EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全第2页

Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.
abstract：:Based on the co-crystal structures of LXRβ and its agonists (spiro [pyrrolidine-3,3'-oxindole] derivatives) discovered by us previously, we designed and synthesized a compound library to explore the agonistic activities. The library was screened with luciferase reporter assays, interestingly, it resulted in the discov...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112793

authors： Chen Z,Chen H,Zhang Z,Ding P,Yan X,Li Y,Zhang S,Gu Q,Zhou H,Xu J

更新日期：2020-11-15 00:00:00
Covalent allosteric modulation: An emerging strategy for GPCRs drug discovery.
abstract：:Designing covalent allosteric modulators brings new opportunities to the field of drug discovery towards G-protein-coupled receptors (GPCRs). Targeting an allosteric binding pocket can allow a modulator to have protein subtype selectivity and low drug resistance. Utilizing covalent warheads further enables the modulat...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2020.112690

authors： Bian Y,Jun JJ,Cuyler J,Xie XQ

更新日期：2020-11-15 00:00:00
Discovery and optimization of benzenesulfonamides-based hepatitis B virus capsid modulators via contemporary medicinal chemistry strategies.
abstract：:Hepatitis B is a vaccine-preventable, but potentially life-threatening liver infection caused by the Hepatitis B virus (HBV). It represents an important health burden, with 257 million active cases globally. Current HBV treatments using nucleos(t)ide analogs and pegylated interferons cannot alleviate the situation com...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2020.112714

authors： Ren Y,Ma Y,Cherukupalli S,Tavis JE,Menéndez-Arias L,Liu X,Zhan P

更新日期：2020-11-15 00:00:00
Selenium as an interesting option for the treatment of Chagas disease: A review.
abstract：:Chagas disease is one of the most prevalent tropical neglected diseases and causes high mortality and morbidity in endemic countries. Current treatments for this disease, nifurtimox and benznidazole, are ineffective in the chronic phase of the disease and produce severe adverse effects. Therefore, novel therapies are ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2020.112673

authors： Alcolea V,Pérez-Silanes S

更新日期：2020-11-15 00:00:00
ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker.
abstract：:Current drugs available in clinic for Alzheimer's disease (AD) treatment can only alleviate disease symptoms without clearly curing or delaying the process of AD. And some AD drugs failed in Phase III clinical trials are only focused on targeting amyloid-β (Aβ). Therefore, an alternative strategy in AD drug design is ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112997

authors： Liu Z,Zhang B,Xia S,Fang L,Gou S

更新日期：2020-11-06 00:00:00
Bicyclic polyprenylated acylphloroglucinols and their derivatives: structural modification, structure-activity relationship, biological activity and mechanism of action.
abstract：:Bicyclic polyprenylated acylphloroglucinols (BPAPs), the principal bioactive benzophenone products isolated from plants of genera Garcinia and Hypericum, have attracted noticeable attention from the synthetic and biological communities due to their fascinating chemical structures and promising biological activities. H...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2020.112646

authors： Phang Y,Wang X,Lu Y,Fu W,Zheng C,Xu H

更新日期：2020-11-01 00:00:00
An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.
abstract：:Estrogen-related receptor gamma (ERRγ) is the NR3B subgroup of associated transcription factors. In this report, a new generation of a potent and selective ERRγ inverse agonist (25) with good biocompatibility was proposed. We also explored the potential of the newly developed compound 25 in the PDTC model to expand th...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112501

authors： Kim J,Hwang H,Yoon H,Lee JE,Oh JM,An H,Ji HD,Lee S,Cha E,Ma MJ,Kim DS,Lee SJ,Kadayat TM,Song J,Lee SW,Jeon JH,Park KG,Lee IK,Jeon YH,Chin J,Cho SJ

