Toward the development of chemoprevention agents. Part 1: Design, synthesis, and anti-inflammatory activities of a new class of 2,5-disubstituted-dioxacycloalkanes.

abstract：:Structural features and hydrogen-bond interactions of dinotefuran (DIN), imidacoloprid (IMI) and acetamiprid (ACE) have been investigated experimentally through analyses of new crystal structures and observations in structural databases, as well as by Density Functional Theory quantum chemical calculations. Several co...

journal_title：Bioorganic & medicinal chemistry

authors： Le Questel JY,Graton J,Cerón-Carrasco JP,Jacquemin D,Planchat A,Thany SH

更新日期：2011-12-15 00:00:00

abstract：:Highly chemo- and regioselective de-esterification has been observed in the deacetylation of peracetylated enolic forms of polyphenolic benzyl phenyl ketones by lipase from porcine pancreas (PPL) suspended in tetrahydrofuran (THF). The enzyme selectively deacetylates the enolic acetoxy over the phenolic acetoxy group(...

journal_title：Bioorganic & medicinal chemistry

authors： Parmar VS,Pati HN,Azim A,Kumar R,Himanshu,Bisht KS,Prasad AK,Errington W

更新日期：1998-01-01 00:00:00

abstract：:3,4-Dihydro-2H,6H-pyrimido[1,2-c][1,3]benzothiazin-6-imine (PD 404182) is an antiretroviral agent with submicromolar inhibitory activity against human immunodeficiency virus-1 (HIV-1) and HIV-2 infection. In the current study, the structure-activity relationships of accessory groups at the 3- and 9-positions of pyrimi...

journal_title：Bioorganic & medicinal chemistry

authors： Mizuhara T,Oishi S,Ohno H,Shimura K,Matsuoka M,Fujii N

更新日期：2012-11-01 00:00:00

abstract：:A detailed investigation of the South China Sea soft coral Sarcophyton trocheliophorum Marenzeller yielded, along with six known terpenes (6-11), the new sarcophytonolides N-R (1-5), whose structures have been elucidated by detailed spectroscopic analysis. Sarcophytonolides N-R are mono- or bicyclic cembranoids charac...

journal_title：Bioorganic & medicinal chemistry

authors： Liang LF,Gao LX,Li J,Taglialatela-Scafati O,Guo YW

更新日期：2013-09-01 00:00:00

abstract：:A series of novel metronidazole aryloxy, carboxy and azole derivatives has been synthesized and their cytotoxic activities on three cancer cell lines were evaluated by MTT assay. Compounds 4m, 4l and 4d showed the most potent cytotoxic activity (IC50s less than 100 µg/mL). Apoptosis was also detected for these compoun...

journal_title：Bioorganic & medicinal chemistry

authors： Faghih-Mirzaei E,Sabouri S,Zeidabadinejad L,AbdolahRamazani S,Abaszadeh M,Khodadadi A,Shamsadinipour M,Jafari M,Pirhadi S

更新日期：2019-01-15 00:00:00

abstract：:Furanfurin (2-beta-D-ribofuranosylfuran-4-carboxamide) derivatives and analogues were synthesized and their affinity for adenosine receptors was determined. The agonistic behavior of furanfurin against A1 receptors is preserved only when the furan ring is substituted with isosteric pentatomic ring systems such as oxaz...

journal_title：Bioorganic & medicinal chemistry

authors： Franchetti P,Cappellacci L,Marchetti S,Martini C,Costa B,Varani K,Borea PA,Grifantini M

更新日期：2000-09-01 00:00:00

abstract：:Breast cancer is the second most common cancer worldwide after lung cancer with the vast majority of early stage breast cancers being hormone-dependent. One of the major therapeutic advances in the clinical treatment of breast cancer has been the introduction of selective estrogen receptor modulators (SERMs). We descr...

journal_title：Bioorganic & medicinal chemistry

authors： Kelly PM,Bright SA,Fayne D,Pollock JK,Zisterer DM,Williams DC,Meegan MJ

更新日期：2016-09-15 00:00:00

abstract：:One phenol-quaternary ammonium salt derivative with a flexible linker and three derivatives with a quinazoline moiety are present. Their binding affinities for DNA are discussed and it is clearly demonstrated that this class of phenol-quaternary ammonium salt derivatives could inhibit DNA transcription effectively. ...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang L,Ren L,Bai M,Weng L,Huang J,Wu L,Deng M,Zhou X

更新日期：2007-11-15 00:00:00

abstract：:A class of tetracyclic terpenes was synthesized and evaluated for antagonistic activity of endothelin-1 (ET-1) induced vasoconstriction and inhibitory activity of voltage-activated Ca(2+) channels. Three repeated Robinson annulation reactions were utilized to construct the tetracyclic molecules. A stereoselective redu...

journal_title：Bioorganic & medicinal chemistry

authors： Lu J,Aguilar A,Zou B,Bao W,Koldas S,Shi A,Desper J,Wangemann P,Xie XS,Hua DH

