Synthesis and α-Glucosidase II inhibitory activity of valienamine pseudodisaccharides relevant to N-glycan biosynthesis.

abstract：:The enediyne natural products have been explored for their phenomenal cytotoxicity. The development of enediynes into anticancer drugs has been successfully achieved through the utilization of polymer- and antibody-drug conjugates (ADCs) as drug delivery systems. An increasing inventory of enediynes would benefit curr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shen B,Hindra,Yan X,Huang T,Ge H,Yang D,Teng Q,Rudolf JD,Lohman JR

更新日期：2015-01-01 00:00:00

abstract：:A structure-activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. Optimization of 1 by introduction of a hydrophilic substituent into the thioether part resulted in identification of potent ORL1 antagonists with high selectivity over bindi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kobayashi K,Kato T,Yamamoto I,Shimizu A,Mizutani S,Asai M,Kawamoto H,Ito S,Yoshizumi T,Hirayama M,Ozaki S,Ohta H,Okamoto O

更新日期：2009-06-01 00:00:00

abstract：:By linking the mercapto groups with isopropyl and introducing L-amino acid into the 5-carboxyl of DMSA a class of novel 5-(1-carbonyl-L-amino-acid)-2,2- dimethyl-[1,3]dithiolane-4-carboxylic acids were prepared. Their in vivo activities were evaluated on lead loaded mice at the dose of 0.4 mmol/kg. The results showed ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu Y,Wang Y,Zhao M,Hou B,Peng L,Zheng M,Wu J,Peng S

更新日期：2011-03-15 00:00:00

abstract：:The X-ray crystal structure for the adduct of human carbonic anhydrase (hCA) II with a topically acting antiglaucoma sulfonamide (the 2-N,N-diethylaminoethylamide of 5-(4-carboxybenzenesulfonamido-1,3,4-thiadiazole-2-sulfonamide), has been resolved at a resolution of 1.6A. This compound is a very potent inhibitor of t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Abbate F,Casini A,Scozzafava A,Supuran CT

更新日期：2004-05-03 00:00:00

abstract：:Practical, asymmetric total syntheses of the title phospholipids from a readily available myo-inositol derivative as well as short chain and cross-linkable aminoether analogues are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Falck JR,Krishna UM,Capdevila JH

更新日期：2000-08-07 00:00:00

abstract：:Peptide therapeutics have traditionally faced many challenges including low bioavailability, poor proteolytic stability and difficult cellular uptake. Conformationally constraining the backbone of a peptide into a macrocyclic ring often ameliorates these problems and allows for the development of a variety of new drug...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ferrie JJ,Gruskos JJ,Goldwaser AL,Decker ME,Guarracino DA

更新日期：2013-02-15 00:00:00

abstract：:A new triterpenoid saponin, julibroside J(28) (1), was isolated from the stem bark of Albizia julibrissin Durazz (Leguminosae) by using chromatographic method. The structure of 1 was established by spectroscopic methods. 1 displayed significant antitumor activity in vitro against PC-3M-1E8, Bel-7402, and HeLa cancer c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liang H,Tong WY,Zhao YY,Cui JR,Tu GZ

更新日期：2005-10-15 00:00:00

abstract：:4-Aryl-5-pyrimidyl based cytokine synthesis inhibitors that contain a novel monocyclic, pyrazolone heterocyclic core are described. Many of these inhibitors showed low nanomolar activity against LPS-induced TNF-alpha production. One of the compounds (6e) was found to be efficacious in the rat iodoacetate (RIA) in vivo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Golebiowski A,Townes JA,Laufersweiler MJ,Brugel TA,Clark MP,Clark CM,Djung JF,Laughlin SK,Sabat MP,Bookland RG,VanRens JC,De B,Hsieh LC,Janusz MJ,Walter RL,Webster ME,Mekel MJ

更新日期：2005-05-02 00:00:00

abstract：:Novel conformationally constrained BET bromodomain inhibitors have been developed. These inhibitors were optimized in two similar, yet distinct chemical series, the 6-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (A) and the 1-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-ones (B). Each series demonstrated excellent activity in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fidanze SD,Liu D,Mantei RA,Hasvold LA,Pratt JK,Sheppard GS,Wang L,Holms JH,Dai Y,Aguirre A,Bogdan A,Dietrich JD,Marjanovic J,Park CH,Hutchins CW,Lin X,Bui MH,Huang X,Wilcox D,Li L,Wang R,Kovar P,Magoc TJ,Raj