更新日期：2020-11-01 00:00:00
Synthesis and biological evaluation of geniposide derivatives as potent and selective PTPlB inhibitors.
abstract：:Herein a series of Geniposide derivatives were designed, synthesized and evaluated as protein tyrosine phosphatase 1B (PTPlB) inhibitors. Most of these compounds exhibited potent in vitro PTP1B inhibitory activities, the representative 7a and 17f were found to be the most potent inhibitors against the enzyme with IC50...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112508

authors： Lei S,Zhang D,Qi Y,Chowdhury SR,Sun R,Wang J,Du Y,Fu L,Jiang F

更新日期：2020-11-01 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
Design, synthesis and in vivo evaluation of 3-arylcoumarin derivatives of rhenium(I) tricarbonyl complexes as potent antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA).
abstract：:We have prepared a series of ten 3-arylcoumarin molecules, their respective fac-[Re(CO)3(bpy)L]+ and fac-[Re(CO)3(L⁀L)Br] complexes and tested all compounds for their antimicrobial efficacy. Whereas the 3-arylcoumarin ligands are virtually inactive against the human-associated pathogens with minimum inhibitory concent...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112533

authors： Sovari SN,Vojnovic S,Bogojevic SS,Crochet A,Pavic A,Nikodinovic-Runic J,Zobi F

更新日期：2020-11-01 00:00:00
The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.
abstract：:Based on the SAR of both α1-AR antagonists and 5α-reductase (5AR) inhibitors, the dual-acting agent 4-(1-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-1H-indol-3-yl)butanoic acid 4aaa was designed against BPH and synthesized by two steps of N-alkylation. One-pot protocol towards 4aaa was newly developed. With IL [C6min...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112616

authors： Zeng LY,Yang F,Chen K,Zeng Y,Jiang Z,Liu S,Xi B

更新日期：2020-11-01 00:00:00
Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes.
abstract：:New promising unsymmetrical bisacridine derivatives (UAs), have been developed. Three groups including 36 compounds were synthesized by the condensation of 4-nitro or 4-methylacridinone, imidazoacridinone and triazoloacridinone derivatives with 1-nitroacridine compounds linked with an aminoalkyl chain. Cytotoxicity sc...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112599

authors： Paluszkiewicz E,Horowska B,Borowa-Mazgaj B,Peszyńska-Sularz G,Paradziej-Łukowicz J,Augustin E,Konopa J,Mazerska Z

更新日期：2020-10-15 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
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
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
An exhaustive perspective on structural insights of SGLT2 inhibitors: A novel class of antidiabetic agent.
abstract：:Diabetes mellitus is the global health issue and become an alarming threat in the modern era where human lifestyle gets compromised with modernization. According to the latest statistical report 2020, USA has 9.47% (31 million among 32.72 cr), China has 8.3% (116.4 million among 139.27 cr) and India has 5.6% (77 milli...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2020.112523

authors： Bhattacharya S,Rathore A,Parwani D,Mallick C,Asati V,Agarwal S,Rajoriya V,Das R,Kashaw SK

更新日期：2020-10-15 00:00:00
Development of dual inhibitors targeting pyruvate dehydrogenase kinases and human lactate dehydrogenase A: High-throughput virtual screening, synthesis and biological validation.
abstract：:Most cancer cells feature an altered glucose metabolism from oxidative phosphorylation to cytoplasmic glycolysis. Pyruvate dehydrogenase kinases (PDKs) and lactate dehydrogenase A (LDHA) play crucial roles in promotion of glycolysis, thus the inhibition of both enzymes is considered a promising strategy for developing...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112579

authors： Xiang S,Huang D,He Q,Li J,Tam KY,Zhang SL,He Y

更新日期：2020-10-01 00:00:00
Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression.
abstract：:Aurora Kinase B is a serine-threonine kinase known to be overexpressed in several cancers, with no inhibitors approved for clinical use. Herein, we present the discovery and optimization of a series of novel quinazoline-based Aurora Kinase B inhibitors. The lead inhibitor SP-96 shows sub-nanomolar potency in Aurora B ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112589

