A stepwise dechlorination/cross-coupling strategy to diversify the vancomycin 'in-chloride'.

abstract：:Prothrombin is a vitamin K-dependent serine protease and plays pivotal roles in both procoagulant and anticoagulant pathway of hemostasis. In this study, prothrombin purified from porcine plasma was modified through PEGylation at N-terminal residue using 40 kDa PEG-phenyl-isothiocyanate (PIT-PEG40K). The monoPEGylated...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhou JG,Chen YM

更新日期：2011-06-01 00:00:00

abstract：:Difluorosialic acids (DFSAs) are potent inhibitors of viral neuraminidase that demonstrate activity against oseltamivir- and zanamivir-resistant strains of influenza. Unfortunately, low oral bioavailability precludes their development as second generation neuraminidase inhibitors for treating influenza as this leaves ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arns S,Tan J,Sun S,Galey A,Zisman N,Ross F,Udechukwu J,Dercho S,Gusti V,Paquette J,Webb M,Bourque E,Withers SG,Liggins R

更新日期：2015-06-15 00:00:00

abstract：:Twenty-five novel pregnenolone/2-cyanoacryloyl conjugates (6-30) were designed and prepared, with the aim of developing novel anticancer drugs with dual NF-κB inhibitory and anti-proliferative activities. Compounds 22 and 27-30 showed inhibition against TNF-α-induced NF-κB activation in luciferase assay, which was con...

journal_title：Bioorganic & medicinal chemistry letters

authors： Song JL,Zhang J,Liu CL,Liu C,Zhu KK,Yang FF,Liu XG,Figueiró Longo JP,Alexandre Muehlmann L,Azevedo RB,Zhang YY,Guo YW,Jiang CS,Zhang H

更新日期：2017-10-15 00:00:00

abstract：:A series of potential new 5-HT2 receptor scaffolds based on a simplification of the clinically studied, 5-HT2CR agonist vabicaserin, were designed. An in vivo feeding assay early in our screening process played an instrumental part in the lead identification process, leading us to focus on a 6,5,7-tricyclic scaffold. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ren A,Zhu X,Feichtinger K,Lehman J,Kasem M,Schrader TO,Wong A,Dang H,Le M,Frazer J,Unett DJ,Grottick AJ,Whelan KT,Morgan ME,Sage CR,Semple G

更新日期：2020-03-01 00:00:00

abstract：:Glucose transporters (GLUTs) facilitate glucose uptake and are overexpressed in most cancer cells. Inhibition of glucose transport has been shown to be an effective method to slow the growth of cancer cells both in vitro and in vivo. We have previously reported on the anticancer activity of an ester derived glucose up...

journal_title：Bioorganic & medicinal chemistry letters

authors： Roberts DA,Wang L,Zhang W,Liu Y,Shriwas P,Qian Y,Chen X,Bergmeier SC

更新日期：2020-09-15 00:00:00

abstract：:New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50=380 nM rat mitochondria) with favorable PK properties (F=93%, t(1/2)=13.6h, dog). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Elzein E,Ibrahim P,Koltun DO,Rehder K,Shenk KD,Marquart TA,Jiang B,Li X,Natero R,Li Y,Nguyen M,Kerwar S,Chu N,Soohoo D,Hao J,Maydanik VY,Lustig DA,Zeng D,Leung K,Zablocki JA

更新日期：2004-12-20 00:00:00

abstract：:Several shortened peptide analogues of the N-terminal domain of GPR1, an orphan G protein-coupled receptor (GPCR), were prepared and their anti-HIV-1 activities were evaluated. Some of the prepared compounds, especially sulfated derivatives, showed potent inhibitory activity against a broad range of HIV-1, including T...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ikeda K,Konishi K,Sato M,Hoshino H,Tanaka K

更新日期：2001-10-08 00:00:00

abstract：:A series of N-2-(4-(4-(2-substitutedthiazol-4-yl) piperazin-1-yl)-2-oxoethyl)acetamides were synthesized in an effort to prepare novel atypical antipsychotic agents. The compounds were synthesized by either microwave irradiation technique or by conventional synthesis and were characterized by spectral data (IR, (1)H N...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sekhar KV,Rao VS,Devambatla RKV,Kumar MM

更新日期：2008-12-01 00:00:00

abstract：:The synthesis and biological evaluation of a set of residue 3 analogues of vancomycin and its aglycon are described. These investigations follow from the promising biological activity of a protected and synthetically modified vancomycin aglycon analogue in which the asparagine side chain was modified to possess a nitr...

