Effective molarity in a nucleic acid-controlled reaction.

abstract：:After the widespread use of the acyclic purine nucleoside analogues for therapy of herpes simplex virus (HSV) infection since the 1980s, new antiviral strategies are urgently needed to counter the emergence of drug-resistant clinical isolates. In this report, we define the anti-HSV efficacies of three optimized 2-amin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiang YF,Qian CW,Xing GW,Hao J,Xia M,Wang YF

更新日期：2012-07-15 00:00:00

abstract：:Derivatives of a CYP1A2 inhibitor rutaecarpine were synthesized to have potent and selective inhibition of human CYP1 members. Structural modelling shows a good fitting of rutaecarpine with the putative active site of human CYP1A2. Among the derivatives, 10- and 11-methoxyrutaecarpine are the most selective CYP1B1 inh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Don MJ,Lewis DF,Wang SY,Tsai MW,Ueng YF

更新日期：2003-08-04 00:00:00

abstract：:In this letter, we describe the first synthesis of two recently isolated flavones 5-carbomethoxymethyl-7-hydroxy-2-pentylchromone (3a), 5-carboethoxymethyl-4',7-dihydroxyflavone (3b) and their derivatives (3c-t), evaluated for their antimicrobial, antioxidant and anticancer activities. Most of the synthesized compound...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamal A,Murty JN,Viswanath A,Sujitha P,Ganesh Kumar C

更新日期：2012-07-15 00:00:00

abstract：:A combinatorial peptidomimetic library containing diversified alpha-methylated amino acids was generated by the Ugi four component condensation (4cc) reaction from acids, amines, isocyanides and ketones in both solution and solid phase synthetic procedures. This one-pot methodology overall gave fair to good yields, wh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim SW,Shin YS,Ro S

更新日期：1998-07-07 00:00:00

abstract：:In an effort to identify a potential back-up to apixaban (Eliquis®), we explored a series of diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing the terminal lactam of apixaban were identified which demonstrated potent FXa binding affinity (FXa Ki), good human plasma anticoagulant...

journal_title：Bioorganic & medicinal chemistry letters

authors： Orwat MJ,Qiao JX,He K,Rendina AR,Luettgen JM,Rossi KA,Xin B,Knabb RM,Wexler RR,Lam PY,Pinto DJ

更新日期：2014-08-01 00:00:00

abstract：:In an effort to find new antibiotics, a novel series of 14-membered macrolides with imidazo[4,5-b]pyridinyl sulfur contained alkyl side chains has been synthesized based on commercially available clarithromycin. Chemical transformation of hydroxy group at position C-3 afforded range of ketolides and acylides. Compared...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu P,Liu L,Chen XZ,Li Y,Liu J,Jin ZP,Wang GQ,Lei PS

更新日期：2009-08-01 00:00:00

abstract：:We report herein the synthesis and stereochemical structure-activity relationships of novel morpholine analogues 12 and 13 with regards to NK1, NK2 and NK3 tachykinin receptor binding affinity. An essential requirement for more potent binding affinities was controlled by absolute configuration. (S,R)-12 and (S,R)-13 e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nishi T,Ishibashi K,Takemoto T,Nakajima K,Fukazawa T,Iio Y,Itoh K,Mukaiyama O,Yamaguchi T

更新日期：2000-08-07 00:00:00

abstract：:Twenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes having a seven-membered ring structure between a bidentate carrier ligand and a platinum atom have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward A549 human non-small cell lung carcinoma and HC...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu H,Cui K,Wang L,Gou S

更新日期：2005-11-15 00:00:00

abstract：:Compounds belonging to a carbazole series have been identified as potent fungal plasma membrane proton adenosine triphophatase (H+-ATPase) inhibitors with a broad spectrum of antifungal activity. The carbazole compounds inhibit the adenosine triphosphate (ATP) hydrolysis activity of the essential fungal H+-ATPase, the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Clausen JD,Kjellerup L,Cohrt KO,Hansen JB,Dalby-Brown W,Winther AL

更新日期：2017-10-01 00:00:00

abstract：:Regiospecific synthesis of 2,3-disubstituted-L-histidines and 2,3-disubstituted histamines starting from L-histidine methyl ester and histamine is reported. The key step involves homolytic free radical alkylation via silver catalyzed oxidative decarboxylation of alkylcarboxylic acids with ammonium persulfate. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Narayanan S,Vangapandu S,Jain R

