal activities represent limitations of current antifunga...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.02.037

    authors： Di Marino S,Scrima M,Grimaldi M,D'Errico G,Vitiello G,Sanguinetti M,De Rosa M,Soriente A,Novellino E,D'Ursi AM

    更新日期：2012-05-01 00:00:00

  • α- and β-hydrazino acid-based pseudopeptides inhibit the chymotrypsin-like activity of the eukaryotic 20S proteasome.

    abstract：:We describe the synthesis of a library of new pseudopeptides and their inhibitory activity of the rabbit 20S proteasome chymotrypsin-like (ChT-L) activity. We replaced a natural α-amino acid by an α- or a β-hydrazino acid and obtained inhibitors of proteasome up to a submicromolar range (0.7 μM for molecule 24b). Stru...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.09.059

    authors： Bordessa A,Keita M,Maréchal X,Formicola L,Lagarde N,Rodrigo J,Bernadat G,Bauvais C,Soulier JL,Dufau L,Milcent T,Crousse B,Reboud-Ravaux M,Ongeri S

    更新日期：2013-01-01 00:00:00

  • Quinazoline derivatives as selective CYP1B1 inhibitors.

    abstract：:CYP1B1 is implicated to have a role in the development of breast, ovarian, renal, skin and lung carcinomas. It has been suggested that identification of potent and specific CYP1B1 inhibitors can lead to a novel treatment of cancer. Flavonoids have a compact rigid skeleton which fit precisely within the binding cavity ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.02.032

    authors： Mohd Siddique MU,McCann GJ,Sonawane VR,Horley N,Gatchie L,Joshi P,Bharate SB,Jayaprakash V,Sinha BN,Chaudhuri B

    更新日期：2017-04-21 00:00:00

  • Synthesis and evaluation of novel hybrids β-carboline-4-thiazolidinones as potential antitumor and antiviral agents.

    abstract：:A series of novel hybrids β-carboline-4-thiazolidinones were synthesized and evaluated for their in vitro antitumor activity against human cancer cell lines and for antiviral activity towards Herpes simplex virus type-1 (HSV-1). From the N'-(2-ylidene-4-thiazolidinone)-β-carboline-3-carbohydrazide series (9-11), compo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.10.018

    authors： Barbosa VA,Baréa P,Mazia RS,Ueda-Nakamura T,Costa WFD,Foglio MA,Goes Ruiz ALT,Carvalho JE,Vendramini-Costa DB,Nakamura CV,Sarragiotto MH

    更新日期：2016-11-29 00:00:00

  • Condensed 1,4-dihydropyridines with various esters and their calcium channel antagonist activities.

    abstract：:New alkyl 2,6,6-(2,7,7)-trimethyl-4-(2-fluoro-3-chloro-5-trifluoromethylphenyl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylates and 9-(3-chloro-2-fluoro-5-trifluoromethylphenyl)-6,6(7,7)-dimethyl-6,7-dihydrofuro[3,4-b]quinoline-1,8-diones have been synthesised and their calcium antagonistic activities on isolated ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.10.008

    authors： Bülbül B,Oztürk GS,Vural M,Simşek R,Sarioğlu Y,Linden A,Ulgen M,Safak C

    更新日期：2009-05-01 00:00:00

  • Discovery of new potent hits against intracellular Trypanosoma cruzi by QSAR-based virtual screening.

    abstract：:Chagas disease is a neglected tropical disease (NTD) caused by the protozoan parasite Trypanosoma cruzi and is primarily transmitted to humans by the feces of infected Triatominae insects during their blood meal. The disease affects 6-8 million people, mostly in Latin America countries, and kills more people in the re...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.11.062

    authors： Melo-Filho CC,Braga RC,Muratov EN,Franco CH,Moraes CB,Freitas-Junior LH,Andrade CH

    更新日期：2019-02-01 00:00:00

  • Synthesis of sulfamoylbenzamide derivatives as HBV capsid assembly effector.

