Amides as bioisosteres of triazole-based geranylgeranyl diphosphate synthase inhibitors.

abstract：:1,2,3-Triazole-, arylamino- and thio-substituted naphthoquinones (24, 8, and 2 representatives, respectively) were synthesized in moderate yields and evaluated against several human cancer cell lines (blood, ovarian, breast, central nervous system, colon, and prostate cancers and melanoma), showing, for some of them, ...

journal_title：Bioorganic & medicinal chemistry

authors： da Cruz EH,Hussene CM,Dias GG,Diogo EB,de Melo IM,Rodrigues BL,da Silva MG,Valença WO,Camara CA,de Oliveira RN,de Paiva YG,Goulart MO,Cavalcanti BC,Pessoa C,da Silva Júnior EN

更新日期：2014-03-01 00:00:00

abstract：:Histamine H(1) and serotonin 5-HT(2A) receptors present in the CNS have been implicated in various neuropsychiatric disorders. 9-Aminomethyl-9,10-dihydroanthracene (AMDA), a conformationally constrained diarylalkyl amine derivative, has affinity for both of these receptors. A structure-affinity relationship (SAFIR) st...

journal_title：Bioorganic & medicinal chemistry

authors： Shah JR,Mosier PD,Roth BL,Kellogg GE,Westkaemper RB

更新日期：2009-09-15 00:00:00

abstract：:Targeting Hsp90-Cdc37 protein-protein interaction (PPI) is becoming an alternative approach for future anti-cancer drug development. We previously reported the discovery of an eleven-residue peptide (Pep-1) with micromolar activity for the disruption of Hsp90-Cdc37 PPI. Efforts to improve upon the Pep-1 led to the dis...

journal_title：Bioorganic & medicinal chemistry

authors： Wang L,Li L,Fu WT,Jiang ZY,You QD,Xu XL

更新日期：2017-01-01 00:00:00

abstract：:Colorectal cancer is the third and fourth leading cause of cancer in males and females, respectively. Flavonoids, including chalcones, are secondary metabolites in plants that exhibit diverse biological activities, including antibacterial, antimalarial, and antitumor activities. In order to find potent and novel chemo...

journal_title：Bioorganic & medicinal chemistry

authors： Shin SY,Yoon H,Hwang D,Ahn S,Kim DW,Koh D,Lee YH,Lim Y

更新日期：2013-11-15 00:00:00

abstract：:The development of remedies against the Alzheimer's disease (AD) is one of the biggest challenges in medicinal chemistry nowadays. Although not completely understood, there are several strategies fighting this disease or at least bringing some relief. During the progress of AD, the level of acetylcholine (ACh) decreas...

journal_title：Bioorganic & medicinal chemistry

authors： Schwarz S,Lucas SD,Sommerwerk S,Csuk R

更新日期：2014-07-01 00:00:00

abstract：:A series of phenyl N-mustard-9-anilinoacridine conjugates via a carbamate or carbonate linker was synthesized for antitumor evaluation. The carbamate or carbonate linker is able to lower the reactivity of the phenyl N-mustard pharmacophore and thus, these conjugates are rather chemically stable. The in vitro studies r...

journal_title：Bioorganic & medicinal chemistry

authors： Kapuriya N,Kapuriya K,Dong H,Zhang X,Chou TC,Chen YT,Lee TC,Lee WC,Tsai TH,Naliapara Y,Su TL

更新日期：2009-02-01 00:00:00

abstract：:The interest in biological functions (benefits or toxics effects) of vanadium species has grown enormously in recent years. In this work, different spectroscopic methods were applied to study the effects of the interaction of vanadyl and vanadate species with bovine serum albumin (BSA), considered as the most abundant...

