当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Development of resveratrol-curcumin hybrids as potential therapeutic agents for inflammatory lung diseases.

Development of resveratrol-curcumin hybrids as potential therapeutic agents for inflammatory lung diseases.

Abstract：

:Acute lung injury (ALI) is a major cause of acute respiratory failure in critically-ill patients. Resveratrol and curcumin are proven to have potent anti-inflammatory efficacy, but their clinical application is limited by their metabolic instability. Here, a series of resveratrol and the Mono-carbonyl analogs of curcumin (MCAs) hybrids were designed and synthesized by efficient aldol construction strategy, and then screened for anti-inflammatory activities in vitro and in vivo. The results showed that the majority of analogs effectively inhibited the LPS-induced production of IL-6 and TNF-α. Five analogs, a9, a18, a19, a20 and a24 exhibited excellent anti-inflammatory activity in a dose-dependent manner along with low toxicity in vitro. Structure activity relationship study revealed that the electron-withdrawing groups at meta-position and methoxyl group (OCH3) at the para position of the phenyl ring were important for anti-inflammatory activities. The most promising compound a18 decreased LPS induced TNF-α, IL-6, IL-12, and IL-33 mRNA expression. Additionally, a18 significantly protected against LPS-induced acute lung injury in the in vivo mouse model. The research of resveratrol and MCAs hybrids could bring insight into the treatment of inflammatory diseases and compound a18 may serve as a lead compound for the development of anti-ALI agents.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Pan J,Xu T,Xu F,Zhang Y,Liu Z,Chen W,Fu W,Dai Y,Zhao Y,Feng J,Liang G

doi

10.1016/j.ejmech.2016.09.033

subject

Has Abstract

pub_date

2017-01-05 00:00:00

pages

478-491

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30763-2

journal_volume

125

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Antihyperglycemic and antihyperlipidemic activities of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol in STZ induced diabetic rats.

    abstract：:Oral administration of 2-(4-[(2-hydroxybenzyl) amino]-phenyl amino-methyl)-phenol (HBPMP) (30 mg/kg) to Streptozotocin (STZ) rats produced significant antidiabetic activity after 6 h of HBPMP administration. Treatment of the STZ rats with HBPMP (30 mg/kg/day) for 30 days resulted in a significant decrease in their Fas...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.05.014

    authors： Sirasanagandla S,Kasetti RB,Shaik AN,Natava R,Surtineni VP,Cirradur SR,Chippada A

    更新日期：2013-08-01 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

  • Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.

    abstract：:To address drug resistance caused by ALK kinase mutations, especially the most refractory and predominant mutation G1202R for the second-generation ALK inhibitor, a series of new diarylaminopyrimidine analogues were designed by incorporating a resorcinol moiety (A-ring) to interact the ALK kinase domain where the G120...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.12.060

    authors： Geng K,Xia Z,Ji Y,Zhang RR,Sun D,Ai J,Song Z,Geng M,Zhang A

    更新日期：2018-01-20 00:00:00

  • Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells.

    abstract：:4'-((2-Propyl-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid derived from telmisartan was identified as lead for the design of cell death modulators. In this study, we evaluated the efficacy of telmisartan itself and other sartans in combination with imatinib against K562-resistant cells. The findi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112258

    authors： Schoepf AM,Salcher S,Obexer P,Gust R

    更新日期：2020-06-01 00:00:00

  • Synthesis and biochemical evaluation of guanidino-alkyl-ribitol derivatives as nucleoside hydrolase inhibitors.

    abstract：:Nucleoside hydrolase (NH) is a key enzyme in the purine salvage pathway. The purine specificity of the IAG-NH from Trypanosoma vivax is at least in part due to cation-pi-stacking interactions. Guanidinium ions can be involved in cation-pi-stacking interactions, therefore a series of guanidino-alkyl-ribitol derivatives...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.03.027

    authors： Goeminne A,McNaughton M,Bal G,Surpateanu G,Van Der Veken P,De Prol S,Versées W,Steyaert J,Haemers A,Augustyns K

    更新日期：2008-02-01 00:00:00

  • Design and synthesis of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents.

