SAR studies of acidic dual γ-secretase/PPARγ modulators.

abstract：:We have designed and synthesized novel irreversible serine protease inhibitors containing aliphatic sulfonyl fluorides as an electrophilic trap. These substituted taurine sulfonyl fluorides derived from taurine or protected amino acids were conveniently synthesized from β-aminoethanesulfonyl chlorides using KF/18-crow...

journal_title：Bioorganic & medicinal chemistry

authors： Brouwer AJ,Ceylan T,Jonker AM,van der Linden T,Liskamp RM

更新日期：2011-04-01 00:00:00

abstract：:The cells of Bacillus stearothermophilus contain an NADH-dependent diacetyl (acetoin) reductase. The enzyme was easily purified to homogeneity, partially characterised, and found to be composed of two subunits with the same molecular weight. In the presence of NADH, it catalyses the stereospecific reduction of diacety...

journal_title：Bioorganic & medicinal chemistry

authors： Giovannini PP,Medici A,Bergamini CM,Rippa M

更新日期：1996-08-01 00:00:00

abstract：:(+/-)-1-(anti-3-Hydroxy-cyclopentyl)-3-(4-methoxy-phenyl)-7-phenylamino-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one (RO4383596) is a potent and selective inhibitor of the pro-angiogenic receptor tyrosine kinases KDR, FGFR, and PDGFR. This agent has an excellent pharmacokinetic profile and is highly efficacious in ro...

journal_title：Bioorganic & medicinal chemistry

authors： McDermott LA,Simcox M,Higgins B,Nevins T,Kolinsky K,Smith M,Yang H,Li JK,Chen Y,Ke J,Mallalieu N,Egan T,Kolis S,Railkar A,Gerber L,Luk KC

更新日期：2005-08-15 00:00:00

abstract：:The anti-inflammatory properties of a heparin-like compound from the shrimp Litopenaeus vannamei are related. Besides reducing significantly (p<0.001) the influx of inflammatory cells to injury site in a model of acute inflammation, shrimp heparin-like compound was able to reduce the matrix metalloproteinase (MMPs) ac...

journal_title：Bioorganic & medicinal chemistry

authors： Brito AS,Arimatéia DS,Souza LR,Lima MA,Santos VO,Medeiros VP,Ferreira PA,Silva RA,Ferreira CV,Justo GZ,Leite EL,Andrade GP,Oliveira FW,Nader HB,Chavante SF

更新日期：2008-11-01 00:00:00

abstract：:Three carboranyltetraphenylporphyrins containing 40 or 80 boron atoms were synthesized and evaluated for their biodistribution and toxicity in EMT-6 tumor-bearing mice. Copper (II) meso-5,10,15,20-tetrakis[3-methoxy-4-(o-carboranylmethoxy)phenyl]porphyrin, 6, and copper (II) meso-5,10,15,20-tetrakis[3-hydroxy-4-(o-car...

journal_title：Bioorganic & medicinal chemistry

authors： Wu H,Micca PL,Makar MS,Miura M

更新日期：2006-08-01 00:00:00

abstract：:As part of our ongoing research on potential new antiepileptic drugs (AEDs), a series of tetramethylcyclopropanecarboxamide derivatives containing benzene ring were designed, synthesized, and evaluated for anticonvulsant activities in the murine maximal electroshock (MES) and subcutaneous pentylenetetrazole (scMet) se...

journal_title：Bioorganic & medicinal chemistry

authors： Shimshoni JA,Bialer M,Yagen B

更新日期：2008-06-01 00:00:00

abstract：:A new series of selective PDE4D inhibitors has been designed and synthesized by replacing 3-methoxy group with 3-difluoromethoxy isoster moiety in our previously reported cathecolic structures. All compounds showed a good PDE4D3 inhibitory activity, most of them being inactive toward other PDE4 isoforms (PDE4A4, PDE4B...

