Acyclic Cucurbit[n]uril-Type Molecular Containers: Influence of Linker Length on Their Function as Solubilizing Agents.

abstract：:A series of four stable synthetic bacteriochlorins was tested in vitro in HeLa cells for their potential in photodynamic therapy (PDT). The parent bacteriochlorin (BC), dicyano derivative (NC)(2)BC and corresponding zinc chelate (NC)(2)BC-Zn and palladium chelate (NC)(2)BC-Pd were studied. Direct dilution of a solutio...

journal_title：ChemMedChem

authors： Huang YY,Balasubramanian T,Yang E,Luo D,Diers JR,Bocian DF,Lindsey JS,Holten D,Hamblin MR

更新日期：2012-12-01 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：:Some hybrid foldamers of various length, all containing the (4R,5S)-4-carboxy-5-methyloxazolidin-2-one (d-Oxd) moiety alternating with an l-amino acid (l-Val, l-Lys, or l-Ala), were prepared in order to study their preferred conformations and to evaluate their biological activity. Surprisingly, only the longer oligome...

journal_title：ChemMedChem

authors： Del Secco B,Malachin G,Milli L,Zanna N,Papini E,Cornia A,Tavano R,Tomasini C

更新日期：2017-02-20 00:00:00

abstract：:Over the past few years, the number of people diagnosed with type 2 diabetes has increased owing to an unhealthy diet, a limited amount of exercise, and obesity. The search for novel and efficient antidiabetes agents has become an urgent task for scientists. Among the antidiabetes drugs, α-glucosidase inhibitor drugs ...

journal_title：ChemMedChem

authors： Liu Z,Ma S

更新日期：2017-06-07 00:00:00

abstract：:The spider polyamine toxins Joro spider toxin-3 (JSTX-3) and Nephila polyamine toxins-1 and -8 (NPTX-1 and NPTX-8) are isolated from the venom of the orb-weaver spider Nephila clavata (Joro spider). They share a high degree of structural resemblance, their aromatic head groups being the only difference, and were recen...

journal_title：ChemMedChem

authors： Xiong XF,Poulsen MH,Hussein RA,Nørager NG,Strømgaard K

更新日期：2014-12-01 00:00:00

abstract：:We previously described synapsin III (Syn III) as a synaptic phosphoprotein that controls dopamine release in cooperation with α-synuclein (aSyn). Moreover, we found that in Parkinson's disease (PD), Syn III also participates in aSyn aggregation and toxicity. Our recent observations point to threo-methylphenidate (MPH...

journal_title：ChemMedChem

authors： Casiraghi A,Longhena F,Straniero V,Faustini G,Newman AH,Bellucci A,Valoti E

更新日期：2020-07-20 00:00:00

abstract：:The first series of 2'-substituted 2-(3'-carboxybicyclo[1.1.1]pentyl)glycine derivatives, (2R)- and (2S)-(2',2'-dichloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (10) and (11), and 2-(2'-chloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (12) were synthesized and evaluated as mGluR ligands. Compounds 11 and 12 were shown to ...

journal_title：ChemMedChem

authors： Pellicciari R,Filosa R,Fulco MC,Marinozzi M,Macchiarulo A,Novak C,Natalini B,Hermit MB,Nielsen S,Sager TN,Stensbøl TB,Thomsen C

更新日期：2006-03-01 00:00:00

abstract：:2-Azetidinones, commonly known as beta-lactams, are well-known heterocyclic compounds. Herein we described the synthesis and biological evaluation of a series of novel beta-lactams. In vitro inhibition assays against HDAC isoforms showed an interesting isoform-selectivity of these compounds towards HDAC6 and HDAC8. Th...

journal_title：ChemMedChem

authors： Galletti P,Quintavalla A,Ventrici C,Giannini G,Cabri W,Penco S,Gallo G,Vincenti S,Giacomini D

更新日期：2009-12-01 00:00:00

abstract：:Herein we describe the synthesis and conformational analysis of a series of bicyclic thymidine derivatives and their evaluation as inhibitors of thymidine monophosphate kinase from Mycobacterium tuberculosis (TMPKmt), based on previously discovered bicyclic sugar nucleosides. With a K(i) value of 2.3 microm, 1-[3-amin...

journal_title：ChemMedChem

authors： Van Daele I,Munier-Lehmann H,Hendrickx PM,Marchal G,Chavarot P,Froeyen M,Qing L,Martins JC,Van Calenbergh S

更新日期：2006-10-01 00:00:00

abstract：:Human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis belong to a group of infectious diseases known as neglected tropical diseases and are induced by infection with protozoan parasites named trypanosomatids. Drugs in current use have several limitations, and therefore new candidate drugs are required...