    abstract：:Type 2 diabetes (T2D) is a lifestyle disease affecting millions of people worldwide. Various therapies are available for the management of T2D and dipeptidyl peptidase-IV (DPP-IV) inhibition has emerged as a promising therapy for the treatment of type 2 diabetes (T2D). Here we report design, synthesis and in vitro eff...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.11.041

    authors： Sharma R,Soman SS

    更新日期：2015-01-27 00:00:00

  • Substitution at the indole 3 position yields highly potent indolecombretastatins against human tumor cells.

    abstract：:Resistance to combretastatin A-4 is mediated by metabolic modification of the phenolic hydroxyl and ether groups of the 3-hydroxy-4-methoxyphenyl (B ring). Replacement of the B ring of combretastatin A-4 by a N-methyl-5-indolyl reduces tubulin polymerization inhibition (TPI) and cytotoxicity against human cancer cell ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.08.078

    authors： Álvarez R,Gajate C,Puebla P,Mollinedo F,Medarde M,Peláez R

    更新日期：2018-10-05 00:00:00

  • Synthesis and biological evaluation of rhein amides as inhibitors of osteoclast differentiation and bone resorption.

    abstract：:Approaches of targeting excessive activation and differentiation of osteoclasts were considered as an effective treatment option for osteoporosis or osteopenia. In the present work, a series of rhein derivatives were synthesized and employed for their cytotoxicity screening against bone marrow-derived macrophages cell...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.08.004

    authors： Xu X,Qi X,Yan Y,Qi J,Qian N,Guo L,Li C,Wang F,Huang P,Zhou H,Jiang M,Yang C,Deng L

    更新日期：2016-11-10 00:00:00

  • Synthesis of antiplatelet ortho-carbonyl hydroquinones with differential action on platelet aggregation stimulated by collagen or TRAP-6.

    abstract：:Cardiovascular diseases are the leading cause of death in the world. Platelets have a major role in cardiovascular events as they bind to the damaged endothelium activating and forming thrombi. Although some hydroquinone scaffold-containing compounds have known antiplatelet activities, currently there is a lack of evi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112187

    authors： Méndez D,Urra FA,Millas-Vargas JP,Alarcón M,Rodríguez-Lavado J,Palomo I,Trostchansky A,Araya-Maturana R,Fuentes E

    更新日期：2020-04-15 00:00:00

  • Naphthyl quinoxaline thymidine conjugate is a potent anticancer agent post UVA activation and elicits marked inhibition of tumor growth through vaccination.

    abstract：:Anticancer anthracyclines are cytotoxic drugs that can induce antitumor immune response as a secondary effect through immunogenic cell death (ICD) mechanism. However, the immunogenic potency is quite limited, possibly due to that these chemotherapeutic agents are not specifically developed as ICD inducers. Thus, new d...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.03.051

    authors： Yuan Y,Wang Z,Yang R,Qian T,Zhou Q

    更新日期：2019-06-01 00:00:00

  • Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.

    abstract：:A series of pentacyclic triterpene 3β-ester derivatives were designed, synthesized and evaluated as a new class of cholesteryl ester transfer protein (CETP) inhibitors for the treatment of dyslipidemia. In vitro screening assay showed that 5 out of 30 compounds displayed moderate inhibiting human CETP activity with IC...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.08.012

    authors： Chen D,Huang X,Zhou H,Luo H,Wang P,Chang Y,He X,Ni S,Shen Q,Cao G,Sun H,Wen X,Liu J

    更新日期：2017-10-20 00:00:00

  • Synthesis and comparative photodynamic properties of two isosteric alkyl substituted zinc(II) phthalocyanines.

    abstract：:The synthesis and photophysical parameters of two novel isosteric cationic zinc(II) phthalocyanines: 2,9(10),16(17),23(24)-tetrakis[(N-butyl-N-methylammoniumethylsulfanyl]phthalocyaninatozinc(II) tetraiodide (6) and 2,9(10),16(17),23(24)-tetrakis[(N-dibutyl-N-methylammonium)ethoxy]phthalocyaninatozinc(II) tetraiodide ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.09.014

    authors： Gauna GA,Marino J,García Vior MC,Roguin LP,Awruch J

    更新日期：2011-11-01 00:00:00

  • Synthesis of 1-[3-(4-benzotriazol-1/2-yl-3-fluoro-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-3-substituted-thiourea derivatives as antituberculosis agents.

