Interaction of binuclear xylylthiolato(2,2',2"-terpyridine)platinum(II) complexes with DNA.

abstract：:With an insight that ligands possessing a N2S2 tetradentate array of donor atoms serve as ideal bifunctional chelating agents (BFCA) in the radiolabeling of target-specific agents, 5-hydroxy-3,7-diazanonan-1,9-dithiol (DAHPES) with a derivatizable substituent in the form of a hydroxyl group in the backbone was synthes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Das T,Banerjee S,Samuel G,Bapat K,Subramanian S,Pillai MR,Venkatesh M

更新日期：2006-11-15 00:00:00

abstract：:The histone methylation on lysine residues is one of the most studied post-translational modifications, and its aberrant states have been associated with many human diseases. In 2012, Kruidenier et al. reported GSK-J1 as a selective Jumonji H3K27 demethylase (JMJD3 and UTX) inhibitor. However, there is limited informa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hu J,Wang X,Chen L,Huang M,Tang W,Zuo J,Liu YC,Shi Z,Liu R,Shen J,Xiong B

更新日期：2016-02-01 00:00:00

abstract：:A series of isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones were synthesized as potent inhibitors against Pim-1 and Pim-2 kinases. The structure-activity-relationship studies started from a high-throughput screening hit and was guided by molecular modeling of inhibitors in the active site of Pim-1 kinase. Installing a hyd...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tong Y,Stewart KD,Thomas S,Przytulinska M,Johnson EF,Klinghofer V,Leverson J,McCall O,Soni NB,Luo Y,Lin NH,Sowin TJ,Giranda VL,Penning TD

更新日期：2008-10-01 00:00:00

abstract：:Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK1 and NK2 antagonists. ZD6021 inhibited binding of [3H]-NKA or [3H]-SP to human NK1 and NK2 receptors, with high-affinity (K(i)=0.12 and 0.62nM, respectively). In functi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bernstein PR,Aharony D,Albert JS,Andisik D,Barthlow HG,Bialecki R,Davenport T,Dedinas RF,Dembofsky BT,Koether G,Kosmider BJ,Kirkland K,Ohnmacht CJ,Potts W,Rumsey WL,Shen L,Shenvi A,Sherwood S,Stollman D,Russell K

更新日期：2001-10-22 00:00:00

abstract：:Phosphoglycolo amidoxime and phosphoglycolo hydrazide, two new derivatives of phosphoglycolic acid, were synthesised and successfully tested as selective competitive inhibitors of class II FBP-aldolases. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fonvielle M,Weber P,Dabkowska K,Therisod M

更新日期：2004-06-07 00:00:00

abstract：:Structure-activity relationships (SAR) of fused 1,2,4-triazolo[1,5-c ]pyrimidine were performed. Various substituents were introduced into the heterocyclic ring to improve the potency of adenosine A(3) receptor binding affinity and A(3)-selectivity against other subtypes. Potent and selective A(3) receptor antagonists...

journal_title：Bioorganic & medicinal chemistry letters

authors： Okamura T,Kurogi Y,Hashimoto K,Sato S,Nishikawa H,Kiryu K,Nagao Y

更新日期：2004-07-16 00:00:00

abstract：:The importance of protein binding cavity volume (PCV) and ligand volume (LV) in rigid and flexible docking has been studied in 48 protein-ligand complexes belonging to eight protein families. In continuation of our earlier study on protein flexibility in relationship to PCV and LV, this study analyzes the importance o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saranya N,Jeyakanthan J,Selvaraj S

更新日期：2012-12-15 00:00:00

abstract：:Sodium channel blocking, anticonvulsant activity, and sigma (sigma) binding of selected leads in a series of alpha-amino amide anticonvulsants were examined. While anticonvulsant compounds were always endowed with low micromolar sodium (Na+) channel site-2 binding, compounds with low site-2 Na+ channel affinity failed...

journal_title：Bioorganic & medicinal chemistry letters

authors： Pevarello P,Bonsignori A,Caccia C,Amici R,McArthur RA,Fariello RG,Salvati P,Varasi M

更新日期：1999-09-06 00:00:00

abstract：:In continuation of our efforts toward hit identification and optimization for a B-Raf kinase project, we have employed a scaffold hopping strategy. The original HTS hit scaffold pyrazolo[1,5-a]pyrimidine was replaced with different thienopyrimidine and thienopyridine scaffolds to append the optimal pharmacophore moiet...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gopalsamy A,Shi M,Hu Y,Lee F,Feldberg L,Frommer E,Kim S,Collins K,Wojciechowicz D,Mallon R

更新日期：2010-04-15 00:00:00

abstract：:In the course of our studies of the structure-activity relationships of himbacine 1, a potent antagonist of the M(2) subtype of muscarinic receptor, the four title compounds, 2, ent-2, 3, and ent-3, were synthesized with a highly stereoselective intermolecular Diels-Alder reaction of tetrahydroisobenzofuran 4 with ach...