更新日期：2015-09-01 00:00:00

abstract：:The serotonin receptor 6 (5-HT(6)) is implicated in the pathophysiology of cognitive diseases, schizophrenia, anxiety and obesity and in vivo studies of this receptor would be of value for studying the pathophysiology of these disorders. Therefore, N-[3,5-dichloro-2-(methoxy)phenyl]-4-(methoxy)-3-(1-piperazinyl)benzen...

journal_title：Bioorganic & medicinal chemistry

authors： Liu F,Majo VJ,Prabhakaran J,Milak MS,John Mann J,Parsey RV,Kumar JS

更新日期：2011-09-01 00:00:00

abstract：:The present report describes the synthesis and anticancer evaluation of certain 11-substituted 6H-indolo[2,3-b]quinolines and their methylated derivatives. These 6H-indolo[2,3-b]quinoline derivatives 11-13 were prepared from the commercially available 1,4-dihydroxyquinoline through alkylation, chlorination, nucleophil...

journal_title：Bioorganic & medicinal chemistry

authors： Chen YL,Hung HM,Lu CM,Li KC,Tzeng CC

更新日期：2004-12-15 00:00:00

abstract：:Dermaseptins are peptides found in the skin secretions of Phyllomedusinae frogs. These peptides exert lytic action on some microorganisms without substantial haemolysis. In an attempt to understand the antimicrobial activity of these peptides we designed several dermaseptin S1 (ALWKTMLKKLGTMALHAGKAALGAAADTISQGTQ) (DS1...

journal_title：Bioorganic & medicinal chemistry

authors： Savoia D,Guerrini R,Marzola E,Salvadori S

更新日期：2008-09-01 00:00:00

abstract：:We previously reported a series of 8-methyl-2-aryl-5-alkylaminoquinolines as a novel class of corticotropin-releasing factor-1 (CRF(1)) receptor antagonists. A critical issue encountered for this series of compounds was low aqueous solubility at physiological pH (pH 7.4). To address this issue, derivatization at key s...

journal_title：Bioorganic & medicinal chemistry

authors： Takeda K,Terauchi T,Hashizume M,Shikata K,Taguchi R,Murata-Tai K,Fujisawa M,Takahashi Y,Shin K,Ino M,Shibata H,Yonaga M

更新日期：2012-11-15 00:00:00

abstract：:The synthesis of 9-(β-d-1,3-dioxolan-4-yl)2,6-diaminopurine nucleoside phosphoramidate prodrugs as well as various 2-amino-6-carbamoylpurine dioxolane derivatives and their phosphoramidates prodrugs is reported. Their ability to block HIV and HBV replication along with their cytotoxicity toward HepG2, human lymphocyte...

journal_title：Bioorganic & medicinal chemistry

authors： Cho JH,Bondana L,Detorio MA,Montero C,Bassit LC,Amblard F,Coats SJ,Schinazi RF

更新日期：2014-12-01 00:00:00

abstract：:Ten 1-phenyl-1H-pyrazolo[3,4-b]pyridine derivatives connected by a linker group to benzenesulfonamide moieties with different substituents in the 4-position were synthesized and assayed against Plasmodium falciparum. These ten compounds exhibited activity in vitro against the chloroquine-resistant clone W2 with IC50 v...

journal_title：Bioorganic & medicinal chemistry

authors： Silva TB,Bernardino AMR,Ferreira MLG,Rogerio KR,Carvalho LJM,Boechat N,Pinheiro LCS

更新日期：2016-09-15 00:00:00

abstract：:In this study, a series of twenty-two ring-substituted 6-hydroxynaphthalene-2-carboxanilides was prepared and characterized. Primary in vitro screening of the synthesized compounds was performed against Mycobacterium tuberculosis H37Ra, Mycobacterium avium complex and M. avium subsp. paratuberculosis. Derivatives subs...

journal_title：Bioorganic & medicinal chemistry

authors： Kos J,Nevin E,Soral M,Kushkevych I,Gonec T,Bobal P,Kollar P,Coffey A,O'Mahony J,Liptaj T,Kralova K,Jampilek J

更新日期：2015-05-01 00:00:00

abstract：:In this study, we disclose the design and synthesis of novel 4-susbtituted nipecotic acid derivatives as inhibitors of the GABA transporter mGAT1. Based on molecular modeling studies the compounds are assumed to adopt a binding pose similar to that of the potent mGAT1 inhibitor nipecotic acid. As substitution in 4-pos...

journal_title：Bioorganic & medicinal chemistry

authors： Hellenbrand T,Höfner G,Wein T,Wanner KT

更新日期：2016-05-01 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：:With the continuing interest in deciphering the interplay between protein function and conformational changes, small fluorescence probes will be especially useful for tracking changes in the crowded protein interior space. Presently, we describe the potential utility of six unnatural amino acid fluorescence donors str...

journal_title：Bioorganic & medicinal chemistry

authors： Talukder P,Chen S,Liu CT,Baldwin EA,Benkovic SJ,Hecht SM

更新日期：2014-11-01 00:00:00

abstract：:Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field. ...

journal_title：Bioorganic & medicinal chemistry

authors： Arredondo Y,Moreno-Mañas M,Pleixats R,Palacín C,Raga MM,Castelló JM,Ortiz JA

