当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and anticancer evaluation of some new hydrazone derivatives of 2,6-dimethylimidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazide.

Synthesis and anticancer evaluation of some new hydrazone derivatives of 2,6-dimethylimidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazide.

Abstract：

:In this study, some novel 2,6-dimethyl-N'-substituted phenylmethylene-imidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazides (3a-3h) were synthesized from 2,6-dimethylimidazo-[2,1-b][1,3,4]thiadiazole-5-carbohydrazide (2). The newly synthesized compounds (3a-3h) were evaluated in the National Cancer Institute's 3-cell line, one dose in vitro primary cytotoxicity assay. Compounds 3c and 3h which passed the criteria for activity in this assay (20-29% growth percentages) were scheduled automatically for evaluation against the full panel of 60 human tumor cell lines at a minimum of five concentrations at 10-fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. 2,6-Dimethyl-N'-(2-hydroxyphenylmethylidene)imidazo[2,1-b][1,3,4]thiadiazole-5-carbohydrazide (3c) showed the most favorable cytotoxicity. This compound demonstrated the most marked effects in the National Cancer Institute's 60 human tumor cell line in vitro screen on an ovarian cancer cell line (OVCAR log(10)GI(50) value -5.51).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Terzioglu N,Gürsoy A

doi

10.1016/s0223-5234(03)00138-7

subject

Has Abstract

pub_date

2003-07-01 00:00:00

pages

781-6

issue

7-8

eissn

0223-5234

issn

1768-3254

pii

S0223523403001387

journal_volume

38

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • A molecular model for cocaine binding by the immunotherapeutic human/mouse chimeric monoclonal antibody 2E2.

    abstract：:Immunotherapy by cocaine-binding monoclonal antibodies (mAbs) has emerged as a promising strategy for the treatment of cocaine addiction. The human (gamma1 heavy chain)/murine (lambda light chain) chimeric mAb 2E2 has excellent affinity and specificity for cocaine and recent animal studies have demonstrated 2E2's abil...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.02.004

    authors： Lape M,Paula S,Ball WJ Jr

    更新日期：2010-06-01 00:00:00

  • Recent advances in small molecule based cancer immunotherapy.

    abstract：:Immunotherapy has been increasingly utilized for the treatment of cancer. Currently available cancer immunotherapies mainly involve the use of antibodies, which have advantages in terms of pharmacodynamics such as efficacy and specificity, however, they exhibit disadvantages in regard to the pharmacokinetics including...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2018.08.028

    authors： Cheng B,Yuan WE,Su J,Liu Y,Chen J

    更新日期：2018-09-05 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

  • Design, synthesis and biological evaluation of novel 2-(5-aryl-1H-imidazol-1-yl) derivatives as potential inhibitors of the HIV-1 Vpu and host BST-2 protein interaction.

    abstract：:Novel ethyl 2-(5-aryl-1H-imidazol-1-yl)-acetates 17 and propionates 18, together with their acetic acid 19 and acetohydrazide 20 derivatives, were designed and synthesized using TosMIC chemistry. Biological evaluation of these newly synthesized scaffolds in the HIV-1 Vpu- Host BST-2 ELISA assay identified seven hits (...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112111

    authors： Rashamuse TJ,Njengele Z,Coyanis EM,Sayed Y,Mosebi S,Bode ML

    更新日期：2020-03-15 00:00:00

  • Development of novel theranostic agents for in vivo amyloid imaging and protective effects on human neuroblastoma cells.

    abstract：:Brain amyloid deposits have been identified as the main neuropathological hallmarks of Alzheimer's diseases (AD) and intensive efforts have been devoted to develop aggregation inhibitors preventing the formation of toxic oligomeric Aβ for therapeutic. In addition, evidence indicates that the formation and accumulation...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111585

    authors： Li Y,Yan L,Cai J,Zhang W,Li L,Du Z,Dong C,Meunier B,Chen H

    更新日期：2019-11-01 00:00:00

  • Cardanol-derived AChE inhibitors: Towards the development of dual binding derivatives for Alzheimer's disease.

    abstract：:Cardanol is a phenolic lipid component of cashew nut shell liquid (CNSL), obtained as the byproduct of cashew nut food processing. Being a waste product, it has attracted much attention as a precursor for the production of high-value chemicals, including drugs. On the basis of these findings and in connection with our...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.12.024

    authors： Lemes LFN,de Andrade Ramos G,de Oliveira AS,da Silva FMR,de Castro Couto G,da Silva Boni M,Guimarães MJR,Souza INO,Bartolini M,Andrisano V,do Nascimento Nogueira PC,Silveira ER,Brand GD,Soukup O,Korábečný J,Romeiro NC,Cas