journal_title：Bioorganic & medicinal chemistry letters

authors： McAtee JJ,Castle SL,Jin Q,Boger DL

更新日期：2002-05-06 00:00:00

abstract：:Makomotindoline (1) was isolated from Makomotake, Zizania latifolia infected with Ustilago esculenta. The structure was determined by the interpretation of spectroscopic data and synthesis. Makomotindoline (1), its l-Glc isomer (2) and its aglycon (3) were synthesized and their effects on rat glioma cells showed adver...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suzuki T,Choi JH,Kawaguchi T,Yamashita K,Morita A,Hirai H,Nagai K,Hirose T,Omura S,Sunazuka T,Kawagishi H

更新日期：2012-07-01 00:00:00

abstract：:Oxidation of 4-methylcatechol previously exposed to aqueous calcium chloride was shown by ion chromatography to be associated with release of calcium ions. The catechol was oxidised to the corresponding orthoquinone by the use of tyrosinase from Agaricus bisporus. The oxidative release of calcium from the catechol is ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Riley PA,Stratford MR

更新日期：2015-04-01 00:00:00

abstract：:(1H-Pyridin-4-ylidene)amines containing lipophilic side chains at the imine nitrogen atom were prepared as potential clopidol isosteres in the development of antimalarials. Their antiplasmodial activity was evaluated in vitro against the Plasmodium falciparum W2 (chloroquine-resistant) and FCR3 (atovaquone-resistant) ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rodrigues T,Guedes RC,dos Santos DJ,Carrasco M,Gut J,Rosenthal PJ,Moreira R,Lopes F

更新日期：2009-07-01 00:00:00

abstract：:Although Au(I) complexes have been used to treat rheumatoid arthritis for over 75 years, their mechanism of action is still poorly understood. A family of enzymes responsible for joint destruction in rheumatoid arthritis, the cathepsins, has been discussed as a possible biological target of Au(I). In this study, inhib...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chircorian A,Barrios AM

更新日期：2004-10-18 00:00:00

abstract：:Three new pseudo-symmetrical tamoxifen derivatives, RID-B (15), C (16), and D (17), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of the pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 15 strongly inhibits the viability of HL-6...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shiina I,Sano Y,Nakata K,Kikuchi T,Sasaki A,Ikekita M,Hasome Y

更新日期：2007-05-01 00:00:00

abstract：:Following the promising activity of Q2FA15 on axonal growth, two new series of N/O-substituted QFAs were synthesized, based on a SN2-type reaction. O-alkylated QFA bearing 14 carbon atoms on the side chain (n=14) shows a very potent activity on axonal growth though lowered when compared to Q2FA15. While O-alkylation a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hanbali M,Bagnard D,Luu B

更新日期：2006-08-01 00:00:00

abstract：:Optically active phenylpropanoic acid derivatives [(S)-5, and (R)-5] were prepared, and their affinities for peroxisome proliferator-activated receptor (PPAR)alpha and PPAR gamma were evaluated. Binding assay and cell-based reporter assay indicated that the activity of these compounds is enantio-dependent, and resides...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miyachi H,Nomura M,Tanase T,Suzuki M,Murakami K,Awano K

更新日期：2002-02-11 00:00:00

abstract：:Halopemide, which was identified by HTS to inhibit phospholipase D2 (PLD2), provided the basis for an exploratory effort to identify potent inhibitors of PLD2 for use as inflammatory mediators. Parallel synthesis and purification were utilized to rapidly identify orally available amide analogs derived from indole 2-ca...

journal_title：Bioorganic & medicinal chemistry letters

authors： Monovich L,Mugrage B,Quadros E,Toscano K,Tommasi R,LaVoie S,Liu E,Du Z,LaSala D,Boyar W,Steed P

更新日期：2007-04-15 00:00:00

abstract：:Inhibition of histone deacetylases class I/II enzymes is a new, promising approach for cancer therapy. In the present study, we disclose a new structural class of HDAC inhibitors with the trithiocarbonate motif. A clear structure-activity-relationship was obtained for the cap-linker motif and the putative Zn(2+) compl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dehmel F,Ciossek T,Maier T,Weinbrenner S,Schmidt B,Zoche M,Beckers T

更新日期：2007-09-01 00:00:00

abstract：:Multidrug resistance in tumor cells poses a major obstacle to efficient chemotherapy. Several types of agents have been recognized as multidrug resistance inhibitors, among which the tetrahydroisoquinolines is the most studied. In current study 16 furoxan-based nitric oxide-releasing derivatives of tetrahydroisoquinol...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zou ZH,Lan XB,Qian H,Huang WL,Li YM

