Zinc(II)-mediated inhibition of a ribonuclease by an N-hydroxyurea nucleotide.

abstract：:From a readily available 5-C-Me ribofuranoside, we have realized a reliable route to valuable 5'-deoxy-5'-amino-5'-C-methyl adenosine derivatives at gram scale with confirmed stereochemistry. These adenosine derivatives are useful starting materials for the preparation of 5'-deoxy-5'-amino-5'-C-methyl adenosine deriva...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu T,Xie W,Li C,Ren H,Mao Y,Chen G,Cheng M,Zhao D,Shen J,Li J,Zhou Y,Xiong B,Chen YL

更新日期：2017-11-15 00:00:00

abstract：:A novel cys-annexin A5 with a single cysteine-residue at its concave side has been developed by site-directed mutagenesis to allow conjugation through thiol-chemistry without affecting its apoptotic cell binding properties and was derivatized with HYNIC in a 1:1 stoichiometry. Similar to that of the 1st generation 99m...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fonge H,de Saint Hubert M,Vunckx K,Rattat D,Nuyts J,Bormans G,Ni Y,Reutelingsperger C,Verbruggen A

更新日期：2008-07-01 00:00:00

abstract：:A comprehensive investigation of chemical constituents from brown algae Stoechospermum marginatum yielded ten known spatane compounds (1-10). To develop the compound libraries on these scaffolds, a series of semi synthetic derivatives was prepared (1a-1d, 2a, 4a, 11 and 12) and investigated for their anti-microbial an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chinnababu B,Purushotham Reddy S,Sankara Rao P,Loka Reddy V,Sudheer Kumar B,Rao JV,Prakasham RS,Suresh Babu K

更新日期：2015-06-15 00:00:00

abstract：:The identification and optimization of a series of substituted tetrahydro-beta-carbolines with potent activity against human papillomavirus is described. Structure-activity studies focused on the substitution pattern and chirality of the beta-carboline ring system are discussed. Optimization of these parameters led to...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miller JF,Turner EM,Sherrill RG,Gudmundsson K,Spaltenstein A,Sethna P,Brown KW,Harvey R,Romines KR,Golden P

更新日期：2010-01-01 00:00:00

abstract：:Caffeic acid derivatives are increasingly regarded as potential oncoprotective that could inhibit both the initiation and progression of cancer. Here we have synthesized seven 1-arylnaphthalene lignans and related compounds and tested their impact on breast cancer cell growth in tissue culture. The product of the oxid...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bailly F,Toillon RA,Tomavo O,Jouy N,Hondermarck H,Cotelle P

更新日期：2013-01-15 00:00:00

abstract：:A series of imidazolopyrazinones 3, substituted at C-2, and C-2/C-6, has been prepared. The compounds behaved as quenchers of superoxide anion. The more active compounds are structurally related to coelenterazine, a natural substrate of marine bioluminescence. Theoretical parameters based on Hartree-Fock instabilities...

journal_title：Bioorganic & medicinal chemistry letters

authors： Devillers I,Dive G,De Tollenaere C,Falmagne B,de Wergifosse B,Rees JF,Marchand-Brynaert J

更新日期：2001-09-03 00:00:00

abstract：:Structure-based design, synthesis, and biological evaluation of a series of peptidomimetic beta-secretase inhibitors incorporating hydroxyethylamine isosteres are described. We have identified inhibitor 24 which has shown exceedingly potent activity in memapsin 2 enzyme inhibitory (K(i) 1.8 nM) and cellular (IC(50)=1 ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ghosh AK,Kumaragurubaran N,Hong L,Kulkarni S,Xu X,Miller HB,Reddy DS,Weerasena V,Turner R,Chang W,Koelsch G,Tang J

更新日期：2008-02-01 00:00:00

abstract：:Seventy-two novel 1,3,4-oxadiazole thioether derivatives containing different flexible-chain moieties were designed and synthesized. The nematicidal activities of all the title compounds were evaluated, and some compounds showed excellent nematicidal activities against citrus nematodes. The compounds 15, 16, 18, 27, 4...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen J,Wei C,Wu S,Luo Y,Wu R,Hu D,Song B

更新日期：2020-04-15 00:00:00

abstract：:Two novel constrained l-AP4 analogues, (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines (7) and (8), were synthesized and evaluated as mGluR ligands. Compound 7 showed to be a group III mGluRs agonist with micromolar activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Amori L,Serpi M,Marinozzi M,Costantino G,Diaz MG,Hermit MB,Thomsen C,Pellicciari R

