Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists.

abstract：:Pyridine-based compounds have been playing a crucial role as agrochemicals or pesticides including fungicides, insecticides/acaricides and herbicides, etc. Since most of the agrochemicals listed in the Pesticide Manual were discovered through screening programs that relied on trial-and-error testing and new agrochemic...

journal_title：Bioorganic & medicinal chemistry

authors： Guan AY,Liu CL,Sun XF,Xie Y,Wang MA

更新日期：2016-02-01 00:00:00

abstract：:A novel series of '4-1' pentacyclic naphthalimides, where the chromophore consists of a naphthalimide moiety, fused to an imidazole ring containing an unfused aryl or heteroaryl ring, were synthesized and evaluated for in vitro antitumor activity. In general, the new derivatives showed an improved cytotoxic activity o...

journal_title：Bioorganic & medicinal chemistry

authors： Li F,Cui J,Guo L,Qian X,Ren W,Wang K,Liu F

更新日期：2007-08-01 00:00:00

abstract：:A protein-cleaving catalyst highly selective for a disease-related protein can be used as a catalytic drug. As the first protein-cleaving catalyst selective for a protein substrate, a catalyst for myoglobin (Mb) was designed by attaching the Cu(II) or Co(III) complex of cyclen to a binding site searched by a combinato...

journal_title：Bioorganic & medicinal chemistry

authors： Jeon JW,Son SJ,Yoo CE,Hong IS,Suh J

更新日期：2003-07-03 00:00:00

abstract：:Focused libraries of multi-substituted epidithiodiketopiperazines (ETP) were prepared and evaluated for efficacy of inhibiting the nucleocapsid protein function of the Feline Immunodeficiency Virus (FIV) as a model for HIV. This activity was compared and contrasted to observed toxicity utilising an in-vitro cell cultu...

journal_title：Bioorganic & medicinal chemistry

authors： Asquith CRM,Sil BC,Laitinen T,Tizzard GJ,Coles SJ,Poso A,Hofmann-Lehmann R,Hilton ST

更新日期：2019-09-15 00:00:00

abstract：:A series of 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives was synthesized and 13 of them were selected by the National Cancer Institute (NCI) and evaluated for their in vitro anticancer activity. Seven of the investigated compounds, 3i, 3j, 3k, 3o, 3p, 3q, and 3r, displayed high a...

journal_title：Bioorganic & medicinal chemistry

authors： Aboraia AS,Abdel-Rahman HM,Mahfouz NM,El-Gendy MA

更新日期：2006-02-15 00:00:00

abstract：:Theoretical and structural studies followed by the directed synthesis and in vitro biological tests lead us to novel noncovalent thrombin pseudopeptide inhibitors. We have incorporated an azapeptide scaffold into the central part of the classical tripeptide D-Phe-Pro-Arg inhibitor structure thus eliminating one stereo...

journal_title：Bioorganic & medicinal chemistry

authors： Zega A,Mlinsek G,Sepic P,Golic Grdadolnik S,Solmajer T,Tschopp TB,Steiner B,Kikelj D,Urleb U

更新日期：2001-10-01 00:00:00

abstract：:A series of eight N-2-phenylethylphosphonyl derivatives of glutamic acid was prepared to determine if the inhibitory potency of a phenylethylphosphonyl derivative of glutamic acid against prostate-specific membrane antigen (PSMA) could be improved through rational substitutions on the phenyl ring. The design of these ...

journal_title：Bioorganic & medicinal chemistry

authors： Wone DW,Rowley JA,Garofalo AW,Berkman CE

更新日期：2006-01-01 00:00:00

abstract：:Several analogues of (Z)-8-dodecenyl acetate (1a), the major pheromone component of the Oriental fruit moth, Cydia molesta, with chloroformate and lactone functional groups in place of the acetate moiety, were synthesized and investigated for their biological activity at four evaluation levels, i.e. by electroantennog...