authors： Lakkaniga NR,Zhang L,Belachew B,Gunaganti N,Frett B,Li HY

更新日期：2020-10-01 00:00:00
Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.
abstract：:Five series of novel thiophene-pyrimidine derivatives (9a-h, 10a-f, 11a-f, 12a-f, 13a-f) have been synthesized and tested for their anti-proliferative activity against several cancer cell lines in which EGF is highly expressed. Most of the target compounds showed excellent activity against one or more cancer cell line...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112511

authors： Xiao Z,Zhou Z,Chu C,Zhang Q,Zhou L,Yang Z,Li X,Yu L,Zheng P,Xu S,Zhu W

更新日期：2020-10-01 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
Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability.
abstract：:We previously reported that MGS0008 is a selective group II metabotropic glutamate receptor (mGlu2/3 receptor) agonist that is effective in animal models of schizophrenia. MGS0008 is a highly hydrophilic glutamate analog and is therefore expected to show low oral bioavailability in humans. To improve the oral bioavail...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112521

authors： Urabe H,Miyakoshi N,Ohtake N,Nozoe A,Ochi M,Fukasawa M,Kinoshita K,Yamaguchi JI,Marumo T,Hikichi H,Chaki S,Hashihayata T

更新日期：2020-10-01 00:00:00
Design, synthesis and antitumour evaluation of pyrrolo[1,2-f]-phenanthridine and dibenzo[f,h]pyrrolo[1,2-b]isoquinoline derivatives.
abstract：:A series of 1,2-bis(hydroxymethyl)pyrrolo[1,2-f]phenanthridine derivatives and their alkyl (ethyl and isopropyl) carbamates and 12,13-bis(hydroxymethyl)-9,14-dihydro-dibenzo[f,h]pyrrolo[1,2-b]isoquinoline derivatives were synthesized for antiproliferative evaluation. The preliminary antitumour studies revealed that th...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112516

authors： Patel AS,Jain V,Rao VN,Lin YW,Shah A,Lai KC,Su TL,Lee TC

更新日期：2020-09-15 00:00:00
Structure-based design, semi-synthesis and anti-inflammatory activity of tocotrienolic amides as 5-lipoxygenase inhibitors.
abstract：:Inflammation contributes to the development of various pathologies, e.g. asthma, cardiovascular diseases, some types of cancer, and metabolic disorders. Leukotrienes (LT), biosynthesized from arachidonic acid by 5-lipoxygenase (5-LO), constitute a potent family of pro-inflammatory lipid mediators. δ-Garcinoic acid (δ-...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112518

authors： Dinh CP,Ville A,Neukirch K,Viault G,Temml V,Koeberle A,Werz O,Schuster D,Stuppner H,Richomme P,Helesbeux JJ,Séraphin D

更新日期：2020-09-15 00:00:00
Discovery of carboxyl-containing biaryl ureas as potent RORγt inverse agonists.
abstract：:GSK805 (1) is a potent RORγt inverse agonist, but a drawback of 1 is its low solubility, leading to a limited absorption in high doses. We have explored detailed structure-activity relationship on the amide linker, biaryl and arylsulfonyl moieties of 1 trying to improve solubility while maintaining RORγt activity. As ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112536

authors： Sun N,Huang Y,Yu M,Zhao Y,Chen JA,Zhu C,Song M,Guo H,Xie Q,Wang Y

更新日期：2020-09-15 00:00:00
Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.
abstract：:ATX was capable of catalyzing the hydrolysis of LPC to the lipid mediator LPA which attracted considerable attention on the development of potent ATX inhibitors. Herein, driven by the HTS product indole-based lead 1, a hybridization strategy was utilized to construct the trifluoroacetyl hydrazone moiety through assemb...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112456

authors： Lei H,Li C,Yang Y,Jia F,Guo M,Zhu M,Jiang N,Zhai X

更新日期：2020-09-01 00:00:00
Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy.
abstract：:Persistently activated signal transducer and activator of transcription 3 (STAT3) plays an important role in the development of multiple cancers, and therefore is a potential therapeutic target for cancer prevention. Herein, we report the rational design, synthesis, and biological evaluation of novel potent STAT3 inhi...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112428