journal_title：ChemMedChem

authors： Dichiara M,Marrazzo A,Prezzavento O,Collina S,Rescifina A,Amata E

更新日期：2017-08-22 00:00:00

abstract：:We developed new 10 B carriers for boron neutron capture therapy (BNCT) that can effectively transport and accumulate boron clusters into cells. These carriers consist of a lipopeptide, mercaptoundecahydrododecaborate (BSH), and a disulfide linker. The carriers were conceived according to the structure of pepducin, a ...

journal_title：ChemMedChem

authors： Isono A,Tsuji M,Sanada Y,Matsushita A,Masunaga S,Hirayama T,Nagasawa H

更新日期：2019-04-17 00:00:00

abstract：:AFMC-AIMECS meetings are internationally organized biannually by the Asian Federation for Medicinal Chemistry (AFMC) and are focused on recent studies in drug discovery and development both in academia and industry. Member organizations of the AFMC are the Pharmaceutical Society of Japan, the Chinese Pharmaceutical As...

journal_title：ChemMedChem

authors： Olgac A,Yalcin I,Aki-Yalcin E

更新日期：2020-01-07 00:00:00

abstract：:Members of the Eph receptor tyrosine kinase family play essential roles in the pathogenesis of cancer and are therefore promising candidates for molecular imaging by positron emission tomography (PET), for example. In this regard, radiochemical access to novel PET radiotracers derived from potent inhibitors that targe...

journal_title：ChemMedChem

authors： Mamat C,Mosch B,Neuber C,Köckerling M,Bergmann R,Pietzsch J

更新日期：2012-11-01 00:00:00

abstract：:For (64) Cu radiolabeling of biomolecules to be used as in vivo positron emission tomography (PET) imaging agents, various chelators are commonly applied. It has not yet been determined which of the most potent chelators--NODA-GA ((1,4,7-triazacyclononane-4,7-diyl)diacetic acid-1-glutaric acid), CB-TE2A (2,2'-(1,4,8,1...

journal_title：ChemMedChem

authors： Litau S,Seibold U,Vall-Sagarra A,Fricker G,Wängler B,Wängler C

更新日期：2015-07-01 00:00:00

abstract：:Schistosomiasis is a neglected parasitic disease that affects more than 265 million people worldwide and for which the control strategy relies on mass treatment with only one drug: praziquantel. Based on the 3-chlorobenzothiophene-2-hydroxamic acid J1075, a series of hydroxamic acids with different scaffolds were prep...

journal_title：ChemMedChem

authors： Bayer T,Chakrabarti A,Lancelot J,Shaik TB,Hausmann K,Melesina J,Schmidtkunz K,Marek M,Erdmann F,Schmidt M,Robaa D,Romier C,Pierce RJ,Jung M,Sippl W

更新日期：2018-08-10 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：:The histone methyltransferase SET7/9 methylates not only histone but also non-histone proteins as substrates, and therefore, SET7/9 inhibitors are considered candidates for the treatment of diseases. Previously, our group identified cyproheptadine, used clinically as a serotonin receptor antagonist and histamine recep...

journal_title：ChemMedChem

authors： Hirano T,Fujiwara T,Niwa H,Hirano M,Ohira K,Okazaki Y,Sato S,Umehara T,Maemoto Y,Ito A,Yoshida M,Kagechika H

更新日期：2018-08-10 00:00:00

abstract：:Targeted photodynamic therapy is a new promising therapeutic strategy to overcome growing problems in contemporary medicine, such as drug toxicity and drug resistance. A series of erlotinib-zinc(II) phthalocyanine conjugates were designed and synthesized. Compared with unsubstituted zinc(II) phthalocyanine, these conj...

journal_title：ChemMedChem

authors： Zhang FL,Huang Q,Liu JY,Huang MD,Xue JP

更新日期：2015-02-01 00:00:00

abstract：:Nuclear magnetic resonance (NMR) spectroscopy is a valuable technique for ligand screening, because it exhibits high specificity toward chemical structure and interactions. Dissolution dynamic nuclear polarization (DNP) is a recent advance in NMR methodology that enables the creation of non-equilibrium spin states, wh...

journal_title：ChemMedChem

authors： Min H,Sekar G,Hilty C

更新日期：2015-09-01 00:00:00

abstract：:The molecular hybridization of different compounds with known pharmacological activity is a particularly prominent approach for the design of potential drugs with improved pharmacokinetic profiles. Much attention over the last decade has been focused on the synthesis of hybrid structures with a nitric oxide (NO)-donor...

journal_title：ChemMedChem

authors： Fershtat LL,Makhova NN

更新日期：2017-05-09 00:00:00

abstract：:Salecan is a water-soluble bacterial polysaccharide consisting of glucopyranosyl units linked by α-1,3 and β-1,3 glycosidic bonds. salecan is suitable for the development of hydrogels for biomedical applications, given its outstanding physicochemical and biological profiles. In this study we designed a new semi-interp...