journal_title：Bioorganic & medicinal chemistry

authors： Hoskovec M,Hovorka O,Kalinová B,Koutek B,Streinz L,Svatos A,Sebek P,Saman D,Vrkoc J

更新日期：1996-03-01 00:00:00

abstract：:Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets in cancer. Using NAD(+) as a substrate, they poly(ADP-ribosyl)ate TRF1 (regulating lengths of telomeres), NuMA (facilitating mitosis) and axin (in wnt/β-catenin signalling). Using molecular modelling and the structure o...

journal_title：Bioorganic & medicinal chemistry

authors： Paine HA,Nathubhai A,Woon EC,Sunderland PT,Wood PJ,Mahon MF,Lloyd MD,Thompson AS,Haikarainen T,Narwal M,Lehtiö L,Threadgill MD

更新日期：2015-09-01 00:00:00

abstract：:3-Metoxycarbonyl isoquinolone derivative 1 has been identified as a potent JNK inhibitor and significantly inhibited cardiac hypertrophy in a rat pressure-overload model. Herein, a series of isoquinolones with an imidazolylmethyl or a pyrazolylmethyl group at the 2-position were designed based on X-ray crystallographi...

journal_title：Bioorganic & medicinal chemistry

authors： Asano Y,Kitamura S,Ohra T,Itoh F,Kajino M,Tamura T,Kaneko M,Ikeda S,Igata H,Kawamoto T,Sogabe S,Matsumoto S,Tanaka T,Yamaguchi M,Kimura H,Fukumoto S

更新日期：2008-04-15 00:00:00

abstract：:For the purpose of rational modification of the TRH molecule, we were pursuing an approach that consists of two steps: (1) 'obligatory' replacement of histidine with glutamine in TRH and (2) the application of conformational constraints for putative bioactive conformation I stabilized by an intramolecular hydrogen bon...

journal_title：Bioorganic & medicinal chemistry

authors： Mazurov AA,Andronati SA,Korotenko TI,Sokolenko NI,Dyadenko AI,Shapiro YE,Gorbatyuk VYa,Voronina TA

更新日期：1997-11-01 00:00:00

abstract：:The preserved fungal species Antrodia camphorata has diverse health-promoting effects and has been popularly used in East Asia as a traditional herb. We isolated a volatile compound from the culture medium of A. camphorata and identified it as gamma-dodecalactone (gamma-DDL). Cytomic screening for immune-modulating ac...

journal_title：Bioorganic & medicinal chemistry

authors： Chen CJ,Vijaya Krishna R,Tsai CC,Wu WH,Chao LK,Hwang KH,Chien CM,Chang HY,Chen ST

更新日期：2010-09-15 00:00:00

abstract：:Small molecules are central players in chemical biology studies. They promote the perturbation of cellular processes underlying diseases and enable the identification of biological targets that can be validated for therapeutic intervention. Small molecules have been shown to accurately tune a single function of plurip...

journal_title：Bioorganic & medicinal chemistry

authors： Abet V,Mariani A,Truscott FR,Britton S,Rodriguez R

更新日期：2014-08-15 00:00:00

abstract：:5-HT(7) receptor antagonists generated antidepressant-like effects in animal model and the involvement of the 5-HT(7) receptor in other pathophysiological mechanisms such as thermoregulation, learning and memory, and sleep has been highlighted by various studies. As one of our efforts to discover a new type of 5-HT(7)...

journal_title：Bioorganic & medicinal chemistry

authors： Na YH,Hong SH,Lee JH,Park WK,Baek DJ,Koh HY,Cho YS,Choo H,Pae AN

更新日期：2008-03-01 00:00:00

abstract：:A series of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives were prepared and evaluated as inhibitors of human liver glycogen phosphorylase a (hLGPa). One compound, 5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide (2f), inhibited hLGPa with an IC(50) of 0.90microM. The pyridine analogue of 2f show...