更新日期：2018-06-01 00:00:00

abstract：:A series of 10-hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones was synthesized and tested for their inhibition of HIV-1 replication in cell culture. Structure-activity studies indicated that high antiviral potency against wild-type virus as well as viruses containing integrase mutation...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wiscount CM,Williams PD,Tran LO,Embrey MW,Fisher TE,Sherman V,Homnick CF,Donnette Staas D,Lyle TA,Wai JS,Vacca JP,Wang Z,Felock PJ,Stillmock KA,Witmer MV,Miller MD,Hazuda DJ,Day AM,Gabryelski LJ,Ecto LT,Schleif WA

更新日期：2008-08-15 00:00:00

abstract：:A series of 2-phenylspiroindenediones was prepared. The spiroindenediones were found to be less active than the corresponding spiroindenes as estrogen receptor ligands and failed to demonstrate the receptor subtype selectivity that had been anticipated from molecular modeling. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Blizzard TA,Mosley RT,Birzin ET,Chan W,Hammond ML

更新日期：2004-03-08 00:00:00

abstract：:The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rosen TJ,Coffman KJ,McLean S,Crawford RT,Bryce DK,Gohda Y,Tsuchiya M,Nagahisa A,Nakane M,Lowe JA 3rd

更新日期：1998-02-03 00:00:00

abstract：:We report the first synthesis of the C-terminally spermine-conjugated stapled peptide-based inhibitors of the p53-Mdm2 interaction. Subsequent biological, biophysical and cellular uptake assays with the spermine-conjugated stapled peptides revealed that spermine conjugation minimally affects biological activity while ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Muppidi A,Li X,Chen J,Lin Q

更新日期：2011-12-15 00:00:00

abstract：:Highly selective orexin receptor antagonists (SORAs) of the orexin 2 receptor (OX2R) have become attractive targets both as potential therapeutics for insomnia as well as biological tools to help further elucidate the underlying pharmacology of the orexin signaling pathway. Herein, we describe the discovery of a novel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Raheem IT,Breslin MJ,Bruno J,Cabalu TD,Cooke A,Cox CD,Cui D,Garson S,Gotter AL,Fox SV,Harrell CM,Kuduk SD,Lemaire W,Prueksaritanont T,Renger JJ,Stump C,Tannenbaum PL,Williams PD,Winrow CJ,Coleman PJ

更新日期：2015-02-01 00:00:00

abstract：:The blood-brain barrier choline transporter may have utility as a drug delivery vector to the central nervous system. Surprisingly, this transporter has as yet not been cloned and expressed. We therefore initiated a 3D-QSAR study to develop predictive models for compound binding and identify structural features import...

journal_title：Bioorganic & medicinal chemistry letters

authors： Geldenhuys WJ,Lockman PR,McAfee JH,Fitzpatrick KT,Van der Schyf CJ,Allen DD

更新日期：2004-06-21 00:00:00

abstract：:A series of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives have been designed, synthesized and evaluated for their potential antiproliferation activity and Aurora-A kinase inhibitory activity. Among all the compounds, compound 10e possessed the most potent biological activity against HCT116 and MCF-7 cell lines...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li X,Lu X,Xing M,Yang XH,Zhao TT,Gong HB,Zhu HL

更新日期：2012-06-01 00:00:00

abstract：:Our process research on OPC-35564 revealed that a mixed borohydride reducing agent (ZrCl4/NaBH4) in DME (Itsuno system) afforded a rapid and direct conversion of N-alkyl-nitroisatin into nitroindole nucleus. Comparison with other reducing agents indicated the superiority of the present system and the key function of Z...

journal_title：Bioorganic & medicinal chemistry letters

authors： Torisawa Y,Nishi T,Minamikawa J

更新日期：2001-03-26 00:00:00

abstract：:The synthesis and evaluation of new analogues of thieno[2,3-d]pyrimidin-4-yl hydrazones are described. 2-Pyrdinecarboxaldehyde [6-(tert-butyl)thieno[2,3-d]pyrimidine-4-yl]hydrazone derivatives have been identified as cyclin-dependent kinase 4 (CDK4) inhibitors. The potency, selectivity profile, and structure-activity ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Horiuchi T,Chiba J,Uoto K,Soga T

更新日期：2009-01-15 00:00:00

abstract：:A series of sixteen β-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-β-carboline and various aldehydes under basic conditions followed by N2-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkataramana Reddy PO,Hridhay M,Nikhil K,Khan S,Jha PN,Shah K,Kumar D