journal_title：ChemMedChem

authors： Qi X,Li J,Wei W,Su T,Zuo G,Pan X,Zhang J,Dong W

更新日期：2017-01-20 00:00:00

abstract：:In the present review the crucial role of the guanidinium functional group in facilitating the transport of dendritic polymers through liposomal and cell membranes is discussed, along with other structural features of guanidinylated dendritic polymers that fine-tune their transport properties, and even determine their...

journal_title：ChemMedChem

authors： Theodossiou TA,Pantos A,Tsogas I,Paleos CM

更新日期：2008-11-01 00:00:00

abstract：:Vascular endothelial growth factor receptor 2 (VEGFR2) has been proven to play a major role in the regulation of tumor angiogenesis. A series of novel glycyrrhetic acid derivatives were synthesized and evaluated for their VEGFR2 inhibitory activity as well as their antiproliferative properties against four cancer cell...

journal_title：ChemMedChem

authors： Yan TL,Bai LF,Zhu HL,Zhang WM,Lv PC

更新日期：2017-07-06 00:00:00

abstract：:Cholesterol esterase (CEase), a serine hydrolase thought to be involved in atherogenesis and thus coronary heart disease, is considered as a target for inhibitor development. We investigated recombinant human and murine CEases with a new fluorometric assay in a structure-activity relationship study of a small library ...

journal_title：ChemMedChem

authors： Dato FM,Sheikh M,Uhl RZ,Schüller AW,Steinkrüger M,Koch P,Neudörfl JM,Gütschow M,Goldfuss B,Pietsch M

更新日期：2018-09-06 00:00:00

abstract：:The CXCR3 receptor, a class A G protein-coupled receptor (GPCR), is involved in the regulation and trafficking of various immune cells. CXCR3 antagonists have been proposed to be beneficial for the treatment of a wide range of disorders including but not limited to inflammatory and autoimmune diseases. The structure-b...

journal_title：ChemMedChem

authors： Admas TH,Bernat V,Heinrich MR,Tschammer N

更新日期：2016-03-17 00:00:00

abstract：:Herbal medicines (HMs) are an important source of drugs. In this study, an efficient strategy integrating ultrafiltration LC-MS, microplate bioassays, and molecular docking was proposed to screen high-potency enzyme inhibitors from HMs. Using this strategy, the structure-activity relationships (SARs) including binding...

journal_title：ChemMedChem

authors： Song HP,Wang H,Liang JX,Qian C,Wu SQ,Xu WJ,Wu B,Liu XG,Li P,Yang H

更新日期：2016-12-06 00:00:00

abstract：:Various structurally modified analogues of FR235222 (1), a natural tetrapeptide inhibitor of mammalian histone deacetylases, were prepared in a convergent approach. The design of the compounds was aimed to investigate the effect of structural modifications of the tetrapeptide core involved in enzyme binding in order t...

journal_title：ChemMedChem

authors： Gomez-Paloma L,Bruno I,Cini E,Khochbin S,Rodriquez M,Taddei M,Terracciano S,Sadoul K

更新日期：2007-10-01 00:00:00

abstract：:The tropical diseases human African trypanosomiasis, Chagas disease, and the various forms of leishmaniasis are caused by parasites of the family of trypanosomatids. These protozoa possess a unique redox metabolism based on trypanothione and trypanothione reductase (TR), making TR a promising drug target. We report th...

journal_title：ChemMedChem

authors： De Gasparo R,Brodbeck-Persch E,Bryson S,Hentzen NB,Kaiser M,Pai EF,Krauth-Siegel RL,Diederich F

更新日期：2018-05-08 00:00:00

abstract：:Six phosphorescent (2-phenyl)pyridine (ppy) gold(III) 2,4,6-tris(trifluoromethyl)phenyl (FMes) complexes were synthesized and investigated for their anticancer potential. The compounds demonstrated strong antiproliferative activity, with EC50 values in the low micromolar range, along with significant accumulation in H...

journal_title：ChemMedChem

authors： Rubbiani R,Zehnder TN,Mari C,Blacque O,Venkatesan K,Gasser G

更新日期：2014-12-01 00:00:00

abstract：:The protozoan parasite Plasmodium falciparum causes the most severe and prevailing form of malaria in sub-Saharan Africa. Previously, we identified the plasmodial lactate transporter, PfFNT, a member of the microbial formate-nitrite transporter family, as a novel antimalarial drug target. With the pentafluoro-3-hydrox...

journal_title：ChemMedChem

authors： Walloch P,Hansen C,Priegann T,Schade D,Beitz E

更新日期：2020-12-18 00:00:00