authors： Feng KR,Wang F,Shi XW,Tan YX,Zhao JY,Zhang JW,Li QH,Lin GQ,Gao D,Tian P

更新日期：2020-09-01 00:00:00
Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation.
abstract：:We report the design of hetero-bifunctional small molecules that selectively target p38α and p38β for degradation. These proteolysis targeted chimeras (PROTACs) are based on an ATP competitive inhibitor of p38α and p38β, which is linked to thalidomide analogues to recruit the Cereblon E3 ubiquitin ligase complex. Comp...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112451

authors： Donoghue C,Cubillos-Rojas M,Gutierrez-Prat N,Sanchez-Zarzalejo C,Verdaguer X,Riera A,Nebreda AR

更新日期：2020-09-01 00:00:00
Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
abstract：:Histone modifying proteins, specifically histone deacetylases (HDACs) and bromodomains, have emerged as novel promising targets for anticancer therapy. In the current work, based on available crystal structures and docking studies, we designed dual inhibitors of both HDAC6/8 and the bromodomain and PHD finger containi...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112338

authors： Ghazy E,Zeyen P,Herp D,Hügle M,Schmidtkunz K,Erdmann F,Robaa D,Schmidt M,Morales ER,Romier C,Günther S,Jung M,Sippl W

更新日期：2020-08-15 00:00:00
Design and synthesis of novel SCM-198 analogs as cardioprotective agents: Structure-activity relationship studies and biological evaluations.
abstract：:SCM-198 (Leonurine) has attracted great attention due to its cardioprotective effects in myocardial infarction (MI). However, no systematic modifications and structure-activity relationship (SAR) studies could be traced so far. In this study, 35 analogs of SCM-198 were designed, synthesized and their cardioprotective ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112469

authors： Luo S,Xu S,Liu J,Ma F,Zhu YZ

更新日期：2020-08-15 00:00:00
Naphthalimide-based macrophage nucleus imaging probes.
abstract：:The photophysical properties of naphthalimide-based fluorophores can be easily tuned by chemical manipulation of the substituents on that privileged scaffold. Replacement of a OMe group at position 6 in 2-(hydroxyl)ethyl-naphthalimide derivatives by diverse amines, including 2-(hydroxyl)ethylamine, trans-(4-acetamido)...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112407

authors： Fueyo-González F,Fernández-Gutiérrez M,García-Puentes D,Orte A,González-Vera JA,Herranz R

更新日期：2020-08-15 00:00:00
Discovery of phenylselenoether-hydantoin hybrids as ABCB1 efflux pump modulating agents with cytotoxic and antiproliferative actions in resistant T-lymphoma.
abstract：:Multidrug resistance (MDR) in cancer cells is a crucial aspect to consider for a successful cancer therapy. P-gp/ABCB1, a member of ABC transporters, is involved in the main tumour MDR mechanism, responsible for the efflux of drugs and cytotoxic substances. Herein, we describe a discovery of potent selenium-containing...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112435

authors： Ali W,Spengler G,Kincses A,Nové M,Battistelli C,Latacz G,Starek M,Dąbrowska M,Honkisz-Orzechowska E,Romanelli A,Rasile MM,Szymańska E,Jacob C,Zwergel C,Handzlik J

更新日期：2020-08-15 00:00:00
Recent advances in DNA gyrase-targeted antimicrobial agents.
abstract：:Antimicrobial resistance is one of the greatest challenges facing the world today. In the United States alone, it is responsible for the death of more than 20,000 people each year. DNA gyrase, a well-validated drug target, is involved in bacterial DNA replication, repair and decatenation. Currently, the fluoroquinolon...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2020.112326

authors： Dighe SN,Collet TA

更新日期：2020-08-01 00:00:00
Dual-acidity-labile polysaccharide-di-drugs conjugate for targeted cancer chemotherapy.
abstract：:Polymer-drug conjugates synthesized by binding therapeutic agents to functional polymers have long been a mainstay of prodrugs, while the slow drug release, insufficient efficacy of a single drug, and low selectivity hamper the clinical translation. By rational prodrug design, a targeted dual-acidity-labile polysaccha...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112367