    abstract：:In continuation of our research program for new antituberculosis drugs, we have designed, synthesized and evaluated antimycobacterial activity of new series of 1-[3-(4-benzotriazol-1/2-yl-3-fluoro-phenyl)-2-oxo-oxazolidin-5-ylmethyl]-3-substituted-thiourea derivatives against different Mycobacterium species i.e. M. tu...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.12.005

    authors： Dixit PP,Patil VJ,Nair PS,Jain S,Sinha N,Arora SK

    更新日期：2006-03-01 00:00:00

  • Design, synthesis and anthelmintic activity of 7-keto-sempervirol analogues.

    abstract：:The plant-derived, diterpenoid 7-keto-sempervirol was recently reported to display moderate activity against larval stages of Schistosoma mansoni (IC50 = 19.1 μM) and Fasciola hepatica (IC50 = 17.7 μM), two related parasitic blood and liver flukes responsible for the neglected tropical diseases schistosomiasis and fas...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.04.032

    authors： Crusco A,Bordoni C,Chakroborty A,Whatley KCL,Whiteland H,Westwell AD,Hoffmann KF

    更新日期：2018-05-25 00:00:00

  • Bivalent bendamustine and melphalan derivatives as anticancer agents.

    abstract：:The alkylating agents bendamustine and melphalan are currently used in the treatment of various tumoral diseases. In order to increase their antitumor potency and tumor selectivity both compounds were integrated in structure-activity relationship studies including new drug carrier systems. Here we describe the synthes...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.02.008

    authors： Scutaru AM,Wenzel M,Gust R

    更新日期：2011-05-01 00:00:00

  • Designing dendrimers for ocular drug delivery.

    abstract：:New series of phosphorus-containing dendrimers, having one quaternary ammonium salt as core and carboxylic acid terminal groups have been synthesized from generation 0 (3 carboxylic acid terminal groups) to generation 2 (12 carboxylic acid terminal groups). These dendrimers react with the neutral form of carteolol (an...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.10.017

    authors： Spataro G,Malecaze F,Turrin CO,Soler V,Duhayon C,Elena PP,Majoral JP,Caminade AM

    更新日期：2010-01-01 00:00:00

  • Synthesis and pharmacological properties of a new hydrophilic and orally bioavailable 5-HT4 antagonist.

    abstract：:5-HT4 receptor antagonists have been suggested to have clinical potential in treatment of atrial fibrillation, diarrhea-prone irritable bowel syndrome and urinary incontinence. Recently, the use of 5-HT4 antagonists has been suggested to have a therapeutic benefit in heart failure. Affinity for the hERG potassium ion ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.03.060

    authors： Brudeli B,Moltzau LR,Nguyen CH,Andressen KW,Nilsen NO,Levy FO,Klaveness J

    更新日期：2013-06-01 00:00:00

  • Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules.

    abstract：:Identification of potent anticancer agents with high selectivity and low toxicity remains on the way to human health. Pyridazine featuring advantageous physicochemical properties and antitumor potential usually is regarded as a central core in numerous anticancer derivatives. There are several approved pyridazine-base...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112946

    authors： He ZX,Gong YP,Zhang X,Ma LY,Zhao W

    更新日期：2021-01-01 00:00:00

  • Asymmetric 1,5-diarylpenta-1,4-dien-3-ones: Antiproliferative activity in prostate epithelial cell models and pharmacokinetic studies.

    abstract：:To further engineer dienones with optimal combinations of potency and bioavailability, thirty-four asymmetric 1,5-diarylpenta-1,4-dien-3-ones (25-58) have been designed and synthesized for the evaluation of their in vitro anti-proliferative activity in three human prostate cancer cell lines and one non-neoplastic pros...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.05.062

    authors： Zhang X,Guo S,Chen C,Perez GR,Zhang C,Patanapongpibul M,Subrahmanyam N,Wang R,Keith J,Chen G,Dong Y,Zhang Q,Zhong Q,Zheng S,Wang G,Chen QH

    更新日期：2017-09-08 00:00:00

  • Design, synthesis and anticholinesterase activity of novel benzylidenechroman-4-ones bearing cyclic amine side chain.