journal_title：Bioorganic & medicinal chemistry

authors： Brullo C,Massa M,Villa C,Ricciarelli R,Rivera D,Pronzato MA,Fedele E,Barocelli E,Bertoni S,Flammini L,Bruno O

更新日期：2015-07-01 00:00:00

abstract：:Bioorthogonal 'click' reactions have recently emerged as promising tools for chemistry and biological applications. By using a combination of two different 'click' reactions, 'double-click' strategies have been developed to attach multiple labels onto biomacromolecules. These strategies require multi-step modification...

journal_title：Bioorganic & medicinal chemistry

authors： Zong H,Goonewardena SN,Chang HN,Otis JB,Baker JR Jr

更新日期：2014-11-01 00:00:00

abstract：:A new class of compounds, the thiopyrano[2,3-e]indol-2-ones, bioisosters of the angular furocoumarin angelicin, was synthesized with the aim of obtaining new photochemotherapeutic agents. In particular 7,8-dimethyl-thiopyranoindolone 6c s showed a remarkable phototoxicity and a great dose UVA dependence reaching IC(50...

journal_title：Bioorganic & medicinal chemistry

authors： Barraja P,Diana P,Montalbano A,Carbone A,Cirrincione G,Viola G,Salvador A,Vedaldi D,Dall'acqua F

更新日期：2008-11-15 00:00:00

abstract：:3-Aryl-4-formylsydnone 4'-phenylthiosemicarbazones (3a-d) and 3-aryl-4-formylsydnone thiosemicarbazones (3e-h), which are precursors of 3-aryl-4-heterocyclic sydnones, are prepared by the condensation of 3-aryl-4-formylsydnones (1a-d) with 4'-phenylthiosemicarbazide (2a) and thiosemicarbazide (2b), respectively. The t...

journal_title：Bioorganic & medicinal chemistry

authors： Shih MH,Ke FY

更新日期：2004-09-01 00:00:00

abstract：:The risk of the presence of haloacetic acids in drinking water as chlorination by-products and the shortage of experimental mutagenicity data for most of them requires a research work. This paper describes a QSAR model to predict direct mutagenicity for these chemicals. The model, able to describe more than 90% of the...

journal_title：Bioorganic & medicinal chemistry

authors： Pérez-Garrido A,González MP,Escudero AG

更新日期：2008-05-15 00:00:00

abstract：:The expression and function of endothelin (ET) receptors is abnormal in cardiovascular diseases, tumor progression, and tumor metastasis. In this study, we prepared two [(18)F]-fluorinated derivatives of the non-peptide ET(A) receptor antagonist PD 156707 and evaluated their ET receptor binding potencies. Ex vivo as w...

journal_title：Bioorganic & medicinal chemistry

authors： Höltke C,Law MP,Wagner S,Kopka K,Faust A,Breyholz HJ,Schober O,Bremer C,Riemann B,Schäfers M

更新日期：2009-10-15 00:00:00

abstract：:A novel series of fluorinated 2-phenylindole derivatives were synthesized and evaluated as β-amyloid imaging probes for PET. The in vitro inhibition assay demonstrated that their binding affinities for Aβ(1-42) aggregates ranged from 28.4 to 1097.8 nM. One ligand was labeled with (18)F ([(18)F]1a) for its high affinit...

journal_title：Bioorganic & medicinal chemistry

authors： Fu H,Yu L,Cui M,Zhang J,Zhang X,Li Z,Wang X,Jia J,Yang Y,Yu P,Jia H,Liu B

更新日期：2013-07-01 00:00:00

abstract：:We have recently communicated that DNA oligonucleotide d(G(3)T(4)G(4)) forms a dimeric G-quadruplex in the presence of K(+) ions [J. Am. Chem. Soc.2003, 125, 7866-7871]. The high-resolution NMR structure of d(G(3)T(4)G(4))(2) G-quadruplex exhibits G-quadruplex core consisting of three stacked G-quartets. The two overh...

