Synthesis and Biological Evaluation of Glycyrrhetic Acid Derivatives as Potential VEGFR2 Inhibitors.

abstract：:We synthesized potential inhibitors of farnesyl diphosphate synthase (FPPS), undecaprenyl diphosphate synthase (UPPS), or undecaprenyl diphosphate phosphatase (UPPP), and tested them in bacterial cell growth and enzyme inhibition assays. The most active compounds were found to be bisphosphonates with electron-withdraw...

journal_title：ChemMedChem

authors： Desai J,Wang Y Dr,Wang K Dr,Malwal SR Dr,Oldfield E

更新日期：2016-10-06 00:00:00

abstract：:A common issue during drug design and development is the discovery of novel scaffolds for protein targets. On the one hand the chemical space of purchasable compounds is rather limited; on the other hand artificially generated molecules suffer from a grave lack of accessibility in practice. Therefore, we generated a n...

journal_title：ChemMedChem

authors： Humbeck L,Weigang S,Schäfer T,Mutzel P,Koch O

更新日期：2018-03-20 00:00:00

abstract：:Protein tyrosine phosphatase 1B (PTP1B) is an important target for the treatment of diabetes. A series of thiazolidin-4-one derivatives 8-22 was designed, synthesized and investigated as PTP1B inhibitors. The new molecules inhibited PTP1B with IC50 values in the micromolar range. 5-(Furan-2-ylmethylene)-2-(4-nitrophen...

journal_title：ChemMedChem

authors： Patel AD,Pasha TY,Lunagariya P,Shah U,Bhambharoliya T,Tripathi RKP

更新日期：2020-07-03 00:00:00

abstract：:Herein we report the design, synthesis, X-ray structural, and biological studies of an exceptionally potent HIV-1 protease inhibitor, compound 5 ((3S,7aS,8S)-hexahydro-4H-3,5-methanofuro[2,3-b]pyran-8-yl ((2S,3R)-4-((2-(cyclopropylamino)-N-isobutylbenzo[d]thiazole)-6-sulfonamido)-1-(3,5-difluorophenyl)-3-hydroxybutan-...

journal_title：ChemMedChem

authors： Ghosh AK,Rao KV,Nyalapatla PR,Kovela S,Brindisi M,Osswald HL,Sekhara Reddy B,Agniswamy J,Wang YF,Aoki M,Hattori SI,Weber IT,Mitsuya H

更新日期：2018-04-23 00:00:00

abstract：:Into the fold: Prion diseases are neurodegenerative disorders characterized by the accumulation in the brain of a self-replicating, misfolded isoform (PrPSc ) of the cellular prion protein (PrPC ). No therapies are available for these pathologies. We capitalized on previously described cell-based assays to screen a li...

journal_title：ChemMedChem

authors： Massignan T,Sangiovanni V,Biggi S,Stincardini C,Elezgarai SR,Maietta G,Andreev IA,Ratmanova NK,Belov DS,Lukyanenko ER,Belov GM,Barreca ML,Altieri A,Kurkin AV,Biasini E

更新日期：2017-08-22 00:00:00

abstract：:TIBO- and TBO-like sulfone derivatives 1 and 2 were designed, synthesized, and tested for their ability to block the replication cycle of HIV-1 in infected cells. The anti-HIV-1 activities of sulfones 3, which were intermediates in the syntheses of 1 and 2, were also evaluated. Surprisingly, the sulfone analogues of T...

journal_title：ChemMedChem

authors： Di Santo R,Costi R,Artico M,Ragno R,Lavecchia A,Novellino E,Gavuzzo E,La Torre F,Cirilli R,Cancio R,Maga G

更新日期：2006-01-01 00:00:00

abstract：:Small-molecule inhibitors of hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) are currently under clinical development as novel treatment options for chronic kidney disease (CKD) associated anemia. Inhibition of HIF-PH mimics hypoxia and leads to increased erythropoietin (EPO) expression and subsequently increas...

journal_title：ChemMedChem

authors： Beck H,Jeske M,Thede K,Stoll F,Flamme I,Akbaba M,Ergüden JK,Karig G,Keldenich J,Oehme F,Militzer HC,Hartung IV,Thuss U