    更新日期：2016-01-27 00:00:00

  • Synthesis of some new pyrimido[2',1':2,3]thiazolo[4,5-b]quinoxaline derivatives as anti-inflammatory and analgesic agents.

    abstract：:Treatment of 6-aminothiouracil (1) with 2,3-dichloroquinoxaline (2) in ethanol/TEA afforded 6-amino-2-(3-chloroquinoxalin-2-ylthio)pyrimidin-4(3H)-one (3), which was refluxed in DMF to give 2-aminopyrimido[2',1':2,3]thiazolo[4,5-b]quinoxaline-4-one (4). Compound 4 was utilized as a key intermediate for the synthesis o...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.01.042

    authors： Abu-Hashem AA,Gouda MA,Badria FA

    更新日期：2010-05-01 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

  • Database mining applied to central nervous system (CNS) activity.

    abstract：:A data set of 389 compounds, active in the central nervous system (CNS) and divided into eight classes according to the receptor type, was extracted from the RBI database and analyzed by Self-Organizing Maps (SOM), also known as Kohonen Artificial Neural Networks. This method gives a 2D representation of the distribut...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(01)01233-8

    authors： Pintore M,Taboureau O,Ros F,Chrétien JR

    更新日期：2001-04-01 00:00:00

  • Thioether-based 2-aminobenzamide derivatives: Novel HDAC inhibitors with potent in vitro and in vivo antitumor activity.

    abstract：:Previously, we focused on a series of 2-aminobenzamide-based histone deacetylase (HDAC) inhibitors, compound 9 of which displayed potent HDAC inhibitory activity against HDAC1 and HDAC2, and moderate anti-proliferative activity against several cancer cell lines. In the current study, we have designed and synthesized a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.05.007

    authors： Yun F,Cheng C,Ullah S,He J,Zahi MR,Yuan Q

    更新日期：2019-08-15 00:00:00

  • Conjugation of substituted ferrocenyl to thiadiazine as apoptosis-inducing agents targeting the Bax/Bcl-2 pathway.

    abstract：:Ferrocene compounds are a class of biologically active compounds that has antitumour and antifungal properties. This study investigated the induction of apoptosis in human fibrosarcoma cells (HT1080) after treatment with a series of 6-ferrocenyl-3-subsituted7H-1,2,4-triazolo[3,4-b]- 1,3,4-thiadiazine (FTFs). We found ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.08.007

    authors： Miao R,Wei J,Lv M,Cai Y,Du Y,Hui X,Wang Q

    更新日期：2011-10-01 00:00:00

  • Design and synthesis of novel quinacrine-[1,3]-thiazinan-4-one hybrids for their anti-breast cancer activity.

    abstract：:In an attempt to develop effective and safe anticancer agents, we designed, synthesized and examined 23 novel quinacrine (QC) derivatives by combining the 9-aminoacridine scaffold and the [1,3]thiazinan-4-ones group. Most of these hybrids showed strong anticancer activities, among which 3-(3-(6-chloro-2-methoxyacridin...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.097

    authors： Solomon VR,Pundir S,Le HT,Lee H

    更新日期：2018-01-01 00:00:00

  • Synthesis and biological evaluation of novel C-indolylxylosides as sodium-dependent glucose co-transporter 2 inhibitors.

    abstract：:Sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors are the current focus on the indication for the management of hyperglycemia in diabetes. Here, a novel series of C-linked indolylxyloside-based inhibitors of SGLT2 has been discovered. Structure-activity relationship studies revealed that substituents at the...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.06.053

    authors： Yao CH,Song JS,Chen CT,Yeh TK,Hsieh TC,Wu SH,Huang CY,Huang YL,Wang MH,Liu YW,Tsai CH,Kumar CR,Lee JC

    更新日期：2012-09-01 00:00:00

  • Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.

    abstract：:Novel diarylpyrimidines (DAPY), which represent next generation of non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus type I (HIV-1) assessed. Modulations at positions 2 and 6 of the left phenyl ring generated interesting derivatives of ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.11.014

    authors： Mordant C,Schmitt B,Pasquier E,Demestre C,Queguiner L,Masungi C,Peeters A,Smeulders L,Bettens E,Hertogs K,Heeres J,Lewi P,Guillemont J

    更新日期：2007-05-01 00:00:00

  • Design, synthesis and biological evaluation of piperazinyl-β-carbolinederivatives as anti-leishmanial agents.