journal_title：Bioorganic & medicinal chemistry

authors： Onda K,Suzuki T,Shiraki R,Yonetoku Y,Negoro K,Momose K,Katayama N,Orita M,Yamaguchi T,Ohta M,Tsukamoto S

更新日期：2008-05-15 00:00:00

abstract：:A series of specific alpha-ketoheterocycles (benzoxazole, thiazole, imidazole, tetrazole, and thiazole-4-carboxylate) has been synthesized in order to assess their potential as beta-lactamase inhibitors. The syntheses were achieved either by construction of the heterocycle (benzoxazole) from an appropriate alpha-hydro...

journal_title：Bioorganic & medicinal chemistry

authors： Kumar S,Pearson AL,Pratt RF

更新日期：2001-08-01 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：:The discovery of 3-methoxy-9-(30,40,50-trimethoxyphenyl)-6,7-dihydro-5H-benzo[7]annulen-4-ol (a benzosuberene-based analogue referred to as KGP18) was originally inspired by the natural products colchicine and combretastatin A-4 (CA4). The relative structural simplicity and ease of synthesis of KGP18, coupled with its...

journal_title：Bioorganic & medicinal chemistry

authors： Herdman CA,Devkota L,Lin CM,Niu H,Strecker TE,Lopez R,Liu L,George CS,Tanpure RP,Hamel E,Chaplin DJ,Mason RP,Trawick ML,Pinney KG

更新日期：2015-12-15 00:00:00

abstract：:A benzothiazole-derived compound (4a) designed to mimic the C(alpha)-C(beta) bond vectors and terminal functionalities of Lys2, Tyr13 and Arg17 in omega-conotoxin GVIA was synthesised, together with analogues (4b-d), which had each side-chain mimic systematically truncated or eliminated. The affinity of these compound...

journal_title：Bioorganic & medicinal chemistry

authors： Baell JB,Duggan PJ,Forsyth SA,Lewis RJ,Lok YP,Schroeder CI

更新日期：2004-08-01 00:00:00

abstract：:The previously reported morphinan derivative SN-28 showed high selectivity and agonist activity for the δ opioid receptor. In the course of examining the structure-activity relationship of SN-28 derivatives, the derivatives with the 4-hydroxy group (SN-24, 26, 27) showed higher selectivities for the δ receptor over th...

journal_title：Bioorganic & medicinal chemistry

authors： Ida Y,Nemoto T,Hirayama S,Fujii H,Osa Y,Imai M,Nakamura T,Kanemasa T,Kato A,Nagase H

更新日期：2012-01-15 00:00:00

abstract：:Pregnane X receptor (PXR) is a ligand-dependent transcription factor that is considered to be a potential therapeutic target for multiple diseases. Herein, we report the development and structure-activity relationship studies of a new series of hPXR agonists. Focusing on our recently developed silanol-sulfonamide scaf...

journal_title：Bioorganic & medicinal chemistry

authors： Toyama H,Shirakawa H,Komai M,Hashimoto Y,Fujii S

更新日期：2018-08-15 00:00:00

abstract：:A series of 5-aryl- and 3,5-bis-aryl-2-amino-1,4-pyrazine derivatives 4 and 6, and related imidazolopyrazinones 7, has been synthesized, the aryl groups of which are catechol and/or phenol substituents. These compounds, tested against human keratinocyte cells stressed by UVB irradiation, showed high antioxidative prop...

journal_title：Bioorganic & medicinal chemistry

authors： Cavalier JF,Burton M,Dussart F,Marchand C,Rees JF,Marchand-Brynaert J

更新日期：2001-04-01 00:00:00

abstract：:In the present article, we have synthesized three different series of pyrazolo[3,4-b]pyridines and their structural analogues using novel synthetic strategy involving one-pot condensation of 5,6-dihydro-4H-pyran-3-carbaldehyde/2-formyl-3,4,6-tri-O-methyl-D-glucal/chromone-3-carbaldehyde with heteroaromatic amines. All...