authors： Li D,Su T,Ma L,Yin F,Xu W,Ding J,Li Z

更新日期：2020-08-01 00:00:00
Cyclopentadienyl ruthenium(II) carbosilane metallodendrimers as a promising treatment against advanced prostate cancer.
abstract：:In searching for efficient and selective antitumour drugs, a new family of carbosilane metallodendrimers functionalized with [Ru(η5-C5H5)(PTA)Cl] (PTA = 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1] decane) is reported. Experiments of the biophysical characterization showed an ability to interact with biological membranes,...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112414

authors： Sanz Del Olmo N,Bajo AM,Ionov M,García-Gallego S,Bryszewska M,Gómez R,Ortega P,de la Mata FJ

更新日期：2020-08-01 00:00:00
Monocarboxylate transporter 1 and 4 inhibitors as potential therapeutics for treating solid tumours: A review with structure-activity relationship insights.
abstract：:Development of multidrug resistance (MDR) is one of the major causes leading to failure of cancer chemotherapy and radiotherapy. Monocarboxylate transporters (MCTs) MCT1 and MCT4, which are overexpressed in solid tumours, play a very important role in cancer cell survival and proliferation. These lactate transporters ...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章,评审

doi：10.1016/j.ejmech.2020.112393

authors： Puri S,Juvale K

更新日期：2020-08-01 00:00:00
Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome.
abstract：:Recent preclinical studies have shown that activation of the serotonin 5-HT7 receptor has the potential to treat neurodevelopmental disorders such as Fragile X syndrome, a rare disease characterized by autistic features. With the aim to provide the scientific community with diversified drug-like 5-HT7 receptor-preferr...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112395

authors： Lacivita E,Niso M,Stama ML,Arzuaga A,Altamura C,Costa L,Desaphy JF,Ragozzino ME,Ciranna L,Leopoldo M

更新日期：2020-08-01 00:00:00
Indole chalcones: Design, synthesis, in vitro and in silico evaluation against Mycobacterium tuberculosis.
abstract：:Indole chalcones were designed and synthesized as a promising set of compounds against H37Rv strain of Mycobacterium tuberculosis. Within this library of compounds, (E)-1-(furan-3-yl)-3-(1H-indol-3-yl)prop-2-en-1-one (18), (E)-3-(1H-indol-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one (20) and (E)-2-((1H-indol-2-yl)methylene)...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112358

authors： Ramesh D,Joji A,Vijayakumar BG,Sethumadhavan A,Mani M,Kannan T

更新日期：2020-07-15 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
Specific stabilization of promoter G-Quadruplex DNA by 2,6-disubstituted amidoanthracene-9,10-dione based dimeric distamycin analogues and their selective cancer cell cytotoxicity.
abstract：:We have designed and synthesized anthraquinone containing compounds which have oligopyrrole side chains of varying lengths. These compounds stabilized the G-quadruplex DNA formed in the promoter regions of c-MYC oncogenes selectively over the duplex DNA. These observations were recorded using UV-vis spectroscopic titr...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112202

authors： Roy S,Ali A,Kamra M,Muniyappa K,Bhattacharya S

更新日期：2020-06-01 00:00:00
Synthesis of novel monocarbonyl curcuminoids, evaluation of their efficacy against MRSA, including ex vivo infection model and their mechanistic studies.
abstract：:In continuation of our effort to improve the physiological stability and the antibacterial activity of curcuminoids against drug-resistant bacteria, a series of novel monocarbonyl curcuminoids were synthesized and screened for antibacterial activity against S. aureus and E. coli strains. These curcuminoids showed pote...

journal_title：European journal of medicinal chemistry

pub_type： 杂志文章

doi：10.1016/j.ejmech.2020.112276

authors： Gagandeep,Kumar P,Kandi SK,Mukhopadhyay K,Rawat DS

更新日期：2020-06-01 00:00:00

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