    abstract：:Molecular hybridization is a ligand based drug design approach is well known recent medicinal chemistry to design anti-parasitic agents. In the present study, we have designed a series of (1-phenyl-9H-pyrido [3,4-b]indol-3-yl) (4-phenylpiperazin-1-yl)methanone derivatives using molecular hybridization approach. Design...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.03.022

    authors： Ashok P,Chander S,Smith TK,Sankaranarayanan M

    更新日期：2018-04-25 00:00:00

  • Synthesis, antibacterial evaluation and QSAR studies of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolone derivatives.

    abstract：:A series of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolones (I-XXI) were synthesized using an appropriate synthetic route and characterized by elemental and spectral analysis. The antibacterial activities of all the synthesized compounds were evaluated against identifiable bacterial strains. Compounds III, ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.04.035

    authors： Kumar R,Kumar A,Jain S,Kaushik D

    更新日期：2011-09-01 00:00:00

  • Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.

    abstract：:Because of the increasing number of immunocompromised patients and due to problems with antifungal treatment, especially with the most widely used antifungals, azoles, there is an urgent need for new, potent and safe antifungals with fewer cytochrome P450 (CYP)-mediated interactions with other drugs. In the present st...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.10.053

    authors： Tani N,Rahnasto-Rilla M,Wittekindt C,Salminen KA,Ritvanen A,Ollakka R,Koskiranta J,Raunio H,Juvonen RO

    更新日期：2012-01-01 00:00:00

  • Discovery of caffeic acid phenethyl ester derivatives as novel myeloid differentiation protein 2 inhibitors for treatment of acute lung injury.

    abstract：:Myeloid differentiation protein 2 (MD2) is an essential molecule which recognizes lipopolysaccharide (LPS), leading to initiation of inflammation through the activation of Toll-like receptor 4 (TLR4) signaling. Caffeic acid phenethyl ester (CAPE) from propolis of honeybee hives could interfere interactions between LPS...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.11.066

    authors： Chen L,Jin Y,Chen H,Sun C,Fu W,Zheng L,Lu M,Chen P,Chen G,Zhang Y,Liu Z,Wang Y,Song Z,Liang G

    更新日期：2018-01-01 00:00:00

  • Combating breast cancer with non-steroidal aromatase inhibitors (NSAIs): Understanding the chemico-biological interactions through comparative SAR/QSAR study.

    abstract：:It is a challenging task to design target-specific and less toxic non-steroidal aromatase inhibitors (NSAIs) though the modeling studies for designing anti-aromatase molecules have been continuing for more than two decades to fight the dreaded estrogen-dependent breast cancer. In this article, different validated QSAR...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.05.041

    authors： Adhikari N,Amin SA,Saha A,Jha T

    更新日期：2017-09-08 00:00:00

  • Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype.

    abstract：:We report the design, synthesis and pharmacological screening of a group of analogues of anabaseine 2, a naturally occurring unselective nicotinic agonist. The novel nAChR ligands 5-15 were planned following a molecular modeling analysis which suggested the replacement of the pyridine ring of 2 with a 3-substituted be...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.11.045

    authors： Matera C,Quadri M,Sciaccaluga M,Pomè DY,Fasoli F,De Amici M,Fucile S,Gotti C,Dallanoce C,Grazioso G

    更新日期：2016-01-27 00:00:00

  • NSAIDs revisited: putative molecular basis of their interactions with peroxisome proliferator-activated gamma receptor (PPARgamma).

    abstract：:This paper describes molecular docking studies of a series of classical NSAIDs with PPARgamma receptor, which has been pointed as a new target for the design of anti-cancer and anti-inflammatory drugs, and has been found to be responsible for some of the already established pharmacological effects observed for markete...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.11.031

    authors： Romeiro NC,Sant'Anna CM,Lima LM,Fraga CA,Barreiro EJ

    更新日期：2008-09-01 00:00:00

  • 1,8-Naphthyridines IV. 9-substituted N,N-dialkyl-5-(alkylamino or cycloalkylamino) [1,2,4]triazolo[4,3-a][1, 8]naphthyridine-6-carboxamides, new compounds with anti-aggressive and potent anti-inflammatory activities.

    abstract：:The title compounds (8) were synthesized through the cyclocondensation of the corresponding N-substituted 4-amino-2-chloro-1,8-naphthyridine-3-carboxamides (4) with the proper hydrazides, in order to evaluate their anti-inflammatory and anti-aggressive properties. Several compounds 8 exhibited high anti-inflammatory a...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)01175-2

    authors： Roma G,Di Braccio M,Grossi G,Mattioli F,Ghia M

    更新日期：2000-11-01 00:00:00

  • Bismuth heterocycles based on a diphenyl sulfone scaffold: synthesis and substituent effect on the antifungal activity against Saccharomyces cerevisiae.