更新日期：2001-05-07 00:00:00

abstract：:The new binuclear platinum(II) complexes, (1,3-benzenedimethanethiolate-S)di(2,2',2"-terpyridine)diplatinum(II) chloride tetrahydrate, 5, and (1,4-benzenedimethanethiolate-S)di(2,2',2"-terpyridine)diplatinum(II) chloride tetrahydrate, 6, were synthesized in order to investigate the binding of platinum(II) complex with...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kurosaki H,Yamakawa N,Sumimoto M,Kimura K,Goto M

更新日期：2003-03-10 00:00:00

abstract：:Spiro-carboxamides were identified as inhibitors of 11beta-hydroxysteroid-dehydrogenase type 1 by high-throughput screening. Structure-based drug design was used to optimise the initial hit yielding a sub-nanomolar IC(50) inhibitor (0.5nM) on human 11beta-HSD1 with a high binding efficiency index (BEI of 32.7) which w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lepifre F,Christmann-Franck S,Roche D,Leriche C,Carniato D,Charon C,Bozec S,Doare L,Schmidlin F,Lecomte M,Valeur E

更新日期：2009-07-01 00:00:00

abstract：:The SAR studies to optimise both potency and rate of clearance in the rat for a series of pyrimidine and pyridine based VLA-4 antagonists are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Porter JR,Archibald SC,Brown JA,Childs K,Critchley D,Head JC,Hutchinson B,Parton TA,Robinson MK,Shock A,Warrellow GJ,Zomaya A

更新日期：2002-06-17 00:00:00

abstract：:New A-ring modified betulinic acid derivatives having small steric hindrance were prepared and tested for cytotoxic activity on 3 cancer cell lines: 10 compounds showed stronger cytotoxic activity than betulinic acid. Especially, the compounds bearing 1-ene-3-oxo with electron-withdrawing groups at C2 showed strong cy...

journal_title：Bioorganic & medicinal chemistry letters

authors： You YJ,Kim Y,Nam NH,Ahn BZ

更新日期：2003-10-06 00:00:00

abstract：:Electron rich 6-[(dimethylamino)methylene]amino uracil 1, undergoes [4+2] cycloaddition reactions with various in situ generated glyoxylate imine and imine oxides 6 to provide novel pyrimido[4,5-d]pyrimidine derivatives of biological significance, after elimination of dimethylamine from the (1:1) cycloadducts and oxid...

journal_title：Bioorganic & medicinal chemistry letters

authors： Prajapati D,Gohain M,Thakur AJ

更新日期：2006-07-01 00:00:00

abstract：:Novel conformationally-restricted mTOR kinase inhibitors with cyclic sulfone scaffold were designed. Synthesis and structure-activity relationship (SAR) studies are described with emphasis on optimization of the mTOR potency and selectivity against class I PI3Kα kinase. PF-05139962 was identified with excellent mTOR b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu KK,Bailey S,Dinh DM,Lam H,Li C,Wells PA,Yin MJ,Zou A

更新日期：2012-08-01 00:00:00

abstract：:The use of doxorubicin (DOX) in the treatment of solid tumors is limited by cardiotoxicity essentially due to oxidative stress generation. The aim of this study was to identify coumarin derivatives displaying a protective antioxidant activity without affecting DOX antitumoral efficiency. A set of eighteen coumarinic d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Beillerot A,Domínguez JC,Kirsch G,Bagrel D

更新日期：2008-02-01 00:00:00

abstract：:Oligonucleotides consisting of 2'-deoxy-2'(S)-ethinyl-thymidine,-uridine, and -adenosine have been prepared. Whereas the modified pyrimidine oligonucleotides uniformly lead to weaker pairing affinity with DNA and RNA complements, the corresponding adenine oligonucleotides show enhanced thermal stability in duplexes wi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Buff R,Hunziker J

更新日期：1998-03-03 00:00:00

abstract：:Incubation of epicubenol synthase with farnesyl pyrophosphate in the presence of 11.1 atom% H2(18)O gave epicubenol (2) in which the hydroxyl oxygen atom was shown to be derived exclusively from water, as established by GC-selected ion monitoring MS of the derived TMS-epicubenol derivative (15). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cane DE,Ke N

更新日期：2000-01-17 00:00:00

abstract：:In the present study we report the synthesis of halogen-substituted phenanthrene β-diketo acids as new HIV-1 integrase inhibitors. The target phenanthrenes were obtained using both standard thermal- and microwave-assisted synthesis. 4-(6-Chlorophenanthren-2-yl)-2,4-dioxobutanoic acid (18) was the most active compound ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sharma H,Sanchez TW,Neamati N,Detorio M,Schinazi RF,Cheng X,Buolamwini JK