    abstract：:The synthesis of novel series of sulfamoylbenzamides as HBV capsid assembly effector is reported. The structure was divided into five parts which were independently modified as part of our lead optimization. All synthesized compounds were evaluated for their anti-HBV activity and toxicity in human hepatocytes, lymphoc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.06.062

    authors： Sari O,Boucle S,Cox BD,Ozturk T,Russell OO,Bassit L,Amblard F,Schinazi RF

    更新日期：2017-09-29 00:00:00

  • New transition metal ion complexes with benzimidazole-5-carboxylic acid hydrazides with antitumor activity.

    abstract：:Metal complexes of 2-methyl-1H-benzimidazole-5-carboxylic acid hydrazide (4a; L(1)) and its Schiff base 2-methyl-N-(propan-2-ylidene)-1H-benzimidazole-5-carbohydrazide (5a; L(2)) with transition metal ions e.g., copper, silver, nickel, iron and manganese were prepared. The complexes formed were 1:1 or 1:2 M:L complexe...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.07.013

    authors： Galal SA,Hegab KH,Kassab AS,Rodriguez ML,Kerwin SM,el-Khamry AM,el-Diwani HI

    更新日期：2009-04-01 00:00:00

  • Synthesis, characterization, molecular docking and in vitro antimalarial properties of new carboxamides bearing sulphonamide.

    abstract：:Sulphonamides and carboxamides have shown large number of pharmacological properties against different types of diseases among which is malaria. Twenty four new carboxamide derivatives bearing benzenesulphonamoyl alkanamides were synthesized and investigated for their in silico and in vitro antimalarial and antioxidan...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.04.029

    authors： Ugwu DI,Okoro UC,Ukoha PO,Okafor S,Ibezim A,Kumar NM

    更新日期：2017-07-28 00:00:00

  • Potential cytotoxic and anti-metastatic effects of berberine on gynaecological cancers with drug-associated resistance.

    abstract：:Gynaecological disorders, such as cervical, ovarian, and endometrial cancers are the second most prevalent cancer types in women worldwide. Therapeutic approaches for gynaecological cancers involve chemotherapy, radiation, and surgery. However, lifespan is not improved, and novel medications are required. Among variou...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2019.111951

    authors： Mortazavi H,Nikfar B,Esmaeili SA,Rafieenia F,Saburi E,Chaichian S,Heidari Gorji MA,Momtazi-Borojeni AA

    更新日期：2020-02-01 00:00:00

  • Organotin complexes containing carboxylate ligands with maleimide and naphthalimide derived partial structures: TrxR inhibition, cytotoxicity and activity in resistant cancer cells.

    abstract：:Di-n-butyltin(IV) carboxylate and tri-n-butyltin(IV) carboxylate derivatives have demonstrated strong cytotoxic effects in different types of tumor cells. Complexes with carboxylate ligands that contain maleimide and naphthalimide derived partial structures were synthesized, characterized and investigated for inhibiti...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.09.075

    authors： Navakoski de Oliveira K,Andermark V,Onambele LA,Dahl G,Prokop A,Ott I

    更新日期：2014-11-24 00:00:00

  • Wake-promoting agents: search for next generation modafinil: part IV.

    abstract：:In search of a next generation molecule to the novel wake promoting agent modafinil, a series of diphenyl ether derived wakefulness enhancing agents (in rat) was developed. From this work, racemic compound 16 was separated into its chiral enantiomers to profile them individually. ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.05.038

    authors： Louvet P,Schweizer D,Gourdel ME,Riguet E,Yue C,Marcy VR,Lin YG,Gruner J,Lesur B,Bacon ER,Chatterjee S

    更新日期：2012-08-01 00:00:00

  • Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity.

    abstract：:A small library of coumarins, carrying butynyl-amino chains, was synthesized continuing our studies in the field of MDR reverting ageEnts and in order to obtain multipotent agents to combat malignancies. In particular, the reported anticancer and chemopreventive natural product 7-isopentenyloxycoumarin was linked to d...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.01.020

    authors： Bisi A,Cappadone C,Rampa A,Farruggia G,Sargenti A,Belluti F,Di Martino RMC,Malucelli E,Meluzzi A,Iotti S,Gobbi S