journal_title：Bioorganic & medicinal chemistry

authors： Ferrer EG,Bosch A,Yantorno O,Baran EJ

更新日期：2008-04-01 00:00:00

abstract：:5-Bromouracil ((Br)U) was incorporated into three types of synthetic RNA and the products of the photoirradiated (Br)U-containing RNAs were investigated using HPLC and MS analysis. The photoirradiation of r(GCA(Br)UGC)(2) and r(CGAA(Br)UUGC)/r(GCAAUUCG) in A-form RNA produced the corresponding 2'-keto adenosine ((keto...

journal_title：Bioorganic & medicinal chemistry

authors： Morinaga H,Kizaki S,Takenaka T,Kanesato S,Sannohe Y,Tashiro R,Sugiyama H

更新日期：2013-01-15 00:00:00

abstract：:Histone H3 methylation plays an important role in regulating gene expression. In histones in general, this mark is dynamically regulated via various demethylases, which found to control cell fate decisions as well as linked to several diseases, including neurological and cancer. Despite major progress in studying meth...

journal_title：Bioorganic & medicinal chemistry

authors： Jbara M,Guttmann-Raviv N,Maity SK,Ayoub N,Brik A

更新日期：2017-09-15 00:00:00

abstract：:A new series of 2-thioether-benzothiazoles has been synthesized and evaluated for JNK inhibition. The SAR studies led to the discovery of potent, allosteric JNK inhibitors with selectivity against p38. ...

journal_title：Bioorganic & medicinal chemistry

authors： De SK,Chen LH,Stebbins JL,Machleidt T,Riel-Mehan M,Dahl R,Chen V,Yuan H,Barile E,Emdadi A,Murphy R,Pellecchia M

更新日期：2009-04-01 00:00:00

abstract：:Cell division cycle 7 (Cdc7) is a serine/threonine kinase that plays important roles in the regulation of DNA replication process. A genetic study indicates that Cdc7 inhibition can induce selective tumor-cell death in a p53-dependent manner, suggesting that Cdc7 is an attractive target for the treatment of cancers. I...

journal_title：Bioorganic & medicinal chemistry

authors： Kurasawa O,Oguro Y,Miyazaki T,Homma M,Mori K,Iwai K,Hara H,Skene R,Hoffman I,Ohashi A,Yoshida S,Ishikawa T,Cho N

更新日期：2017-04-01 00:00:00

abstract：:Cyclic D- and L-4-aminothreose were synthesised from ethyl D- and L-tartrate, respectively. D-aminothreose was a potent inhibitor of alpha-glucosidase and of alpha-mannosidase. From the glycosidase inhibition potencies of the four 4-amino-4-deoxy-tetroses, the contribution of binding of each functionality of the 5 and...

journal_title：Bioorganic & medicinal chemistry

authors： Chevrier C,Defoin A,Tarnus C

更新日期：2007-06-15 00:00:00

abstract：:A quantitative structure-activity analysis of binding affinity of a series of 30 steroids for corticosteroid-binding globulin was performed using Wang-Ford charges of the non-hydrogen common atoms obtained from molecular electrostatic potential surface of AM1 optimized energy-minimized geometries of the compounds. Att...

journal_title：Bioorganic & medicinal chemistry

authors： De K,Sengupta C,Roy K

更新日期：2004-06-15 00:00:00

abstract：:Cells have evolved complex biochemical pathways for DNA interstrand crosslink (ICL) removal. Despite the chemotherapeutic importance of ICL repair, there have been few attempts to identify which mechanistic DNA repair inhibitor actually inhibits ICL repair. To identify such compounds, a new and robust ICL repair assay...

journal_title：Bioorganic & medicinal chemistry

authors： Fujii N,Evison BJ,Actis ML,Inoue A

更新日期：2015-11-01 00:00:00

abstract：:Three different photoprobes were synthesized to label beta-glucosidases; one probe was based on glucose, two probes on the iminosugar deoxynojirimycin. The affinity of the probes for three different beta-glucosidases was determined. Furthermore, their labeling efficiencies, binding specificities through competition wi...

