A novel neoglycopeptide building block.

abstract：:Hydroxylated 6H-benzo[c]chromen-6-one derivatives (i.e., urolithins) are the main bioavailable metabolites, and biomarkers of ellagitannins present in various nutrition. Although these dietaries, the sources of urolithins, are employed in folk medicine as cognitive enhancer in the treatment of Alzheimer's Disease, uro...

journal_title：Bioorganic & medicinal chemistry

authors： Gulcan HO,Unlu S,Esiringu I,Ercetin T,Sahin Y,Oz D,Sahin MF

更新日期：2014-10-01 00:00:00

abstract：:The kainoids are a class of excitatory and excitotoxic pyrrolidine dicarboxylates that act at ionotropic glutamate receptors. The kainoids bind kainate receptors with high affinity and, while binding affinity is lower at AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptors, they are active in func...

journal_title：Bioorganic & medicinal chemistry

authors： Carcache LM,Rodriguez J,Rein KS

更新日期：2003-02-20 00:00:00

abstract：:Matrix metalloproteinases are implicated in a wide range of pathophysiological processes and potent selective inhibitors for these enzymes continue to be eagerly sought. 5,5-Disubstituted barbiturates hold promise as inhibitor types being stable in vivo and relatively selective for the gelatinases (MMP-2 and MMP-9). I...

journal_title：Bioorganic & medicinal chemistry

authors： Wang J,Medina C,Radomski MW,Gilmer JF

更新日期：2011-08-15 00:00:00

abstract：:All-trans-retinoic acid (ATRA) as a physiological metabolite of vitamin A is widely applied in the treatment of cancer, skin, neurodegenerative and autoimmune diseases. CYP26A1 enzyme, induced by ATRA in liver and target tissues, metabolizes ATRA into 4-hydroxyl-RA. Inhibition of CYP26A1 metabolic enzyme represents a ...

journal_title：Bioorganic & medicinal chemistry

authors： Sun B,Liu K,Han J,Zhao LY,Su X,Lin B,Zhao DM,Cheng MS

更新日期：2015-10-15 00:00:00

abstract：:A novel peptidyl chemosensor (PySO2-His-Gly-Gly-Lys(PySO2)-NH2, 1) was synthesized by incorporation of two pyrene (Py) fluorophores into the tetrapeptide using sulfonamide group. Compound 1 exhibited selective fluorescence response towards Hg(II) over the other metal ions in aqueous buffered solutions. Furthermore, 1 ...

journal_title：Bioorganic & medicinal chemistry

authors： Thirupathi P,Lee KH

更新日期：2013-12-15 00:00:00

abstract：:(R)-1-(10,11-Dihydro-dibenzo[b,f]azepin-5-yl)-3-methylamino-propan-2-ol ((R)-OHDMI) and (S,S)-1-cyclopentyl-2-(5-fluoro-2-methoxy-phenyl)-1-morpholin-2-yl-ethanol (CFMME) were synthesized and found to be potent inhibitors of norepinephrine reuptake. Each was labelled efficiently in its methyl group with carbon-11 (t(1...

journal_title：Bioorganic & medicinal chemistry

authors： Schou M,Pike VW,Sóvágó J,Gulyás B,Gallagher PT,Dobson DR,Walter MW,Rudyk H,Farde L,Halldin C

更新日期：2007-01-15 00:00:00

abstract：:Scutione (1), a new norquinonemethide triterpene with a netzahualcoyene type skeleton, has been isolated from the root bark of Maytenus scutioides (Celastraceae) by bioactivity-directed fractionation. The structure of 1 has been elucidated by means of 1H and 13C NMR spectroscopic studies, including 1H-13C heteronuclea...

journal_title：Bioorganic & medicinal chemistry

authors： González AG,Alvarenga NL,Ravelo AG,Bazzocchi IL,Ferro EA,Navarro AG,Moujir LM

更新日期：1996-06-01 00:00:00

abstract：:Endothelial dysfunction and consequent reduction of biosynthesis of endogenous nitric oxide (NO) play an important pathogenetic role in the cardiovascular complications associated with type II diabetes. In this work, the hybrid drugs 3a and 3b, nitrooxymethylbenzoate-derivatives of 1 (which is a hydroxylated active me...

journal_title：Bioorganic & medicinal chemistry

authors： Calderone V,Rapposelli S,Martelli A,Digiacomo M,Testai L,Torri S,Marchetti P,Breschi MC,Balsamo A

更新日期：2009-08-01 00:00:00

abstract：:A series of arylidene N-alkoxydiketopiperazines was designed and stereoselectively synthesized via oxime-ether formation and intramolecular acylation. Possible cyclization and acid-catalyzed rearrangement-fragmentation mechanisms were discussed. The crystal structure of the novel diketopiperazine further confirmed the...

journal_title：Bioorganic & medicinal chemistry

authors： Tian X,Feng J,Fan SM,Zhen XL,Han JR,Liu SX

更新日期：2016-11-01 00:00:00

abstract：:Analogues of mitoQ and idebenone were synthesized to define the structural elements that support oxygen consumption in the mitochondrial respiratory chain. Eight analogues were prepared and fully characterized, then evaluated for their ability to support oxygen consumption in the mitochondrial respiratory chain. While...