journal_title：Bioorganic & medicinal chemistry

authors： Sket P,Crnugelj M,Plavec J

更新日期：2004-11-15 00:00:00

abstract：:The Wnt signaling pathway plays a key role in organ and tissue homeostasis, and when dysregulated, can become a major underlying mechanism of disease, particularly cancer. We reported previously that the anthelmintic drug Niclosamide inhibits Wnt/β-catenin signaling and suppresses colon cancer cell growth in vitro and...

journal_title：Bioorganic & medicinal chemistry

authors： Mook RA Jr,Ren XR,Wang J,Piao H,Barak LS,Kim Lyerly H,Chen W

更新日期：2017-03-15 00:00:00

abstract：:A series of 3-(pyrazolyl)-1,2,5,6-tetrahydropyridine derivatives (B) was synthesized and tested for muscarinic activity in receptor binding assays using [3H]-oxotremorine-M (3H-OXO-M) and [3H]-pirenzepine (3H-PZ) as ligands. Potential muscarinic agonistic or antagonistic properties of the compounds were determined usi...

journal_title：Bioorganic & medicinal chemistry

authors： Plate R,Plaum MJ,de Boer T,Andrews JS,Rae DR,Gibson S

更新日期：1996-02-01 00:00:00

abstract：:A new bis-pyrene-labeled oligonucleotide probe (BP-probe) has been designed for the detection of a single base mismatch in single strand (ss) DNA as a target. The sequence of BP-probe was chosen to form stem-loop structure similar to a molecular beacon (MB-probe), yielding bis-pyrene-labeled molecular beacon (BP-MB-pr...

journal_title：Bioorganic & medicinal chemistry

authors： Yamana K,Ohshita Y,Fukunaga Y,Nakamura M,Maruyama A

更新日期：2008-01-01 00:00:00

abstract：:A growing number of proteins are known to exert their regulatory or biological functions via RNA binding. In some cases genetic interactions allow us to infer candidate targets for RNA directed regulation, but in many other cases identification of potential regulatory targets is problematic. We have developed an in vi...

journal_title：Bioorganic & medicinal chemistry

authors： Brunel C,Ehresmann B,Ehresmann C,McKeown M

更新日期：2001-10-01 00:00:00

abstract：:Bexarotene (1), a retinoid X receptor (RXR) agonist approved for the treatment of cutaneous T cell lymphoma (CTCL), was reported to migrate into baboon brain based on findings obtained by positron emission tomography (PET) with a 11C-labeled tracer. However, co-administration of non-radioactive 1 had no effect on the ...

journal_title：Bioorganic & medicinal chemistry

authors： Takamura Y,Shibahara O,Watanabe M,Fujihara M,Yamada S,Akehi M,Sasaki T,Hirano H,Kakuta H

更新日期：2019-07-15 00:00:00

abstract：:We previously identified dibenzooxepine derivative 1 as a potent PPARγ ligand with a unique binding mode owing to its non-thiazolidinedione scaffold. However, while 1 showed remarkably potent MKN-45 gastric cancer cell aggregation activity, an indicator of cancer differentiation-inducing activity induced by PPARγ acti...

journal_title：Bioorganic & medicinal chemistry

authors： Yamamoto K,Tamura T,Nakamura R,Hosoe S,Matsubara M,Nagata K,Kodaira H,Uemori T,Takahashi Y,Suzuki M,Saito JI,Ueno K,Shuto S

更新日期：2019-11-15 00:00:00

abstract：:Erypoegin K, an isoflavone isolated from the stem bark of Erythrina poeppigiana, has a single chiral carbon in its structure and exists naturally as a racemic mixture. Our previous study showed (S)-erypoegin K selectively exhibits potent anti-proliferative and apoptosis-inducing activity against human leukemia HL-60 c...

journal_title：Bioorganic & medicinal chemistry

authors： Hikita K,Yamakage Y,Okunaga H,Motoyama Y,Matsuyama H,Matsuoka K,Murata T,Nakayoshi T,Oda A,Kato K,Tanaka H,Asao N,Dan S,Kaneda N

