SAR of N-phenyl piperidine based oral integrin alpha5beta1 antagonists.

abstract：:(Me)FGC(Bz)DEVD was radiolabeled with technetium-99m in high yield. This tracer was preferentially accumulated in apoptotic cells in the in vitro studies. Tumor uptake occurred in vivo after cisplatin injection due to the apoptosis induction, which not observed in the untreated tumors. Therefore, (99m)Tc-(Me)FGCDEVD i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bohn P,Mouchard F,Rouvet J,de Boisgrollier AC,Vera P

更新日期：2013-03-01 00:00:00

abstract：:Heterocyclic substituted derivatives of the antipsoriatic anthralin were synthesized and evaluated in vitro for their antiproliferative action against keratinocytes and their ability to induce keratinocyte differentiation. The indole-2-carboxylic acid analogue 2e exhibited the same excellent antiproliferative activity...

journal_title：Bioorganic & medicinal chemistry letters

authors： Müller K,Reindl H,Breu K

更新日期：2001-01-08 00:00:00

abstract：:Elevated triglycerides (TG) contribute towards increased risk for cardiovascular disease. Lipoprotein lipase (LPL) is an enzyme that is responsible for the metabolism of core triglycerides of very-low density lipoproteins (VLDL) and chylomicrons in the vasculature. In this study, we explored the structure-activity rel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Geldenhuys WJ,Caporoso J,Leeper TC,Lee YK,Lin L,Darvesh AS,Sadana P

更新日期：2017-01-15 00:00:00

abstract：:The synthesis and pharmacological evaluation of substituted oximino-ethers 1 and 2 of naphth[1,2-b]- and naphth[2,1-b]-oxepin-5-ones (4 and 8) were carried out. The hypotensive activity of oximino-ethers 1 and 2 was evaluated on anaesthetized cats. The results indicated that 1c caused a fall of 80 mm/Hg for >100' at a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tandon VK,Kumar M,Awasthi AK,Saxena HO,Goswamy GK

更新日期：2004-06-21 00:00:00

abstract：:We describe the identification, SAR, and in vivo pharmacology of a new series of Src-family selective Lck inhibitors. These thienopyridines were designed based on a desire to access the unique residues in the extended hinge region of Lck. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Abbott L,Betschmann P,Burchat A,Calderwood DJ,Davis H,Hrnciar P,Hirst GC,Li B,Morytko M,Mullen K,Yang B

更新日期：2007-03-01 00:00:00

abstract：:Kynurenine monooxygenase (KMO) is a potential drug target for treatment of neurodegenerative disorders such as Huntington's and Alzheimer's diseases. We have evaluated substituted kynurenines as substrates or inhibitors of KMO from Cytophaga hutchinsonii. Kynurenines substituted with a halogen at the 5-position are ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Phillips RS,Anderson AD,Gentry HG,Güner OF,Bowen JP

更新日期：2017-04-15 00:00:00

abstract：:The trans-enantiomers of the commercially important anti-protozoal compound Halofuginone have been prepared and characterized, and the absolute configuration was assigned by X-ray crystallography. The activity of both enantiomers against Cryptosporidium parvum was determined in vitro and related to acute toxicity in v...

journal_title：Bioorganic & medicinal chemistry letters

authors： Linder MR,Heckeroth AR,Najdrowski M,Daugschies A,Schollmeyer D,Miculka C

更新日期：2007-08-01 00:00:00

abstract：:In the present study, an efficient synthesis of some Mannich base of 5-methyl-2-[(2-oxo-2H-chromen-3-yl)carbonyl]-2,4-dihydro-3H-pyrazol-3-one (4a-j) have been described by using conventional and non-conventional (microwave) techniques. Microwave assisted reactions showed that require shorter reaction time and good yi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sivakumar KK,Rajasekaran A,Senthilkumar P,Wattamwar PP

更新日期：2014-07-01 00:00:00

abstract：:We re-examined the accessory site of the 4,5-epoxymorphinan skeleton by camdas conformational analysis in an effort to deign novel delta opioid receptor antagonists. We synthesized three novel compounds (SN-11, 23 and 28) with a 10-methylene bridge and without a 4,5-epoxy ring. Among them, compounds SN-23 (17-isobutyl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nagase H,Osa Y,Nemoto T,Fujii H,Imai M,Nakamura T,Kanemasa T,Kato A,Gouda H,Hirono S