更新日期：2018-05-23 00:00:00

abstract：:The glucocorticoid receptor (GR) is a member of the nuclear receptor superfamily that affects immune response, development, and metabolism in target tissues. Glucocorticoids are widely used to treat diverse pathophysiological conditions, but their clinical applicability is limited by side effects. A prediction of the ...

journal_title：ChemMedChem

authors： Spreafico M,Ernst B,Lill MA,Smiesko M,Vedani A

更新日期：2009-01-01 00:00:00

abstract：:Bromodomains (BRDs) are small protein domains found in a variety of proteins that recognize and bind to acetylated histone tails. This binding affects chromatin structure and facilitates the localisation of transcriptional complexes to specific genes, thereby regulating epigenetically controlled processes including ge...

journal_title：ChemMedChem

authors： Mirguet O,Lamotte Y,Chung CW,Bamborough P,Delannée D,Bouillot A,Gellibert F,Krysa G,Lewis A,Witherington J,Huet P,Dudit Y,Trottet L,Nicodeme E

更新日期：2014-03-01 00:00:00

abstract：:Iridium(III) complexes of the type [Ir(η(5) -C5 Me5 )Cl2 {Ph2 PCH2 CH2 CH2 S(O)x Ph-κP}] (x=0-2; 1-3) and [Ir(η(5) -C5 Me5 )Cl{Ph2 PCH2 CH2 CH2 S(O)x Ph-κP,κS}][PF6 ] (x=0-1; 4 and 5) with 3-(diphenylphosphino)propyl phenyl sulfide, sulfoxide, and sulfone ligands Ph2 PCH2 CH2 CH2 S(O)x Ph were designed, synthesized, a...

journal_title：ChemMedChem

authors： Ludwig G,Ranđelović I,Maksimović-Ivanić D,Mijatović S,Bulatović MZ,Miljković D,Korb M,Lang H,Steinborn D,Kaluđerović GN

更新日期：2014-07-01 00:00:00

abstract：:The NLRP3 inflammasome is an important regulator of the sterile inflammatory response, and its activation by host-derived sterile molecules leads to the intracellular activation of caspase-1, processing of the pro-inflammatory cytokines interleukin-1β (IL-1β)/IL-18, and pyroptotic cell death. Inappropriate activation ...

journal_title：ChemMedChem

authors： Baldwin AG,Tapia VS,Swanton T,White CS,Beswick JA,Brough D,Freeman S

更新日期：2018-02-20 00:00:00

abstract：:Computational chemistry has shown that backbone-alkylated imidazoles ought to be efficient ligands for transition metal catalysts with improved carbene-to-metal donation. In this work, such alkylated imidazoles were synthesized and complexed with silver(I) by means of an eight/nine-step synthetic pathway we devised to...

journal_title：ChemMedChem

authors： Sandtorv AH,Leitch C,Bedringaas SL,Gjertsen BT,Bjørsvik HR

更新日期：2015-09-01 00:00:00

abstract：:Src homology 2 (SH2)-domain-mediated interactions with phosphotyrosine (pY)-containing ligands are critical for the regulation of SHP-1 phosphatase activity. Peptides based on a binding site from receptor tyrosine kinase Ros (EGLN-pY2267-MVL, 1) have recently been shown to bind to the SHP-1 N-terminal SH2 domain (N-SH...

journal_title：ChemMedChem

authors： Hampel K,Kaufhold I,Zacharias M,Böhmer FD,Imhof D

更新日期：2006-08-01 00:00:00

abstract：:A severe limitation in cancer therapy is the often insufficient differentiation between malign and benign tissue using known chemotherapeutics. One approach to decrease side effects is antibody-directed enzyme prodrug therapy (ADEPT). We have developed new glycosidic prodrugs such as (-)-(1S)-26 b based on the antibio...

journal_title：ChemMedChem

authors： Tietze LF,von Hof JM,Krewer B,Müller M,Major F,Schuster HJ,Schuberth I,Alves F

更新日期：2008-12-01 00:00:00

abstract：:A small library of 17 organoruthenium compounds with the general formula [RuII (fcl)(chel)(L)]n+ (in which fcl=face capping ligand, chel=chelating bidentate ligand, and L=monodentate ligand) were screened for inhibitory activity against cholinesterases and glutathione-S-transferases of human and animal origins. Compou...