journal_title：Bioorganic & medicinal chemistry

authors： Duveau DY,Arce PM,Schoenfeld RA,Raghav N,Cortopassi GA,Hecht SM

更新日期：2010-09-01 00:00:00

abstract：:Two of the histone deacetylases, TbDAC1 and TbDAC3, have been reported to be essential genes in trypanosomes. Therefore, we tested the activity of a panel of human histone deacetylase inhibitors (HDACi) for their ability to block proliferation of Trypanosoma brucei brucei. Among the HDACi's, the hydroxamic acid deriva...

journal_title：Bioorganic & medicinal chemistry

authors： Carrillo AK,Guiguemde WA,Guy RK

更新日期：2015-08-15 00:00:00

abstract：:A series of 18 cycloalkyl arylpyrimidines (CAPYs) were designed from lead compounds diarylpyrimidines (DAPYs), synthesized and evaluated for in vitro anti-HIV activity. Among them, the compound 1p displayed potent anti-HIV-1 activity against WT HIV-1 with an EC(50) value of 0.055 μM and a selectivity index (SI) >7290....

journal_title：Bioorganic & medicinal chemistry

authors： Gu SX,Yang SQ,He QQ,Ma XD,Chen FE,Dai HF,Clercq ED,Balzarini J,Pannecouque C

更新日期：2011-12-01 00:00:00

abstract：:A novel series of 8-amino imidazo[1,2-a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyraz...

journal_title：Bioorganic & medicinal chemistry

authors： Sayer JR,Walldén K,Pesnot T,Campbell F,Gane PJ,Simone M,Koss H,Buelens F,Boyle TP,Selwood DL,Waksman G,Tabor AB

更新日期：2014-11-15 00:00:00

abstract：:Fourteen hybrids of farnesylthiosalicylic acid (FTS) with various diamines were synthesized and biologically evaluated. It was found that FTS-monoamide molecules (10a-g) displayed strong anti-proliferative activity against seven human cancer cell lines, superior to FTS and FTS-bisamide compounds (11a-g). The mono-amid...

journal_title：Bioorganic & medicinal chemistry

authors： Ling Y,Wang Z,Zhu H,Wang X,Zhang W,Wang X,Chen L,Huang Z,Zhang Y

更新日期：2014-01-01 00:00:00

abstract：:In radiation therapy, adverse side effects are often induced due to the excessive cell death that occurs in radiosensitive normal cells. The radiation-induced cell death of normal cells is caused, at least in part, by apoptosis, which undergoes via activation of p53 and increase in the p53 protein, a zinc-containing t...

journal_title：Bioorganic & medicinal chemistry

authors： Ariyasu S,Sawa A,Morita A,Hanaya K,Hoshi M,Takahashi I,Wang B,Aoki S

更新日期：2014-08-01 00:00:00

abstract：:When a neutral solution of thymidine and ascorbic acid was irradiated with UV light of wavelength longer than 300 nm in the presence of salicylic acid as a photosensitizer, six product peaks appeared in an HPLC chromatogram in addition to small amounts of thymidine dimers. The six products were identified as three pai...

journal_title：Bioorganic & medicinal chemistry

authors： Suzuki T,Kishida Y

更新日期：2019-10-01 00:00:00

abstract：:Introduction of an alkylcarboxylic acid unit, which is a partial structure of endogenous peroxisome proliferator-activated receptor (PPAR) ligands, into a phenethylphenylphthalimide skeleton, which possesses liver X receptor (LXR) antagonistic activity, afforded novel PPAR ligands. The results of structure-activity re...

journal_title：Bioorganic & medicinal chemistry

authors： Motoshima K,Ishikawa M,Hashimoto Y,Sugita K

更新日期：2011-05-15 00:00:00

abstract：:The chemistries of S-nitroso-DL-penicillamine (SNAP) and S-nitrosoglutathione (GSNO) in relation to their ability to relax vascular smooth muscle and prevent platelet aggregation have been investigated. Metal ion catalysis greatly accelerates the decomposition of SNAP, but has little effect on GSNO. Instead, NO releas...

journal_title：Bioorganic & medicinal chemistry

authors： Askew SC,Butler AR,Flitney FW,Kemp GD,Megson IL

更新日期：1995-01-01 00:00:00

abstract：:Geranylgeranyl diphosphate synthase (GGDPS) inhibitors are of potential therapeutic interest as a consequence of their activity against the bone marrow cancer multiple myeloma. A series of bisphosphonates linked to an isoprenoid tail through an amide linkage has been prepared and tested for the ability to inhibit GGDP...

journal_title：Bioorganic & medicinal chemistry

authors： Goetz DB,Varney ML,Wiemer DF,Holstein SA

更新日期：2020-08-15 00:00:00

abstract：:A series of indole analogs that are synthesized using the scaffold of a potent radiosensitizer, YTR107, were tested for their ability to alter the solubility of phosphorylated nucleophosmin 1 (pNPM1). NPM1 is critical for DNA double strand break (DSB) repair. In response to formation of DNA DSBs, phosphorylated T199 N...