更新日期：2009-05-15 00:00:00

abstract：:The isopolar nonisosteric phosphonate analogs of ApA differing in the position of extra methylene group introduced into the sugar-phosphate backbone, featuring both possible 2',5'- and 3',5'- pairs as well as their conformationally restricted congeners, were investigated for their ability to form complexes with polyU....

journal_title：Bioorganic & medicinal chemistry letters

authors： Pressová M,Endová M,Toĉík Z,Liboska R,Rosenberg I

更新日期：1998-05-19 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：:Triphosphate of a new fluorescent labeled thymidine analogue was incorporated as a substrate for PCR using KOD Dash DNA polymerase forming the corresponding fluorescent labeled DNA which is useful for a DNA probe. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Obayashi T,Masud MM,Ozaki AN,Ozaki H,Kuwahara M,Sawai H

更新日期：2002-04-22 00:00:00

abstract：:The in vitro activity of novel 4-substituted imidazole antifungals was optimized by solid-phase chemistry and parallel synthesis. Potent yeast-selective as well as broad-spectrum antifungal compounds (32 and 20) were discovered. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Saha AK,Liu L,Marichal P,Odds F

更新日期：2000-12-18 00:00:00

abstract：:We report the discovery of the pyrimido-diazepine scaffolds as novel adenine mimics. Structure-based design led to the discovery of analogs with potent inhibitory activity against receptor tyrosine kinases, such as KDR, Flt3 and c-Kit. Compound 14 exhibited low nanomolar KDR enzymatic and cellular potencies (IC(50)=9 ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gracias V,Ji Z,Akritopoulou-Zanze I,Abad-Zapatero C,Huth JR,Song D,Hajduk PJ,Johnson EF,Glaser KB,Marcotte PA,Pease L,Soni NB,Stewart KD,Davidsen SK,Michaelides MR,Djuric SW

更新日期：2008-04-15 00:00:00

abstract：:Mu opioid receptor antagonists have clinical utility and are important research tools. To develop non-peptide and highly selective mu opioid receptor antagonist, a series of 14-O-heterocyclic-substituted naltrexone derivatives were designed, synthesized, and evaluated. These compounds showed subnanomolar-to-nanomolar ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li G,Aschenbach LC,He H,Selley DE,Zhang Y

更新日期：2009-03-15 00:00:00

abstract：:Viral infectivity factor (Vif) is one of the accessory protein of human immunodeficiency virus type I (HIV-1) that inhibits host defense factor, APOBEC3G (A3G), mediated viral cDNA hypermutations. Previous work developed a novel Vif inhibitor 2-amino-N-(2-methoxyphenyl)-6-((4-nitrophenyl)thio)benzamide (1) with strong...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang RH,Wang S,Luo RH,Zhou M,Zhang H,Xu GB,Zhao YL,Li YJ,Wang YL,Yan G,Liao SG,Zheng YT,Li R

更新日期：2019-12-15 00:00:00

abstract：:Rhus verniciflua Stokes has been used as a traditional herbal medicine in Asia. In this study, the effect of R. verniciflua extract on human aromatase (cytochrome P450 19, CYP19) activity was investigated to elucidate the mechanism for the effect of R. verniciflua extract on androgen hormone levels. Androstenedione wa...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park MH,Kim IS,Kim SA,Na CS,Hong CY,Dong MS,Yoo HH

更新日期：2014-04-01 00:00:00

abstract：:Inositols play an important role in membrane lipid metabolism and mitogenic signaling of most cancer cells. There is paucity of data on the distribution of radiolabelled inositols. Based on work previously carried out on 1-deoxy-1-[(18)F]fluoro-scyllo-inositol ([(18)F]2), we began a program of work to label myo-inosit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Carroll L,Perumal M,Vasdev N,Robins E,Aboagye EO

更新日期：2012-10-01 00:00:00

abstract：:A potential anti-HIV and HCV drug candidate is highly desirable as coinfection has become a worldwide public health challenge. A potent compound based on a tetrabutoxy-calix[4]arene scaffold that possesses dual inhibition for both HIV and HCV is described. Structural activity relationship studies demonstrate the effec...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tsou LK,Dutschman GE,Gullen EA,Telpoukhovskaia M,Cheng YC,Hamilton AD