    abstract：:A series of heterocyclic organobismuth(III) compounds 2 [ClBi(5-R-C6H(3)-2-SO2C6H(4)-1'-): R=Me, Ph, MeO, Cl, H, t-Bu, CF3, F, Me2N] was synthesized in order to study the relative importance of structure and specific substitutions in relation to their lipophilicity and antifungal activity against the yeast Saccharomyc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.11.031

    authors： Murafuji T,Fujiwara Y,Yoshimatsu D,Miyakawa I,Migita K,Mikata Y

    更新日期：2011-02-01 00:00:00

  • Synthesis of novel cinnamanilides as potential immunosuppressive agents.

    abstract：:A series of new cinnamanilides (6-40) were synthesized and their immunosuppressive activity and cytotoxicity were evaluated. Most of the cinnamanilides showed good immunosuppressive activity. Among the synthesized compounds, (Z)-N-(4-bromophenyl)-2-methoxy-3-(4-methoxyphenyl)acrylamide (37) and (Z)-2-methoxy-3-(4-meth...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.10.027

    authors： Shi L,Wang L,Wang Z,Zhu HL,Song Q

    更新日期：2012-01-01 00:00:00

  • Synthesis of novel triazole derivatives as inhibitors of cytochrome P450 14alpha-demethylase (CYP51).

    abstract：:A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substitutedphenyl)-piperazin-1-yl]-propan-2-ols have been designed and synthesized on the basis of the structure-activity relationships and antimycotic mechanism of azole antifungal agents. Their structures were confirmed by elemental analysis, IR, MS ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.01.006

    authors： Sun QY,Xu JM,Cao YB,Zhang WN,Wu QY,Zhang DZ,Zhang J,Zhao HQ,Jiang YY

    更新日期：2007-09-01 00:00:00

  • Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.

    abstract：:5-(1-Methyl-4-phenyl-imidazol-5-yl)indoles 5 were prepared and tested as analogs of the natural vascular-disrupting agent combretastatin A-4 (CA-4). The 3-bromo-4,5-dimethoxyphenyl derivative 5c was far more active than CA-4 with low nanomolar IC50 concentrations against multidrug-resistant KB-V1/Vbl cervix and MCF-7/...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.04.045

    authors： Mahal K,Biersack B,Schruefer S,Resch M,Ficner R,Schobert R,Mueller T

    更新日期：2016-08-08 00:00:00

  • Discovery of fast-acting dual-stage antimalarial agents by profiling pyridylvinylquinoline chemical space via copper catalyzed azide-alkyne cycloadditions.

    abstract：:To identity fast-acting, multistage antimalarial agents, a series of pyridylvinylquinoline-triazole analogues have been synthesized via CuAAC. Most of the compounds display significant inhibitory effect on the drug-resistant malarial Dd2 strain at low submicromolar concentrations. Among the tested analogues, compound ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112889

    authors： Huang G,Solano CM,Melendez J,Yu-Alfonzo S,Boonhok R,Min H,Miao J,Chakrabarti D,Yuan Y

    更新日期：2021-01-01 00:00:00

  • Donepezil-butylated hydroxytoluene (BHT) hybrids as Anti-Alzheimer's disease agents with cholinergic, antioxidant, and neuroprotective properties.

    abstract：:The multifactorial nature of Alzheimer's disease (AD) calls for the development of multitarget agents addressing key pathogenic processes. A novel family of donepezil-butylated hydroxytoluene (BHT) hybrids were designed, synthesized and evaluated as multifunctional ligands against AD. The optimal compound 7d displayed...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.08.005

    authors： Cai P,Fang SQ,Yang HL,Yang XL,Liu QH,Kong LY,Wang XB

    更新日期：2018-09-05 00:00:00

  • Antimicrobial study of newly synthesized 6-substituted indolo[1,2-c]quinazolines.

    abstract：:A new series of indolo[1,2-c]quinazoline derivatives were prepared in good yield through reaction of 2-(o-aminophenyl)indole with a variety of arylaldehydes. The structures of the newly synthesized compounds were confirmed by IR, (1)H NMR, (13)C NMR and mass spectral studies and elemental analysis. All the title compo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.11.038

    authors： Rohini R,Muralidhar Reddy P,Shanker K,Hu A,Ravinder V

    更新日期：2010-03-01 00:00:00

  • Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.

    abstract：:TGR5, a GPCR, is involved in energy and glucose homeostasis, and as such, is a target for the treatment of diabetes, obesity and other metabolic syndromes. A new class of TGR5 agonists based on a 4-phenyl pyridine scaffold was designed, synthesized and evaluated in vitro and in vivo. Extensive structure-activity relat...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.07.050

    authors： Zhu J,Ning M,Guo C,Zhang L,Pan G,Leng Y,Shen J

    更新日期：2013-11-01 00:00:00