journal_title：Bioorganic & medicinal chemistry letters

authors： Takadoi M,Yamaguchi K,Terashima S

更新日期：2002-11-18 00:00:00

abstract：:The halogenated and oxidized derivatives (1a-1e, 1a'-1c', 2a-2d, 2a'-2b', 3a-3e, 3' and 3a'-3b') of schizandrin (1), schizandrin B (2) and schisanhenol (3) were synthesized. The hepatoprotective effects of these dibenzocyclooctadiene lignan analogues against CCl4-induced injury were preliminarily evaluated. Most of th...

journal_title：Bioorganic & medicinal chemistry letters

authors： He T,Wang QY,Shi JZ,Fan TY,Yan C,Huang LJ,Liu S,Hao XJ,Mu SZ

更新日期：2014-04-01 00:00:00

abstract：:Novel, metabolically stable and centrally acting TRH analogues with substituted pyridinium moieties replacing the [His(2)] residue of the endogenous peptide were prepared by solid-phase Zincke reaction. The 1,4-dihydropyridine prodrugs of these analogues obtained after reducing the pyridinium moiety were able to reach...

journal_title：Bioorganic & medicinal chemistry letters

authors： Prokai-Tatrai K,Perjési P,Zharikova AD,Li X,Prokai L

更新日期：2002-08-19 00:00:00

abstract：:The lead optimisation of the diaminopyrimidine carboxamide series of spleen tyrosine kinase inhibitors is described. The medicinal chemistry strategy was focused on optimising the human whole blood activity whilst achieving a sufficient margin over liability kinases and hERG activity. GSK143 is a potent and highly sel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liddle J,Atkinson FL,Barker MD,Carter PS,Curtis NR,Davis RP,Douault C,Dickson MC,Elwes D,Garton NS,Gray M,Hayhow TG,Hobbs CI,Jones E,Leach S,Leavens K,Lewis HD,McCleary S,Neu M,Patel VK,Preston AG,Ramirez-Molina

更新日期：2011-10-15 00:00:00

abstract：:A series of pyrrolo[3,2,1-ij]quinoline derivatives was synthesized, evaluated for their activity against the 5-HT2c and 5-HT2a, receptors and found to be agonists at 5-HT2c with selectivity over 5-HT2a. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Isaac M,Slassi A,O'Brien A,Edwards L,MacLean N,Bueschkens D,Lee DK,McCallum K,De Lannoy I,Demchyshyn L,Kamboj R

更新日期：2000-05-01 00:00:00

abstract：:A series of novel oxime-containing pyrazole derivatives were synthesized by the reaction of ethyl 3-phenyl-1H-pyrazole-5-carboxylate derivatives and 2-bromo-1-phenylethanone followed by the reaction with hydroxylamine hydrochloride. The structures were determined by IR, (1)H NMR, HRMS, and X-ray analysis. A dose- and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng LW,Li Y,Ge D,Zhao BX,Liu YR,Lv HS,Ding J,Miao JY

更新日期：2010-08-15 00:00:00

abstract：:Analogs of the potent antifungal agent, bengazole A, were prepared and evaluated against Candida spp. in both microbroth dilution and disk diffusion assays. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mulder RJ,Shafer CM,Dalisay DS,Molinski TF

更新日期：2009-06-01 00:00:00

abstract：:P2X purinoceptors are ligand-gated ion channels whose endogenous ligand is ATP. Both the P2X(3) and P2X(2/3) receptor subtypes have been shown to play an important role in the regulation of sensory function and dual P2X(3)/P2X(2/3) antagonists offer significant potential for the treatment of pain. A high-throughput sc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carter DS,Alam M,Cai H,Dillon MP,Ford AP,Gever JR,Jahangir A,Lin C,Moore AG,Wagner PJ,Zhai Y

更新日期：2009-03-15 00:00:00

abstract：:6-Arylamino-5,8-quinolinediones 3 and 7-arylamino-5,8-isoquinolinediones 4 were synthesized as inhibitors of endothelium-dependent vasorelaxation. The quinones inhibited the vasorelaxation of rat aorta with the endothelium. Among them, the quinones 3a, 3b, 3f, 4b, 4d and 4g strongly inhibited the vasorelaxation. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ryu CK,Jung SH,Lee JA,Kim HJ,Lee SH,Chung JH

更新日期：1999-09-06 00:00:00

abstract：:The shift in apparent IC(50) that attends addition of serum proteins to in vitro cellular, enzymatic, and receptor binding assays can be used to determine the dissociation constant for compound-serum protein complexes. We show here that a simple linear relationship exists between the apparent IC(50) in the presence of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rusnak DW,Lai Z,Lansing TJ,Rhodes N,Gilmer TM,Copeland RA

更新日期：2004-05-03 00:00:00

abstract：:A new halicyclamine derivative, tetradehydrohalicyclamine B (1), was isolated from the marine sponge Acanthostrongylophora ingens, along with halicyclamine B (2) as proteasome inhibitors. Compound 1 is the second example found to have a pyridinium ring in the halicyclamine family. Although the relative configuration o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kato H,El-Desoky AH,Takeishi Y,Nehira T,Angkouw ED,Mangindaan REP,de Voogd NJ,Tsukamoto S