journal_title：Bioorganic & medicinal chemistry

authors： van Scherpenzeel M,van den Berg RJ,Donker-Koopman WE,Liskamp RM,Aerts JM,Overkleeft HS,Pieters RJ

更新日期：2010-01-01 00:00:00

abstract：:Mycobacterium tuberculosis glutamate racemase is an essential enzyme involved in peptidoglycan synthesis and conserved in most bacteria. Small molecule inhibitors were reported on other bacterial species whereas in M. tuberculosis it wasn't explored much. In this study we have screened in house compound library using ...

journal_title：Bioorganic & medicinal chemistry

authors： Malapati P,Siva Krishna V,Nallangi R,Meda N,Reshma Srilakshmi R,Sriram D

更新日期：2018-01-01 00:00:00

abstract：:A series of anacardic acid analogues possessing different side chains viz. phenolic, branched, and alicyclic were synthesized and their antibacterial activity tested against methicillin-resistant Staphylococcus aureus (MRSA). The maximum activity against this bacterium occurred with the branched side-chain analogue, 6...

journal_title：Bioorganic & medicinal chemistry

authors： Green IR,Tocoli FE,Lee SH,Nihei K,Kubo I

更新日期：2007-09-15 00:00:00

abstract：:The kainoids are a class of excitatory and excitotoxic pyrrolidine dicarboxylates that act at ionotropic glutamate receptors. The kainoids bind kainate receptors with high affinity and, while binding affinity is lower at AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptors, they are active in func...

journal_title：Bioorganic & medicinal chemistry

authors： Carcache LM,Rodriguez J,Rein KS

更新日期：2003-02-20 00:00:00

abstract：:Following our studies on structure-activity relationships of anti-rhinovirus chromene and chroman derivatives, we designed and synthesized new series of 3-phenylalkyl-2H-chromenes and -chromans bearing differently sized, aliphatic linker chains between the two cycles. The cytotoxicity and the antiviral activity of the...

journal_title：Bioorganic & medicinal chemistry

authors： Conti C,Proietti Monaco L,Desideri N

更新日期：2017-04-01 00:00:00

abstract：:Compounds from a wide variety of structural classes inhibit HIV-1 integrase. However, a single unified understanding of the relationship between the structures and activities of these compounds still eludes researchers. We report herein the development of QSAR models for integrase inhibition. The genetic function appr...

journal_title：Bioorganic & medicinal chemistry

authors： Yuan H,Parrill AL

更新日期：2002-12-01 00:00:00

abstract：:Xestoquinone isolated from a marine sponge binds to skeletal muscle myosin and inhibits its Ca(2+) ATPase activity. In this study, we first examined xestoquinone and its analogues to assess the relationships between structure and myosin Ca(2+) ATPase inhibitory activity. On the basis of the resultant data, we then des...

journal_title：Bioorganic & medicinal chemistry

authors： Nakamura M,Kakuda T,Oba Y,Ojika M,Nakamura H

更新日期：2003-07-17 00:00:00

abstract：:Liposomes, capable of temperature-triggered content release at the site of interest, can be of great importance for imaging and therapy of tumors. The delivery of imaging agents or therapeutics can be improved by application of liposomes with a gel-to-liquid phase-transition temperature suitable for mild hyperthermia ...

journal_title：Bioorganic & medicinal chemistry

authors： Djanashvili K,ten Hagen TL,Blangé R,Schipper D,Peters JA,Koning GA

更新日期：2011-02-01 00:00:00

abstract：:A novel artificial peptide named HPH-Pep, comprising a pyridine and two histidine units, was synthesized. The HPH-Pep-CuII complex had unique pentacoordinated structure as shown by X-ray crystallography and exhibited superoxide-scavenging activity as indicated by ESR spectroscopy. The superoxide-quenching profile of H...