更新日期：2006-01-01 00:00:00

abstract：:The proprotein convertases PCSK8 and PCSK4 are, respectively, the 8th and 4th members of Ca(+2)-dependent serine endoprotease of Proprotein Convertase Subtilisin Kexin (PCSK) super family structurally related to the bacterial subtilisin and yeast kexin. The membrane bound PCSK8 (also called SKI-1 or S1P) is implicated...

journal_title：Bioorganic & medicinal chemistry letters

authors： Basak A,Goswami M,Rajkumar A,Mitra T,Majumdar S,O'Reilly P,Bdour HM,Trudeau VL,Basak A

更新日期：2015-01-01 00:00:00

abstract：:A series of MT-II related cyclic peptides, based on potent but non-selective hMC4R agonist (Penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2)) was prepared in which His(6) residue was systematically substituted. Two of the most interesting peptides identified in this study are Penta-c[Asp-5-ClAtc-DPhe-Arg-Trp-Lys]-N...

journal_title：Bioorganic & medicinal chemistry letters

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

更新日期：2003-04-07 00:00:00

abstract：:A series of (R)-3-(N-methylpyrrolidin-2-ylmethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives (2) have been prepared using parallel synthesis, and their structure-activity relationship studied. High affinity human 5-HT(1B/1D) (h5-HT(1B/1D)) ligands have been identified. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Egle I,MacLean N,Demchyshyn L,Edwards L,Slassi A,Tehim A

更新日期：2003-10-20 00:00:00

abstract：:The first enantioselective biocatalytic synthesis of (S)-monastrol has been developed via an unexpected and unusual enzymatic pathway as suitable route. Whereas attempts for a direct hydrolysis of racemic monastrol were not successful, formation of racemic O-butanoyl monastrol and subsequent enantioselective hydrolysi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Blasco MA,Thumann S,Wittmann J,Giannis A,Gröger H

更新日期：2010-08-01 00:00:00

abstract：:Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised intracellular levels of the amino acid, cystine. If untreated, the disease, progressively deteriorates towards end stage renal disease (ESRD) at the end of the first decade. The disease is caused by a defect in the lysosomal transpor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Omran Z,Kay G,Hector EE,Knott RM,Cairns D

更新日期：2011-04-15 00:00:00

abstract：:Novel potent derivatives of (azol-1-yl)methyl-N-arylbenzamides with improved solubility (>3mM) are described as ATP-competitive inhibitors of vascular endothelial growth factor receptor 2 (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity reaching IC(50)<100 nM in the enzymatic assay. The compounds also inh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kiselyov AS,Semenova M,Semenov VV,Piatnitski E

更新日期：2006-03-15 00:00:00

abstract：:2,6-Diamino-4,N-diarylpyridines were identified as potent, isoform selective inhibitors of the enzymatic activity of lysophosphatidic acid acyltransferase-beta (LPAAT-beta). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hong F,Hollenback D,Singer JW,Klein P

更新日期：2005-11-01 00:00:00

abstract：:Chemoselective purification technologies have seen great success in biomolecule isolation, with a classic example being the genetically-encoded His tag utilized to enrich desired proteins from a crude lysate. We sought to translate this purification tactic into a powerful tool for the isolation of natural products and...

journal_title：Bioorganic & medicinal chemistry letters

authors： Trader DJ,Carlson EE

更新日期：2015-11-01 00:00:00

abstract：:Based on our earlier reported neuropeptide FF receptors antagonist (RF9), we carried out an extensive structural exploration of the N-terminus part of the amidated dipeptide Arg-Phe-NH(2) in order to establish a structure-activity relationships (SAR) study towards both NPFF receptor subtypes. This SAR led to the disco...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gealageas R,Schneider S,Humbert JP,Bertin I,Schmitt M,Laboureyras E,Dugave C,Mollereau C,Simonnet G,Bourguignon JJ,Simonin F,Bihel F

更新日期：2012-12-15 00:00:00

abstract：:In the course of screening for a novel anticancer drug candidate, we previously isolated HY251 with the molecular structure of 3-propyl-2-vinyl-1,2,3,3a,3b,6,7,7a,8,8a-decahydrocyclopenta[a]indene-3,3a,7a,8a-tetraol from the roots of Aralia continentalis. The current study was designed to evaluate the detailed mechani...

journal_title：Bioorganic & medicinal chemistry letters

authors： Oh HL,Lee CH

更新日期：2011-03-01 00:00:00

abstract：:A highly practicable synthesis of both enantiomers of 3-hydroxypipecolic acid derivatives 1, 2, 3, 4 is described. Screening of these molecules for glycosidase inhibition has been examined. Compound 3 was shown to be a potent inhibitor of beta-N-acetylglucosaminidase as well as Escherichia coli beta-glucuronidase. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohara C,Takahashi R,Miyagawa T,Yoshimura Y,Kato A,Adachi I,Takahata H