更新日期：2010-04-01 00:00:00

abstract：:A focused library of rhodanine compounds containing novel substituents at the C5-position was synthesized and tested in vitro against a panel of clinically relevant MRSA strains. The present SAR study was based on our lead compound 1 (MIC=1.95 μg/mL), with a focus on identifying optimal C5-arylidene substituents. In o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patel BA,Ashby CR Jr,Hardej D,Talele TT

更新日期：2013-10-15 00:00:00

abstract：:A general protocol for the synthesis of paclitaxel C-10 carbamates is described. The method entails MeI-mediated activation of 2'-O-TBS-7-O-TES-10-O-deacetyl-paclitaxel-10-O-carbonylimidazole prior to reaction with amines. This method is effective for the synthesis of paclitaxel C-10 derivatives, including bifunctiona...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ballatore C,Aspland SE,Castillo R,Desharnais J,Eustaquio T,Sun C,Castellino AJ,Smith AB 3rd

更新日期：2005-05-16 00:00:00

abstract：:In the search for plants, containing compounds with α-glucosidase inhibitory activity, we found that a methanolic extract from the leaves and twigs of Archidendron clypearia (Jack.) Nielsen significantly inhibited rat intestinal sucrase in vitro. A phytochemical investigation of the aqueous layer of an A. clypearia ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thao NP,Luyen BT,Vinh le B,Lee JY,Kwon YI,Kim YH

更新日期：2016-09-01 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：:The synthesis of novel C6-aryl substituted derivatives of 3-(dimethylamino)chroman is described. The novel derivatives display 5-HT(7) receptor affinities that varies from nM to muM, indicating that this small set of derivatives constitute a novel and interesting starting point for further structure-serotonin 5-HT(7) ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Holmberg P,Tedenborg L,Rosqvist S,Johansson AM

更新日期：2005-02-01 00:00:00

abstract：:The development of novel non-phosphopeptide inhibitors for the Src family SH2 domain is described. Several commercially available hydroxyl aromatic acids have been appended off the N-terminus of pYEEIE and the potent phosphopeptide inhibitors of GST-Lck-SH2 were identified via ELISA. The most potent inhibitor, caffeic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park SH,Won J,Lee KH

更新日期：2002-10-07 00:00:00

abstract：:The designed cytosine-carbohydrate hybrid molecule selectively recognized and stabilized the bulged duplex DNA possessing the complementary bulged DNA base, guanine, while the nucleotide base itself did not exhibit any such ability. It was also found that the assistance of the carbohydrate to stabilize the interaction...

journal_title：Bioorganic & medicinal chemistry letters

authors： Idutsu Y,Sasaki A,Matsumura S,Toshima K

更新日期：2005-10-01 00:00:00

abstract：:In order to establish structural elements responsible for inhibition of trypanothione reductase (TR) from Trypanosoma cruzi by 2-aminodiphenylsulfides, a series of dissymmetrical derivatives, corresponding to the replacement of one aromatic moiety by different amines, was synthesized. TR inhibition studies revealed th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Girault S,Davioud-Charvet E,Salmon L,Berecibar A,Debreu MA,Sergheraert C

更新日期：1998-05-19 00:00:00

abstract：:Synthesis of novel 1,2,3-triazole-linked beta-lactam-bile acid conjugates 17-24 using 1,3-dipolar cycloaddition reaction of azido beta-lactam and terminal alkyne of bile acids in the presence of Cu(I) catalyst (click chemistry) have been realized. These molecules were evaluated in vitro for their antifungal and antiba...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vatmurge NS,Hazra BG,Pore VS,Shirazi F,Chavan PS,Deshpande MV

更新日期：2008-03-15 00:00:00

abstract：:Attachment of DOTA to a novel monofluoro-cyclooctyne facilitates bioconjugation to an azide-modified peptide via Cu-free click chemistry. The resulting conjugate was radiolabeled with (111)In to afford a potential targeted molecular imaging agent with high specific activity and an excellent radiochemical purity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Martin ME,Parameswarappa SG,O'Dorisio MS,Pigge FC,Schultz MK

更新日期：2010-08-15 00:00:00

abstract：:Developing efficient controlled release system of insecticide can facilitate the better use of insecticide. We described here a first example of photo-controlled release of an insecticide by linking fipronil with photoresponsive coumarin covalently. The generated coumarin-fipronil (CF) precursor could undergo cleavage...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gao Z,Yuan P,Wang D,Xu Z,Li Z,Shao X

更新日期：2017-06-01 00:00:00