journal_title：ChemMedChem

authors： Ristovski S,Uzelac M,Kljun J,Lipec T,Uršič M,Zemljič Jokhadar Š,Žužek MC,Trobec T,Frangež R,Sepčić K,Turel I

更新日期：2018-10-22 00:00:00

abstract：:We previously found that p97 ATPase inhibitors 2-(2-amino-1H-benzo[d]imidazol-1-yl)-N-benzyl-8-methoxyquinazolin-4-amine (ML240) and 2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine (ML241) specifically target the D2 domain of wild-type p97. In addition, one of the major p97 cofactors,...

journal_title：ChemMedChem

authors： Fang CJ,Gui L,Zhang X,Moen DR,Li K,Frankowski KJ,Lin HJ,Schoenen FJ,Chou TF

更新日期：2015-01-01 00:00:00

abstract：:Cardiotoxicity is a common side effect of a large variety of drugs that is often caused by off-target human ether-à-go-go-related gene (hERG) potassium channel blockade. In this study, we designed and synthesized a series of derivatives of the class III antiarrhythmic agent E-4031. These compounds where evaluated in a...

journal_title：ChemMedChem

authors： Vilums M,Overman J,Klaasse E,Scheel O,Brussee J,IJzerman AP

更新日期：2012-01-02 00:00:00

abstract：:Plasmodium parasites kill 435 000 people around the world every year due to unavailable vaccines, a limited arsenal of antimalarial drugs, delayed treatment, and the reduced clinical effectiveness of current practices caused by drug resistance. Therefore, there is an urgent need to discover and develop new antiplasmod...

journal_title：ChemMedChem

authors： de Souza Pereira C,Costa Quadros H,Magalhaes Moreira DR,Castro W,Santos De Deus Da Silva RI,Botelho Pereira Soares M,Fontinha D,Prudêncio M,Schmitz V,Dos Santos HF,Gendrot M,Fonta I,Mosnier J,Pradines B,Navarro M

更新日期：2020-11-24 00:00:00

abstract：:A facile protocol that enables synthetic interconversion of CUR-BF2 and CUR compounds is described that significantly widens the preparative scope of curcuminoids, providing access to larger libraries of compounds, thus enabling comparative antiproliferative and apoptotic study of a larger library of synthetic analogs...

journal_title：ChemMedChem

authors： Abonia R,Laali KK,Raja Somu D,Bunge SD,Wang EC

更新日期：2020-02-17 00:00:00

abstract：:The therapeutic potential of photoactive CO-releasing molecules (photoCORMs) have called for close examination of the roles of the ligand(s) and the central metal atoms on the overall photochemical labilization of the metal-CO bonds. Along this line, we have synthesized four metal complexes, namely, [MnBr(azpy)(CO)3 ]...

journal_title：ChemMedChem

authors： Chakraborty I,Carrington SJ,Mascharak PK

更新日期：2014-06-01 00:00:00

abstract：:The Eph-ephrin system, including the EphA2 receptor and the ephrinA1 ligand, plays a critical role in tumor and vascular functions during carcinogenesis. We previously identified (3α,5β)-3-hydroxycholan-24-oic acid (lithocholic acid) as an Eph-ephrin antagonist that is able to inhibit EphA2 receptor activation; it is ...

journal_title：ChemMedChem

authors： Tognolini M,Incerti M,Hassan-Mohamed I,Giorgio C,Russo S,Bruni R,Lelli B,Bracci L,Noberini R,Pasquale EB,Barocelli E,Vicini P,Mor M,Lodola A

更新日期：2012-06-01 00:00:00

abstract：:The histamine H1 G protein-coupled receptor (GPCR) plays an important role in allergy and inflammation. Existing drugs that address the H1 receptor differ in their chemical structure, pharmacology, and side effects. Light-controllable spatial and temporal activity regulation of photochromic H1 ligands may contribute t...