更新日期：2008-03-15 00:00:00

abstract：:Taspase1 is a threonine protease responsible for cleaving MLL (Mixed-Lineage Leukemia) to achieve proper HOX gene expression. Subsequent studies identified additional Taspase1 substrates including Transcription Factor IIA (TFIIA) and Drosophila HCF. Taspase1 is essential for cell proliferation and is overexpressed in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JT,Chen DY,Yang Z,Ramos AD,Hsieh JJ,Bogyo M

更新日期：2009-09-01 00:00:00

abstract：:Thirty-five novel chromone derivatives containing dithioacetal moiety were designed, synthesized, and their anti-TMV activities were evaluated through half-leaf method. The results showed compound c23 illustrates highly curative, protective and inactivating activities against TMV at 500 mg/L, with the values of 68.8%,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li M,Zan N,Huang M,Jiang D,Hu D,Song B

更新日期：2020-03-01 00:00:00

abstract：:In general, serine protease chymase inhibitors readily decompose in plasma. We previously found that thiazolidine-2,4-dione and thiadiazole derivatives are also unstable. Using a pharmacophore-based database search, we identified a benzo[b]thiophen-2-sulfonamide derivative as a stable chymase inhibitor. Finding a lead...

journal_title：Bioorganic & medicinal chemistry letters

authors： Koide Y,Tatsui A,Hasegawa T,Murakami A,Satoh S,Yamada H,Kazayama S,Takahashi A

更新日期：2003-01-06 00:00:00

abstract：:Benzothiazole benzimidazole (S)-isothiazolidinone ((S)-IZD) derivatives 5 were discovered through a peptidomimetic modification of the tripeptide (S)-IZD protein tyrosine phosphatase 1B (PTP1B) inhibitor 1. These derivatives are potent, competitive, and reversible inhibitors of PTP1B with improved caco-2 permeability....

journal_title：Bioorganic & medicinal chemistry letters

authors： Sparks RB,Polam P,Zhu W,Crawley ML,Takvorian A,McLaughlin E,Wei M,Ala PJ,Gonneville L,Taylor N,Li Y,Wynn R,Burn TC,Liu PC,Combs AP

更新日期：2007-02-01 00:00:00

abstract：:Sphingosine-1-phosphate (S1P) is a ubiquitous, endogenous small molecule that is synthesized by two isoforms of sphingosine kinase (SphK1 and 2). Intervention of the S1P signaling pathway has attracted significant attention because alteration of S1P levels is linked to several disease states including cancer, fibrosis...

journal_title：Bioorganic & medicinal chemistry letters

authors： Congdon MD,Childress ES,Patwardhan NN,Gumkowski J,Morris EA,Kharel Y,Lynch KR,Santos WL

更新日期：2015-11-01 00:00:00

abstract：:3-(N-Alkyl)aminopropylphosphonic acids are potent agonists of four of the five known sphingosine-1-phosphate (S1P) receptor subtypes. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hale JJ,Doherty G,Toth L,Li Z,Mills SG,Hajdu R,Ann Keohane C,Rosenbach M,Milligan J,Shei GJ,Chrebet G,Bergstrom J,Card D,Rosen H,Mandala S

更新日期：2004-07-05 00:00:00

abstract：:A series of transdermal permeation enhancers based on dicarboxylic acid esters was studied. Single-chain amphiphiles were markedly more effective than the double-chain ones. Monododecyl maleate, that is a cis derivative, was a more potent enhancer than its trans isomer, while the activity of succinates strongly depend...

journal_title：Bioorganic & medicinal chemistry letters

authors： Novotný M,Hrabálek A,Janůsová B,Novotný J,Vávrová K

更新日期：2009-01-15 00:00:00

abstract：:A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Webster SP,Ward P,Binnie M,Craigie E,McConnell KM,Sooy K,Vinter A,Seckl JR,Walker BR

更新日期：2007-05-15 00:00:00

abstract：:The first example of dual inhibitors for matrix metalloproteinase (MMP) and cathepsin is described. An appropriate alignment of peptide-parts and two different specific functional groups in one molecule led to the discovery of a potent dual inhibitor (3a). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yamamoto M,Ikeda S,Kondo H,Inoue S

更新日期：2002-02-11 00:00:00

abstract：:We report the use of fragment screening and fragment based drug design to develop a PI3γ kinase fragment hit into a lead. Initial fragment hits were discovered by high concentration biochemical screening, followed by a round of virtual screening to identify additional ligand efficient fragments. These were developed i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hughes SJ,Millan DS,Kilty IC,Lewthwaite RA,Mathias JP,O'Reilly MA,Pannifer A,Phelan A,Stühmeier F,Baldock DA,Brown DG

更新日期：2011-11-01 00:00:00