    更新日期：2017-02-15 00:00:00

  • Recent methodologies toward the synthesis of valdecoxib: a potential 3,4-diarylisoxazolyl COX-II inhibitor.

    abstract：:Non-steroidal anti-inflammatory drugs are widely used therapeutic agents in the treatment of inflammation, pain and fever. Cyclooxygenase catalyzes the initial step of biotransformation of arachidonic acid to prostanoids, and exist as three distinct isozymes; COX-I, COX-II and COX-III. Selective COX-II inhibitors are ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2010.07.045

    authors： Dadiboyena S,Nefzi A

    更新日期：2010-11-01 00:00:00

  • Synthesis and antitumor activities of naturally occurring oleanolic acid triterpenoid saponins and their derivatives.

    abstract：:Twenty-six naturally occurring oleanolic acid saponins and their derivatives, 16 of which were synthesized in this study, were preliminarily evaluated against human cancer cells. From SAR studies, the presence of α-l-rhamnosyl residue at the terminal of both C-3 and C-28 position for oleanolic acid bidesmosides was im...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.04.016

    authors： Liu Q,Liu H,Zhang L,Guo T,Wang P,Geng M,Li Y

    更新日期：2013-06-01 00:00:00

  • Tetracyclic indolines as a novel class of β-lactam-selective resistance-modifying agent for MRSA.

    abstract：:Antibiotic-resistant bacterial infections have seen a marked increase in recent years, while antibiotic discovery has waned. Resistance-modifying agents (RMA) offer an intriguing alternative strategy to fight against resistant bacteria. Here we report the discovery, antibiotic profiling, and structure-activity relatio...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.09.034

    authors： Zhu Y,Cleaver L,Wang W,Podoll JD,Walls S,Jolly A,Wang X

    更新日期：2017-01-05 00:00:00

  • Chalcones: Unearthing their therapeutic possibility as monoamine oxidase B inhibitors.

    abstract：:In the last years the continuous efforts in the development of novel and effective inhibitors of human monoamine oxidases (hMAOs) promoted the discovery of new agents able to effectively and selectively bound one of the two isoforms (hMAO-A and hMAO-B). However, the parent chalcone scaffold still covers an important r...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112650

    authors： Guglielmi P,Mathew B,Secci D,Carradori S

    更新日期：2020-11-01 00:00:00

  • Ni(II) curcumin complexes for cellular imaging and photo-triggered in vitro anticancer activity.

    abstract：:Nickel(II) complexes [Ni(cur)(L)2](OAc) (1-3) where L is N,N-donor heterocyclic bases namely 1,10-phenanthroline (phen in 1), dipyrido[3,2-d:2',3'-f]quinoxaline (dpq in 2), dipyrido[3,2-a:2',3'-c]phenazine (dppz in 3) and Hcur is curcumin were prepared, fully characterized and light-induced in vitro anticancer activit...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112632

    authors： Banaspati A,Raza MK,Goswami TK

    更新日期：2020-10-15 00:00:00

  • New 5-substituted thiazolo[3,2-b][1,2,4]triazol-6-ones: synthesis and anticancer evaluation.

    abstract：:Following [2+3]-cyclocondensation reaction of 1,2,4-triazole-3(5)-thiol with N-arylmaleimides or with monochloroacetic acid and oxocompounds, N-(R-phenyl)-(6-oxo-5,6-dihydro[1,3]thiazol[3,2-b][1,2,4]triazol-5-yl)acetamides (1-5) and 5-ylidene-[1,3]thiazolo[3,2-b][1,2,4]triazol-6-ones (6-11) were synthesized as possibl...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.12.006

    authors： Lesyk R,Vladzimirska O,Holota S,Zaprutko L,Gzella A

    更新日期：2007-05-01 00:00:00