journal_title：ChemMedChem

authors： Rustler K,Pockes S,König B

更新日期：2019-03-22 00:00:00

abstract：:(±)-6-Alkyl-2,4-diaminopyrimidine-based inhibitors of bacterial dihydrofolate reductase (DHFR) have been prepared and evaluated for biological potency against Bacillus anthracis and Staphylococcus aureus. Biological studies revealed attenuated activity relative to earlier structures lacking substitution at C6 of the d...

journal_title：ChemMedChem

authors： Nammalwar B,Bourne CR,Bunce RA,Wakeham N,Bourne PC,Ramnarayan K,Mylvaganam S,Berlin KD,Barrow EW,Barrow WW

更新日期：2012-11-01 00:00:00

abstract：:Following the discovery of a type III allosteric modulator of cyclin-dependent kinase 2 (CDK2) characterized by a hexahydrocyclopenta[c]quinolone scaffold, three different series of its derivatives were synthesized and biologically evaluated. Docking of the synthesized compounds into the allosteric pocket of CDK2 allo...

journal_title：ChemMedChem

authors： Carlino L,Christodoulou MS,Restelli V,Caporuscio F,Foschi F,Semrau MS,Costanzi E,Tinivella A,Pinzi L,Lo Presti L,Battistutta R,Storici P,Broggini M,Passarella D,Rastelli G

更新日期：2018-12-20 00:00:00

abstract：:Numerous studies have shown that chalcones are promising scaffolds for the development of new monoamine oxidase-B (MAO-B) inhibitors. As a continuation of our ongoing research into the development of reversible human MAO-B (hMAO-B) inhibitors, two series of twenty chalcones containing electron-donating and electron-wi...

journal_title：ChemMedChem

authors： Mathew B,Uçar G,Mathew GE,Mathew S,Kalatharakkal Purapurath P,Moolayil F,Mohan S,Varghese Gupta S

更新日期：2016-12-16 00:00:00

abstract：:Polo-like kinase 1 (PLK1) plays crucial functions in multiple stages of mitosis and is considered to be a potential drug target for cancer therapy. The functions of PLK1 are mediated by its N-terminal kinase domain and C-terminal polo-box domain (PBD). Most inhibitors targeting the kinase domain of PLK1 have a selecti...

journal_title：ChemMedChem

authors： Shan HM,Shi Y,Quan J

更新日期：2015-01-01 00:00:00

abstract：:Cellular chaperones that belong to the heat-shock protein 90 (Hsp90) family are a prerequisite for successful viral propagation for most viruses. The hepatitis C virus (HCV) uses Hsp90 for maturation, folding, and modification of viral proteins. Based on our previous discovery that marine alkaloid analogues with a 4,5...

journal_title：ChemMedChem

authors： Lillsunde KE,Tomašič T,Schult P,Lohmann V,Kikelj D,Tammela P

更新日期：2019-02-05 00:00:00

abstract：:Protein-protein interactions (PPIs) control many cellular processes in cancer and tumour growth. Of significant interest is the role PPIs play in regulating apoptosis. The overexpression of the antiapoptosis regulating Bcl-2 family of proteins is commonly observed in several cancers, leading to resistance towards both...

journal_title：ChemMedChem

authors： Beekman AM,O'Connell MA,Howell LA

更新日期：2016-04-19 00:00:00

abstract：:Tau-tubulin kinase 1 (TTBK1) is a serine/threonine/tyrosine kinase that putatively phosphorylates residues including S422 in tau protein. Hyperphosphorylation of tau protein is the primary cause of tau pathology and neuronal death associated with Alzheimer's disease. A library of 12 truncation variants comprising the ...

journal_title：ChemMedChem

authors： Xue Y,Wan PT,Hillertz P,Schweikart F,Zhao Y,Wissler L,Dekker N

更新日期：2013-11-01 00:00:00

abstract：:Having oxaliplatin as archetype, several platinum complexes with a carbohydrate moiety resembling the cyclohexane-1,2-diamine ligand of oxaliplatin have been prepared. As leaving groups, the anionic ligands iodide, oxalate, and malonate were utilized, and for comparison purposes the chloro complex was employed. All co...

journal_title：ChemMedChem

authors： Berger I,Nazarov AA,Hartinger CG,Groessl M,Valiahdi SM,Jakupec MA,Keppler BK

更新日期：2007-04-01 00:00:00