更新日期：1997-10-01 00:00:00

abstract：:Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC(50) of 16 compounds which have displayed MIC of 0.25 microg/mL were also recorded. One of the compounds (...

journal_title：Bioorganic & medicinal chemistry

authors： Madapa S,Tusi Z,Mishra A,Srivastava K,Pandey SK,Tripathi R,Puri SK,Batra S

更新日期：2009-01-01 00:00:00

abstract：:A series of benzazolone compounds were synthesized utilizing benzoxazolinonic and benzothiazolinonic heterocycles as the building unit. The antioxidant activity of these compounds was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO(4) or 2,2'-azobis(2-amidinopro...

journal_title：Bioorganic & medicinal chemistry

authors： Yekini I,Hammoudi F,Martin-Nizard F,Yous S,Lebegue N,Berthelot P,Carato P

更新日期：2009-11-15 00:00:00

abstract：:We have surveyed the utility of Beckmann rearrangement for the conversion of indanones into carbostyrils. Initial attempts at the conversion of 6-methoxy indanone oxime under classical conditions resulted in the formation of the two unusual products: 2-sulfonyloxyindanone and the dimeric product. This unusual rearrang...

journal_title：Bioorganic & medicinal chemistry

authors： Torisawa Y,Nishi T,Minamikawa Ji

更新日期：2003-05-15 00:00:00

abstract：:A systematic synthesis of the N-methyl-1-deoxynojirimycin-containing oligosaccharides related to the Lewis x, Lewis a, sialyl-Lewis x and sialyl-Lewis a antigens has been achieved. The couplings of the suitably protected 1-deoxynojirimycin derivative 10 with methyl-1-thioglycosides (glycosyl donors) of L-fucose (11), ...

journal_title：Bioorganic & medicinal chemistry

authors： Kiso M,Furui H,Ando K,Ishida H,Hasegawa A

更新日期：1994-11-01 00:00:00

abstract：:Z-1,1-Dichloro-2,3-diphenylcyclopropane (1) is an effective anti-breast cancer agent in rodents and in cell culture. We recently determined that 1 inhibits tubulin assembly in vitro and causes microtubule loss in breast cancer cells, leading to accumulation in the G2/M portion of the cell cycle. Aryl ring-halogenated,...

journal_title：Bioorganic & medicinal chemistry

authors： Jonnalagadda SS,ter Haar E,Hamel E,Lin CM,Magarian RA,Day BW

更新日期：1997-04-01 00:00:00

abstract：:γ-Aminobutyric acid (GABA) receptors are important targets of parasiticides/insecticides. Several 4-substituted analogs of the partial GABAA receptor agonist 5-(4-piperidyl)-3-isothiazolol (Thio-4-PIOL) were synthesized and examined for their antagonism of insect GABA receptors expressed in Drosophila S2 cells or Xeno...

journal_title：Bioorganic & medicinal chemistry

authors： Liu G,Furuta K,Nakajima H,Ozoe F,Ozoe Y

更新日期：2014-09-01 00:00:00

abstract：:A labeling probe containing a pyrenecarboxamide-tethered modified DNA base, (Py)U, has been developed for fluorometric detection of RNA poly(A) tracts, in which the fluorescence emission intensity was controlled by the microstructural change around (Py)U caused by binding with the target RNA. ...

journal_title：Bioorganic & medicinal chemistry

authors： Tanaka K,Okamoto A

更新日期：2008-01-01 00:00:00

abstract：:Protein-tyrosine phosphatase (PTP) inhibitors are attractive as potential signal transduction-directed therapeutics which may be useful in the treatment of a variety of diseases. We have previously reported the X-ray structure of 1,1-difluoro-1-(2-naphthalenyl)methyl] phosphonic acid (4) complexed with the human the p...

journal_title：Bioorganic & medicinal chemistry

authors： Yao ZJ,Ye B,Wu XW,Wang S,Wu L,Zhang ZY,Burke TR Jr

更新日期：1998-10-01 00:00:00

abstract：:A series of 1-(1-arylethylidene)thiosemicarbazide compounds and their analogues were synthesized and characterized by 1H NMR, MS. Their tyrosinase inhibitory activities were investigated by an assay based on the catalyzing ability of tyrosinase for the oxidation of L-DOPA, comparing with 4-methoxycinnamic acid and arb...

journal_title：Bioorganic & medicinal chemistry

authors： Liu J,Yi W,Wan Y,Ma L,Song H

更新日期：2008-02-01 00:00:00

abstract：:A small molecule library of pyrido[2,3-d]pyrimidine-2,4-dione derivatives 6-16 was synthesized from 6-amino-1,3-disubstituted uracils 18, characterized, and screened for inhibitory activity against eukaryotic elongation factor-2 kinase (eEF-2K). To understand the binding pocket of eEF-2K, structural modifications of t...

journal_title：Bioorganic & medicinal chemistry

authors： Edupuganti R,Wang Q,Tavares CD,Chitjian CA,Bachman JL,Ren P,Anslyn EV,Dalby KN

更新日期：2014-09-01 00:00:00