更新日期：2021-01-15 00:00:00

abstract：:Novel paclitaxel-mimicking alkaloids were designed and synthesized based on a bioactive conformation of paclitaxel, that is, REDOR-Taxol. The alkaloid 2 bearing a 5-7-6 tricyclic scaffold mimics REDOR-Taxol best among the compounds designed and was found to be the most potent compound against several drug-sensitive an...

journal_title：Bioorganic & medicinal chemistry

authors： Sun L,Veith JM,Pera P,Bernacki RJ,Ojima I

更新日期：2010-10-01 00:00:00

abstract：OBJECTIVE:A new family of 3'-(Mono, di or tri-substituted phenyl)-4'-(4-(methylsulfonyl) phenyl) spiroisoxazoline derivatives containing indanone spirobridge was designed, synthesized, and evaluated for their selective COX-2 inhibitory potency and cytotoxicity on different cell lines. METHODS:A synthetic reaction base...

journal_title：Bioorganic & medicinal chemistry

authors： Abolhasani H,Zarghi A,Komeili Movahhed T,Abolhasani A,Daraei B,Dastmalchi S

更新日期：2021-01-02 00:00:00

abstract：:A series of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles 14a-e, 15a-e, 17a-c, and 18a-d have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The 6-quinolinyl pyrazole analogue 14b inhibited ALK5 phosphorylation ...

journal_title：Bioorganic & medicinal chemistry

authors： Jin CH,Krishnaiah M,Sreenu D,Rao KS,Subrahmanyam VB,Park CY,Son JY,Sheen YY,Kim DK

更新日期：2011-04-15 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：:Concise total syntheses of (R)- and (S)-argentilactone have been developed via enantioselective catalytic allylation (ECA) and ring-closing metathesis pathways (four steps, 39% overall yield and 82-84% ee) from 2-octynal and their in vitro activity against cancer cells is described. ...

journal_title：Bioorganic & medicinal chemistry

authors： de Fatima A,Kohn LK,Antônio MA,de Carvalho JE,Pilli RA

更新日期：2004-10-15 00:00:00

abstract：:Posttranslational modification of proteins with ubiquitin and ubiquitin-like modifiers such as SUMO can be reverted by specific proteases, also referred to as deubiquitinases and isopeptidases, most of which are cysteine-dependent. We have found that the replacement of the conserved C-terminal glycine with propargylam...

journal_title：Bioorganic & medicinal chemistry

authors： Sommer S,Weikart ND,Linne U,Mootz HD

更新日期：2013-05-01 00:00:00

abstract：:Endogenous opioid peptides consist of a conserved amino acid residue of Phe(3) and Phe(4), although their binding modes for opioid receptors have not been elucidated in detail. Endomorphin-2, which is highly selective and specific for the mu opioid receptor, possesses two Phe residues at the consecutive positions 3 an...

journal_title：Bioorganic & medicinal chemistry

authors： Honda T,Shirasu N,Isozaki K,Kawano M,Shigehiro D,Chuman Y,Fujita T,Nose T,Shimohigashi Y

更新日期：2007-06-01 00:00:00

abstract：:The hepatitis C virus (HCV) NS3/4A protease that plays an important role in the viral life cycle has been proven to be an excellent target for the discovery of anti-HCV drugs. Enlightened by some P2-triazole and amide compounds, which had been found as HCV NS3 protease inhibitors, we designed and synthesized a series ...

journal_title：Bioorganic & medicinal chemistry

authors： Shi F,Zhang Y,Xu W

更新日期：2015-09-01 00:00:00

abstract：:An efficient technique is presented which integrates cofactor dependent enzymic phosphorylation and dehydrogenation into a single, closed-loop system by employing phosphoenolpyruvate as the sacrificial reagent for sequential ATP and NAD+ recycling steps. Exemplary applications are developed for the synthesis of 6-phos...

journal_title：Bioorganic & medicinal chemistry

authors： Fessner WD,Sinerius G

更新日期：1994-07-01 00:00:00