journal_title：Bioorganic & medicinal chemistry

authors： Otsuka M,Satake H,Murakami S,Doi M,Ishida T,Shibasaki M,Sugiura Y

更新日期：1996-10-01 00:00:00

abstract：:The aim of this work was to synthesize a set of heterocyclic derivatives of lupane, lup-20(29)-ene, and 18α-oleanane, and to investigate their cytotoxic activities. Some of those heterocycles were previously known in the oleanane (allobetulin) group; however, to our knowledge the syntheses and biological activities of...

journal_title：Bioorganic & medicinal chemistry

authors： Urban M,Vlk M,Dzubak P,Hajduch M,Sarek J

更新日期：2012-06-01 00:00:00

abstract：:Using hydroxy-/dihydroxybenzoic acids as leads, a series of methyl, ethyl and iso-propyl esters of 4-hydroxy-benzoic acid, 2,4-, 2,5-, 2,6-, 3,4-, and 3,5-dihydroxybenzoic acids and of coumaric acid, were obtained and investigated for the inhibition of six mammalian carbonic anhydrase (CA, EC 4.2.1.1) isoforms, that i...

journal_title：Bioorganic & medicinal chemistry

authors： Carta F,Vullo D,Maresca A,Scozzafava A,Supuran CT

更新日期：2013-03-15 00:00:00

abstract：:Opioid compounds with mixed micro agonist/delta antagonist properties could be used as analgesics with low propensity to induce tolerance and dependence. Here we report the synthesis of a new designed multiple ligand deriving from the micro selective agonist endomorphin-2 and the delta selective antagonist pharmacopho...

journal_title：Bioorganic & medicinal chemistry

authors： Salvadori S,Trapella C,Fiorini S,Negri L,Lattanzi R,Bryant SD,Jinsmaa Y,Lazarus LH,Balboni G

更新日期：2007-11-15 00:00:00

abstract：:A series of non-covalent piperidine-containing peptidyl derivatives with various substituents at side chains of different residues were designed, synthesized and evaluated as proteasome inhibitors. After proteasome inhibitory evaluations of all the synthesized target compounds, selected ones were tested for their anti...

journal_title：Bioorganic & medicinal chemistry

authors： Zhao Y,Xu L,Zhang J,Zhang M,Lu J,He R,Xi J,Zhuang R,Li J,Zhou Y

更新日期：2021-01-01 00:00:00

abstract：:We report the synthesis and properties of oligonucleotides incorporating N(6)-[N-(pyren-1-ylmethyl)carbamoyl]-deoxyadenosine (dA(pymcm)). We designed the ODN which incorporated two consecutive dA(pymcm) residues. It was revealed that on hybridization with the target DNA and RNA oligomers, the fluorescence spectra of O...

journal_title：Bioorganic & medicinal chemistry

authors： Seio K,Mizuta M,Tasaki K,Tamaki K,Ohkubo A,Sekine M

更新日期：2008-09-01 00:00:00

abstract：:This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and good oral bioavailability in man. Optimisation of the preclinical profi...

journal_title：Bioorganic & medicinal chemistry

authors： Rawson DJ,Ballard S,Barber C,Barker L,Beaumont K,Bunnage M,Cole S,Corless M,Denton S,Ellis D,Floc'h M,Foster L,Gosset J,Holmwood F,Lane C,Leahy D,Mathias J,Maw G,Million W,Poinsard C,Price J,Russel R,Street S

更新日期：2012-01-01 00:00:00

abstract：:Valinol is part of numerous pharmaceuticals and has various other important applications. Optically pure valinol (ee >99%) was prepared employing different ω-transaminases from the corresponding prochiral hydroxy ketone. By the choice of the enzyme the (R)- as well as the (S)-enantiomer were accessible. Reductive amin...

journal_title：Bioorganic & medicinal chemistry

authors： Fuchs CS,Simon RC,Riethorst W,Zepeck F,Kroutil W

更新日期：2014-10-15 00:00:00