    abstract：:A series of 3-(4-(aminoalkoxy)benzylidene)-chroman-4-ones 7a-r were designed and synthesized as analogs of homoisoflavonoids which are well known natural products with diverse pharmacological properties related to Alzheimer's disease. The in vitro anti-cholinesterase activity of designed compounds 7a-r against AChE an...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.04.055

    authors： Pourshojaei Y,Gouranourimi A,Hekmat S,Asadipour A,Rahmani-Nezhad S,Moradi A,Nadri H,Moghadam FH,Emami S,Foroumadi A,Shafiee A

    更新日期：2015-06-05 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

  • Polymeric bile acid sequestrants: Review of design, in vitro binding activities, and hypocholesterolemic effects.

    abstract：:Polymeric bile acid sequestrants (BAS) have recently attracted much attention as lipid-lowering agents. These non-absorbable materials specifically bind bile acids (BAs) in the intestine, preventing bile acid (BA) reabsorption into the blood through enterohepatic circulation. Therefore, it is important to understand t...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.12.015

    authors： Heřmánková E,Žák A,Poláková L,Hobzová R,Hromádka R,Širc J

    更新日期：2018-01-20 00:00:00

  • Synthesis and evaluation of tetrahydroquinolin-2(1H)-one derivatives as novel anti-pancreatic cancer agents via targeting autophagy.

    abstract：:Pancreatic cancer is one of the most deadly neoplasm with a 5-year survival rate of less than 6% owing to its remarkable tolerance to nutrient starvation, and new drugs and treatment strategies are urgently needed. During a project aiming at discovery of anticancer agents, we performed a structure modification on poly...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.03.013

    authors： Shen Q,Wang J,Liu CX,Cui W,Zhang L,Zhang YC,Wang Y,Wu J,Li JX

    更新日期：2019-05-15 00:00:00

  • Recent developments of quinolone-based derivatives and their activities against Escherichia coli.

    abstract：:Escherichia coli (E. coli) is the most common pathogen in both hospital and community settings, and is capable of causing infections that can lead to serious consequences. Quinolones, one of the most common antibiotics in clinical use, are effective weapons to treat E. coli infections. However, the resistance of E. co...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2018.08.095

    authors： Gao F,Wang P,Yang H,Miao Q,Ma L,Lu G

    更新日期：2018-09-05 00:00:00

  • Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.

    abstract：:Targeting epigenetic dysregulation has emerged as a valuable therapeutic strategy in cancer treatment. Especially epigenetic combination therapy of histone deacetylase inhibitors (HDACi) with established anti-cancer drugs has provided promising results in preclinical and clinical studies. The structural optimization o...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113095

    authors： Alves Avelar LA,Schrenk C,Sönnichsen M,Hamacher A,Hansen FK,Schliehe-Diecks J,Borkhardt A,Bhatia S,Kassack MU,Kurz T

    更新日期：2021-02-05 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

  • 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

  • Synthesis, in vitro β-glucuronidase inhibitory potential and molecular docking studies of quinolines.

    abstract：:In this study synthesis and β-glucuronidase inhibitory potential of 3/5/8 sulfonamide and 8-sulfonate derivatives of quinoline (1-40) are discussed. Studies reveal that all the synthetic compounds were found to have good inhibitory activity against β-glucuronidase. Nonetheless, compounds 1, 2, 5, 13, and 22-24 having ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.08.052

    authors： Bano B,Arshia,Khan KM,Kanwal,Fatima B,Taha M,Ismail NH,Wadood A,Ghufran M,Perveen S

    更新日期：2017-10-20 00:00:00

  • Indoles as therapeutics of interest in medicinal chemistry: Bird's eye view.

    abstract：:Indoles constitute extensively explored heterocyclic ring systems with wide range of applications in pathophysiological conditions that is, cancer, microbial and viral infections, inflammation, depression, migraine, emesis, hypertension, etc. Presence of indole nucleus in amino acid tryptophan makes it prominent in ph...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.04.003

    authors： Chadha N,Silakari O

    更新日期：2017-07-07 00:00:00

  • Pharmacophore model for pentamidine analogs active against Plasmodium falciparum.

    abstract：:Pentamidine and its analogs constitute a class of compounds that are known to be active against Plasmodium falciparum, which causes the most dangerous malarial infection. Malaria is a widespread disease known to affect hundreds of millions of people and presents a perceivable threat of spreading. Hence, there is a nee...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.09.012

    authors： Athri P,Wenzler T,Tidwell R,Bakunova SM,Wilson WD

    更新日期：2010-12-01 00:00:00