更新日期：2011-10-01 00:00:00

abstract：:Protein-protein interactions (PPIs) are key elements of several important biological processes and have emerged as valuable targets in medicinal chemistry. Importantly, numerous specific protein-protein interactions (e.g., p53-HDM2 and Bcl-2-BH3 domains) were found to be involved in the development of several diseases...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wójcik P,Berlicki Ł

更新日期：2016-02-01 00:00:00

abstract：:A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H(+)/K(+) ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a pote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yoon YA,Park CS,Cha MH,Choi H,Sim JY,Kim JG

更新日期：2010-10-01 00:00:00

abstract：:Ganglioside GM1 mimics including (R)-2-hydroxy-3-cyclohexylpropionic acid or (R)-2-hydroxy-3-phenylpropionic acid as replacements for NeuAc are stronger cholera toxin binders than the parent ligand 2, which includes (R)-2-hydroxy-propionic acid. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arosio D,Baretti S,Cattaldo S,Potenza D,Bernardi A

更新日期：2003-11-03 00:00:00

abstract：:A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Na...

journal_title：Bioorganic & medicinal chemistry letters

authors： Danho W,Swistok J,Cheung AW,Kurylko G,Franco L,Chu XJ,Chen L,Yagaloff K

更新日期：2003-02-24 00:00:00

abstract：:A new series of 2-(benzyloxy)benzamides are presented that are potent functional antagonists of TRPM8 and possess improved LipE and LE compared to the original lead. They were discovered through a series of compound libraries and we present a powerful visualization method for the chemical space explored with each libr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Brown A,Ellis D,Favor DA,Kirkup T,Klute W,MacKenny M,McMurray G,Stennett A

更新日期：2013-11-15 00:00:00

abstract：:Thienylpyrimidines substituted at position 2 of the pyrimidine with a chiral aminoalkoxy group were synthesized. Upon interaction with duplex DNA, the unfused heteroaromatic system of these compounds intercalates with DNA base pairs and the protonated side chain is located in the major groove. The S-enantiomers bind m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Strekowski L,Cegla MT,Honkan V,Buczak H,Winkeljohn WR,Baumstark AL,Wilson WD

更新日期：2005-06-02 00:00:00

abstract：:Novel bioreductive and long-wavelength fluorescent markers for hypoxic cells in solid tumor, 9-isocyano-8H-acenaphtho[l,2-b]pyrrol-8-one with the side chain of 2-nitroimidazole, were designed, synthesized, and evaluated in V79 379A Chinese hamster cells in vitro. Compounds A(2) and A(4) showed good hypoxic-oxic fluore...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu Y,Xu Y,Qian X,Xiao Y,Liu J,Shen L,Li J,Zhang Y

更新日期：2006-03-15 00:00:00

abstract：:Synthesis of a symmetrically branched diglycerol (BGL002, involving one iminodiacetic residue) as a G2 dendron, and the tetradecaglycerol (BGL014, involving one iminodiacetic residue) as a G4 dendron, is described. Several members of the BGL family of G2-G4 dendrons were assembled, with G2 bearing four hydroxyl groups...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nemoto H,Ishihara A,Araki T,Katagiri A,Kamiya M,Matsushita T,Hattori H,Mimura Y,Tomoda Y,Yamasaki M

更新日期：2011-08-15 00:00:00

abstract：:Based on a screening lead from a yeast-based assay to identify Src family kinase inhibitors, a series of 4-anilino-7-thienyl-3-quinolinecarbonitriles was prepared. When the thiophene ring was substituted with a water-solubilizing group in a 2,5-, 3,5- or 2,4-pattern, potent inhibition of Src kinase activity was observ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Boschelli DH,Wang DY,Ye F,Yamashita A,Zhang N,Powell D,Weber J,Boschelli F

更新日期：2002-08-05 00:00:00

abstract：:A novel class of benzocinnolinones analogs of irdabisant were designed and synthesized as histamine H3R antagonists/inverse agonists. Modifications to the pyridazinone portion of the core and linker led to the identification of molecules with excellent target potency and selectivity with improved rat pharmacokinetic p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Josef KA,Aimone LD,Lyons J,Raddatz R,Hudkins RL

更新日期：2012-06-15 00:00:00

abstract：:We designed and synthesized of 1,3,5-trioxazatriquinanes with o- or p-hydroxyphenyl rings as analogs of the κ opioid receptor agonist SYK-146 with m-hydroxyphenyl groups. Although almost all tested compounds did not bind to the opioid receptors, only 17b (SYK-524) with two o-hydroxyphenyl rings showed moderate or pote...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hirayama S,Wada N,Kuroda N,Iwai T,Yamaotsu N,Hirono S,Fujii H,Nagase H

更新日期：2014-10-15 00:00:00