journal_title：Bioorganic & medicinal chemistry

authors： Bharate SB,Mahajan TR,Gole YR,Nambiar M,Matan TT,Kulkarni-Almeida A,Balachandran S,Junjappa H,Balakrishnan A,Vishwakarma RA

更新日期：2008-08-01 00:00:00

abstract：:Several studies have demonstrated that N-substituted amino acid derivatives exhibit weak anticonvulsant activities in vivo. In the present study, a series of amides of aminoacids structurally related to aminoacetamide have been synthesised and investigated for anticonvulsant activity. Among the molecules investigated,...

journal_title：Bioorganic & medicinal chemistry

authors： Ghidini E,Delcanale M,De Fanti R,Rizzi A,Mazzuferi M,Rodi D,Simonato M,Lipreri M,Bassani F,Battipaglia L,Bergamaschi M,Villetti G

更新日期：2006-05-15 00:00:00

abstract：:Novel pyrazole carboxamides with a diarylamine-modified scaffold were modified based on the bixafen (Bayer) fungicide, which has excellent activity against Rhizoctonia solani, Rhizoctonia cerealis and Sclerotinia sclerotiorum. To discover the potential insecticidal activity of these novel pyrazole carboxamides, the pr...

journal_title：Bioorganic & medicinal chemistry

authors： Ren Y,Yang N,Yue Y,Jin H,Tao K,Hou T

更新日期：2018-05-15 00:00:00

abstract：:Novel photoactive bridged polysilsesquioxane films were prepared by doped with a porphyrin derivative. The films were formed by acid-catalyzed polycondensation reaction of a precursor of a bridged silsesquioxane, based on the reaction product of (glycidoxypropyl)trimethoxysilane with n-dodecylamine in the presence of ...

journal_title：Bioorganic & medicinal chemistry

authors： Alvarez MG,Gómez ML,Mora SJ,Milanesio ME,Durantini EN

更新日期：2012-07-01 00:00:00

abstract：:The efficacy of anthracycline based anticancer drugs is limited by pleiotropic drug resistance of tumor cells. Aiming at the design of anthracyclinone congeners capable of circumventing drug resistance, we synthesized naphthoindole containing derivatives of tryptophan and tryptamine. In doing so we adapted the traditi...

journal_title：Bioorganic & medicinal chemistry

authors： Shchekotikhin AE,Dezhenkova LG,Susova OY,Glazunova VA,Luzikov YN,Sinkevich YB,Buyanov VN,Shtil AA,Preobrazhenskaya MN

更新日期：2007-04-01 00:00:00

abstract：:Sphingosine kinases (SphKs) are oncogenic enzymes that regulate the critical balance between ceramide and sphingosine-1-phosphate. Much effort has been dedicated to develop inhibitors against these enzymes. Naturally occurring pachastrissamine (jaspine B) and all its stereoisomers were prepared and evaluated for their...

journal_title：Bioorganic & medicinal chemistry

authors： Yoshimitsu Y,Oishi S,Miyagaki J,Inuki S,Ohno H,Fujii N

更新日期：2011-09-15 00:00:00

abstract：:In lead optimization efforts starting from the tetrahydroisoquinoline (S)-1, we identified 2-{[(2R)-2-hydroxypropyl]amino}-1-[(1S)-8-methoxy-1-phenyl-3,4-dihydroisoquinolin-2(1H)-yl]ethanone ((1S)-8t) as a novel orally active small-molecule N-type calcium channel blocker without CYP inhibition liability. CYP3A4 inhibi...

journal_title：Bioorganic & medicinal chemistry

authors： Ogiyama T,Yonezawa K,Inoue M,Katayama N,Watanabe T,Yoshimura S,Gotoh T,Kiso T,Koakutsu A,Kakimoto S,Shishikura JI

更新日期：2015-08-01 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