更新日期：2018-05-01 00:00:00

abstract：:The reductive amination of an amino acid derived glyoxal, with the free amino group of a protected amino acid or oligopeptide fragment, has been developed as a simple and efficient method for the preparation of ketomethylene amino pseudo-oligopeptide isosteres Aa psi(COCH2NH)Aa. Trichlorosilane-DMF is the reagent of c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Groarke M,Hartzoulakis B,McKervey MA,Walker B,Williams CH

更新日期：2000-01-17 00:00:00

abstract：:Naturally occurring flavonoids co-exist as glycoside conjugates, which dominate aglycones in their content. To unveil the structure-activity relationship of a naturally occurring flavonoid, we investigated the effects of the glycosylation of naringenin on the inhibition of enzyme systems related to diabetes (protein t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jung HA,Paudel P,Seong SH,Min BS,Choi JS

更新日期：2017-06-01 00:00:00

abstract：:Fifteen new alpha-acylaminoketones were prepared by four different routes in an initial effort to optimize the potency of these compounds as ecdysone agonists. The compounds were assayed in mammalian cells expressing the ecdysone receptors from Bombyx mori (BmEcR) and Choristoneura fumiferana (CfEcR) for their ability...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tice CM,Hormann RE,Thompson CS,Friz JL,Cavanaugh CK,Saggers JA

更新日期：2003-06-02 00:00:00

abstract：:(-)-Renieramycin G and fifteen C-22 analogs were prepared employing l-tyrosine as the chiral starting material. These analogs, along with (-)-renieramycin G itself, were evaluated in vitro for cytotoxicity against HCT-8, BEL-7402, A2780, MCF-7, A549, BGC-823, Ketr3, KB, Hela cells. The IC(50) values of most of these a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu W,Dong W,Liao X,Yan Z,Guan B,Wang N,Liu Z

更新日期：2011-03-01 00:00:00

abstract：:A major challenge in the application of cytotoxic anti-cancer drugs is their general lack of selectivity, which often leads to systematic toxicity due to their inability to discriminate between malignant and healthy cells. A particularly promising target for selective targeting are the folate receptors (FR) that are o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Geersing A,de Vries RH,Jansen G,Rots MG,Roelfes G

更新日期：2019-08-01 00:00:00

abstract：:On-resin macrocyclization via an SNAr reaction is employed in the synthesis of tocinoic acid analogs. Specifically, an N-terminal nitrofluorobenzene is attacked by a nucleophilic C-terminal sidechain. The remaining nitro group can be reduced and acylated. NMR is used to compare the conformation of the new macrocyclic ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fotsch C,Kumaravel G,Sharma SK,Wu AD,Gounarides JS,Nirmala NR,Petter RC

更新日期：1999-08-02 00:00:00

abstract：:The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is disclosed. Compound 10i was identified as lead compound with a promising overall profile. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Belanger DB,Curran PJ,Hruza A,Voigt J,Meng Z,Mandal AK,Siddiqui MA,Basso AD,Gray K

更新日期：2010-09-01 00:00:00

abstract：:Hypericin monocarboxylic acid was synthesized in an overall yield of 25% in four steps and radiolabelled with iodine-123 in good yield (>75%). The resulting mono-[(123)I]iodohypericin monocarboxylic acid was evaluated in normal mice and in rats with ethanol induced liver necrosis. In this model, tracer concentration i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fonge H,Jin L,Wang H,Ni Y,Bormans G,Verbruggen A

更新日期：2007-07-15 00:00:00

abstract：:A series of N-8 substituted analogs based upon the spiropiperidine core of the original lead compound 1 was synthesized. This lead has been elaborated to compounds to give compounds 2 and 3 (R=H) that exhibited high NOP binding affinity as well as selectivity against other known opioid receptors. These two series have...

journal_title：Bioorganic & medicinal chemistry letters

authors： Caldwell JP,Matasi JJ,Fernandez X,McLeod RL,Zhang H,Fawzi A,Tulshian DB

更新日期：2009-02-15 00:00:00

abstract：:The CO-releasing properties of iron(0)tricarbonyl complexes bearing a 2-pyrone ligand have been evaluated. In this report, we demonstrate that the intrinsic stability of the (eta4-2-pyrone)Fe(CO)3 complex influences the extent and rate of CO release, which is affected by the presence of a halogen substituent on the 2-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fairlamb IJ,Duhme-Klair AK,Lynam JM,Moulton BE,O'Brien CT,Sawle P,Hammad J,Motterlini R

更新日期：2006-02-15 00:00:00

abstract：:Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibito...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lin S,Han F,Liu P,Tao J,Zhong X,Liu X,Yi C,Xu H

更新日期：2014-02-01 00:00:00