更新日期：2013-11-15 00:00:00

abstract：:Two reactive metabolites were identified in vivo for the dual A(2A)/A(1) receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a number of amide, ether, and amino analogs having comparable in vitro a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shook BC,Rassnick S,Chakravarty D,Wallace N,Ault M,Crooke J,Barbay JK,Wang A,Leonard K,Powell MT,Alford V,Hall D,Rupert KC,Heintzelman GR,Hansen K,Bullington JL,Scannevin RH,Carroll K,Lampron L,Westover L,Russell

更新日期：2010-05-01 00:00:00

abstract：:A series of anthranilodinitrile-based biaryls were synthesized and evaluated in vitro against extracellular promastigotes and intracellular amastigotes of Leishmania donovani. Among various screened compounds, a biaryl with trifluoromethyl group 5f showed 83% inhibition against promastigotes and 70% inhibition against...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh FV,Vatsyayan R,Roy U,Goel A

更新日期：2006-05-15 00:00:00

abstract：:In the search of new antihyperglycemic agents and following rational approach of drug designing here new 2-hydrazolyl-4-thiazolidinone-5-carboxylic acids (4a-g) with pyrazolyl pharmacophore have been synthesized via thia Michael addition reaction of 1-((3-(4-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)thios...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhosle MR,Mali JR,Pal S,Srivastava AK,Mane RA

更新日期：2014-06-15 00:00:00

abstract：:A series of dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)) have been identified. The synthesis, structure-activity relationships and selectivity against several other ion channels are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vaccaro W,Huynh T,Lloyd J,Atwal K,Finlay HJ,Levesque P,Conder ML,Jenkins-West T,Shi H,Sun L

更新日期：2008-12-15 00:00:00

abstract：:The synthesis, SAR, pharmacokinetic profile, and modeling studies of both monocyclic and fused pyrazoles containing substituted N-arylpiperidinyl P4 moieties that are potent and selective factor Xa inhibitors will be discussed. Fused pyrazole analog 16a, with a 2'-methylsulfonylphenyl piperidine P4 group, was shown to...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiao JX,Cheng X,Smallheer JM,Galemmo RA,Drummond S,Pinto DJ,Cheney DL,He K,Wong PC,Luettgen JM,Knabb RM,Wexler RR,Lam PY

更新日期：2007-03-01 00:00:00

abstract：:Peptides containing Nepsilon-thioacetyl-lysine and Nepsilon-acetyl-lysine were evaluated for their de(thio)acetylation catalyzed by human HDAC8 and SIRT1, two distinct protein deacetylases. Nepsilon-Thioacetyl-lysine was found to be a mimic of Nepsilon-acetyl-lysine for HDAC8-catalyzed reaction, but to confer inhibiti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fatkins DG,Monnot AD,Zheng W

更新日期：2006-07-15 00:00:00

abstract：:A MeOH extract of the dry root of Lithospermum erythrorhizon showed strong increasing effect on serine palmitoyltransferase (SPT) in normal human keratinocyte cells (HaCaT cells). Bioassay-guided separation on this extract using repeated chromatography resulted in the isolation of lithospermic acid (1) and two derivat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thuong PT,Kang KW,Kim JK,Seo DB,Lee SJ,Kim SH,Oh WK

更新日期：2009-03-15 00:00:00

abstract：:Phenylpiperazine derivatives were synthesized as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity. Lead optimization led to compound 5k having the potent regulatory activity and demonstrating remarkable protective effects against the lethal challenge of LPS in mice. suggesting that 5k ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hanano T,Adachi K,Aoki Y,Morimoto H,Naka Y,Hisadome M,Fukuda T,Sumichika H

更新日期：2000-05-01 00:00:00

abstract：:A series of substituted 4-anilino-7-phenyl-3-quinolinecarbonitriles has been prepared as Src kinase inhibitors. Optimal activity is observed with compounds that have basic amines attached via the para position of the 7-phenyl ring, and a hydrogen atom at the C-6 position. The best compounds are low nanomolar inhibitor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Berger D,Dutia M,Powell D,Wissner A,DeMorin F,Raifeld Y,Weber J,Boschelli F

更新日期：2002-10-21 00:00:00

abstract：:A series of oligo-peptide based catalysts were prepared using Fmoc solid-phase peptide synthesis. It was found that peptides with N-terminal proline residues catalyzed an aldol reaction yielding enantiomeric enriched product. Peptide H-Pro-Glu-Leu-Phe-OH catalyzed the reaction with good activity and moderate enantiose...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kofoed J,Nielsen J,Reymond JL

更新日期：2003-08-04 00:00:00