journal_title：Bioorganic & medicinal chemistry

authors： Penthala NR,Crooks PA,Freeman ML,Sekhar KR

更新日期：2015-07-01 00:00:00

abstract：:Two series of combretastatin A4 derivatives (acrylamide=carboxamide and carbamate) were synthesized in order to improve the water solubility and stabilize the cis-configuration of the double bond. Their cytotoxic effects were evaluated against MCF-7, KB-3-1 and IGROV human cancer cell lines, as well as their inhibitor...

journal_title：Bioorganic & medicinal chemistry

authors： Borrel C,Thoret S,Cachet X,Guénard D,Tillequin F,Koch M,Michel S

更新日期：2005-06-01 00:00:00

abstract：:In order to find novel and environmental friendly insecticides targeting the ryanodine receptor, three series of novel phthalamides containing heptafluoroisopropyl group, low fluorine atoms group and non-fluorine group were designed and synthesized. 35 novel structures of three series were obtained. Insecticidal activ...

journal_title：Bioorganic & medicinal chemistry

authors： Chen Y,Li Y,Pan L,Liu J,Wan Y,Chen W,Xiong L,Yang N,Song H,Li Z

更新日期：2014-11-15 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

abstract：:Emerging as an epidemic of the 21st century type 2 diabetes has become a major health problem throughout the globe. The number of deaths attributable to diabetes reflects the insufficient glycemic control achieved with the treatments used in recent past. DPP-4 inhibitors have been investigated as a new therapy with no...

journal_title：Bioorganic & medicinal chemistry

authors： Havale SH,Pal M

更新日期：2009-03-01 00:00:00

abstract：:In the current study, a series of pyrazole-sulfonamide derivatives (2-14) were synthesized, characterized, and the inhibition effects of the derivatives on human carbonic anhydrases (hCA I and hCA II) were investigated as in vitro. Structures of these sulfonamides were confirmed by FT-IR, (1)H NMR, (13)C NMR and LC-MS...

journal_title：Bioorganic & medicinal chemistry

authors： Balseven H,Mustafa İşgör M,Mert S,Alım Z,Beydemir S,Ok S,Kasımoğulları R

更新日期：2013-01-01 00:00:00

abstract：:(1S,2E,4S,6R,7E,11E)-2,7,11-Cembratriene-4,6-diol (1) and its 4-epi-analog (2) are the cembranoid precursors to several key flavor ingredients in most Nicotiana (tobacco) species. Nearly 40-60% of 1 and 2 are purposely degraded during the commercial tobacco fermentation. However, 1 and 2 display promising bioactivitie...

journal_title：Bioorganic & medicinal chemistry

authors： Ebrahim HY,Mohyeldin MM,Hailat MM,El Sayed KA

更新日期：2016-11-15 00:00:00

abstract：:We investigated sequence-specific DNA alkylation using conjugates between the N-methylpyrrole (Py)-N-methylimidazole (Im) polyamide and the DNA alkylating agent, chlorambucil, or 1-(chloromethyl)-5-hydroxy-1,2-dihydro-3H-benz[e]indole (seco-CBI). Polyamide-chlorambucil conjugates 1-4 differed in the position at which ...

journal_title：Bioorganic & medicinal chemistry

authors： Minoshima M,Bando T,Shinohara K,Kashiwazaki G,Nishijima S,Sugiyama H

更新日期：2010-02-01 00:00:00

abstract：:In continuing our screening program of naphthoquinone activity against Trypanosoma cruzi, the aetiological agent of Chagas' disease, new beta-lapachone-based 1,2,3-triazoles, 3-arylamino-nor-beta-lapachones, 3-alkoxy-nor-beta-lapachones and imidazole anthraquinones were synthesised and evaluated against bloodstream tr...

journal_title：Bioorganic & medicinal chemistry

authors： da Silva EN Jr,Guimarães TT,Menna-Barreto RF,Pinto Mdo C,de Simone CA,Pessoa C,Cavalcanti BC,Sabino JR,Andrade CK,Goulart MO,de Castro SL,Pinto AV

更新日期：2010-05-01 00:00:00

abstract：:In recent years, special attention has been paid to the A3 adenosine receptor (A3AR) as a possible pharmacological target to treat intestinal inflammation. In this work, it was set up a novel method to quantify the concentration of a promising anti-inflammatory agent inside and outside of intestinal barrier using the ...

journal_title：Bioorganic & medicinal chemistry

authors： Buccioni M,Dal Ben D,Lambertucci C,Martí Navia A,Ricciutelli M,Spinaci A,Volpini R,Marucci G

更新日期：2019-08-01 00:00:00

abstract：:Alternative splicing of the androgen receptor (AR) is frequently observed in castration resistant prostate cancer (CRPC). One AR isoform, the AR-V7 splice variant, is a constitutively active transcription factor which lacks a ligand binding domain and is therefore undruggable. AR-V7 expression correlates with resistan...

journal_title：Bioorganic & medicinal chemistry

authors： Melnyk JE,Steri V,Nguyen HG,Hann B,Feng FY,Shokat KM

更新日期：2020-10-15 00:00:00