更新日期：2019-01-01 00:00:00

abstract：:Herein we report the preparation of 3,4-dibenzylfurans and some oxidized derivatives with lignan backbone. The compounds were prepared using the Friedel-Crafts reaction with BF3 etherate as catalyst, demethylation with iodocyclohexane, acetylation and oxidation reactions. The antimicrobial activity was evaluated throu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tufano I,Buommino E,Iesce MR,De Filippis A,Grieco P,Lembo F,DellaGreca M

更新日期：2020-09-01 00:00:00

abstract：:In the search of molecules that can serve as leads in the design of a new drug for the treatment of Chagas' disease, we found that some brevifolin carboxylate derivatives isolated from Geranium bellum Rose, inactivate triosephosphate isomerase from Trypanosoma cruzi (TcTIM) in a species-specific manner. After spectros...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gayosso-De-Lucio J,Torres-Valencia M,Rojo-Domínguez A,Nájera-Peña H,Aguirre-López B,Salas-Pacheco J,Avitia-Domínguez C,Téllez-Valencia A

更新日期：2009-10-15 00:00:00

abstract：:New inhibitors have been designed for cdc2 kinase based on a multiple pseudosubstrate structure. The new inhibitors have three different structural components: 3,4-bis(indol-3-yl)maleimide, Ac-Cys-(Ser)-Pro-Lys-Lys-NHMe, and ethyloxy group between the two components. Inhibitory activities toward cdc2 and other protein...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sasaki S,Hashimoto T,Obana N,Yasuda H,Uehara Y,Maeda M

更新日期：1998-05-05 00:00:00

abstract：:Herein we describe the SAR of 1,5-biaryl pyrrole derivatives, with substituents in the 6-position of the benzoic acid moiety, as EP(1) receptor antagonists. Substitution at this position was well tolerated and led to the identification of several analogues with high affinity for the EP(1) receptor that displayed good ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hall A,Brown SH,Chessell IP,Chowdhury A,Clayton NM,Coleman T,Giblin GM,Hammond B,Healy MP,Johnson MR,Metcalf A,Michel AD,Naylor A,Novelli R,Spalding DJ,Sweeting J,Winyard L

更新日期：2007-02-15 00:00:00

abstract：:The synthesis of a 20 member 2-aminoimidazole/triazole pilot library is reported. Each member of the library was screened for its ability to inhibit or promote biofilm development of either Escherichia coli and Acinetobacter baumannii. From this screen, E. coli-selective 2-aminoimidazoles were discovered, with the bes...

journal_title：Bioorganic & medicinal chemistry letters

authors： Reed CS,Huigens RW 3rd,Rogers SA,Melander C

更新日期：2010-11-01 00:00:00

abstract：:A series of N-(1-methyl-1H-indol-3-yl)methyleneamines and eight new 3,3-diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized and screened for their antileishmanial activity against Leishmania major. 3,3-Diaryl-4-(1-methyl-1H-indol-3-yl)azetidin-2-ones have been synthesized by the Staudinger's ketene-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh GS,Al-Kahraman YM,Mpadi D,Yasinzai M

更新日期：2012-09-01 00:00:00

abstract：:A series of cis-3,4-disubstituted piperidines was synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. Compound 24 emerged with an attractive profile, possessing excellent binding (CCR2 IC(50)=3.4 nM) and functional antagonism (calcium flux IC(50)=2.0 nM and chemotaxis IC(50)=5.4 nM). Studies to ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cherney RJ,Nelson DJ,Lo YC,Yang G,Scherle PA,Jezak H,Solomon KA,Carter PH,Decicco CP

更新日期：2008-09-15 00:00:00

abstract：:A novel method to generate RNA binding D-peptide has been developed. To achieve the screening method, phage display was applied to "Mirrored" RNA (L-enantiomer of RNA). We have selected pre-miR21 as an initial screening target to demonstrate the method. The mirrored pre-miR-21 binding peptide sequences were successful...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sakamoto K,Otake K,Umemoto T

更新日期：2017-02-15 00:00:00

abstract：:A series of m-carborane derivatives was prepared based upon the structures of antiestrogenic drugs and their activities were evaluated by estrogen receptor alpha (ERalpha) binding assay and transactivation assay using human breast cancer cell line, MCF-7 cells. The m-carborane bisphenol 5 exhibited about a thousand ti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogawa T,Ohta K,Yoshimi T,Yamazaki H,Suzuki T,Ohta S,Endo Y

更新日期：2006-08-01 00:00:00

abstract：:Beta-2'-C-methyl purines (1, 2) are known inhibitors of hepatitis C virus (HCV). We herein report the synthesis, biological and enzymatic evaluation of their 5'-phosphoramidate ProTides. Described herein are seven l-alanine phosphoramidate derivatives with variations to the amino acid ester. The 1-naphthyl phosphorami...

journal_title：Bioorganic & medicinal chemistry letters

authors： McGuigan C,Perrone P,Madela K,Neyts J

更新日期：2009-08-01 00:00:00