Novel fluorescent markers for hypoxic cells of naphthalimides with two heterocyclic side chains for bioreductive binding.

abstract：:Cells have evolved complex biochemical pathways for DNA interstrand crosslink (ICL) removal. Despite the chemotherapeutic importance of ICL repair, there have been few attempts to identify which mechanistic DNA repair inhibitor actually inhibits ICL repair. To identify such compounds, a new and robust ICL repair assay...

journal_title：Bioorganic & medicinal chemistry

authors： Fujii N,Evison BJ,Actis ML,Inoue A

更新日期：2015-11-01 00:00:00

abstract：:Petrosaspongiolides M-R (PM-PR, 1-5) are marine sesterterpenes structurally characterised by a gamma-hydroxybutenolide moiety. They have shown an in vitro and in vivo potent anti-inflammatory activity, mediated by specific inhibition of secretory phospholipase A(2) (sPLA(2) enzymes). The molecular mechanism underlying...

journal_title：Bioorganic & medicinal chemistry

authors： Monti MC,Casapullo A,Riccio R,Gomez-Paloma L

更新日期：2004-03-15 00:00:00

abstract：:The auxins, plant hormones, regulate many aspects of the growth and development of plants. Terfestatin A (TrfA), a novel auxin signaling inhibitor, was identified in a screen of Streptomyces sp. F40 extracts for inhibition of the expression of an auxin-inducible gene. However, the mode of action of TrfA has not been e...

journal_title：Bioorganic & medicinal chemistry

authors： Hayashi K,Yamazoe A,Ishibashi Y,Kusaka N,Oono Y,Nozaki H

更新日期：2008-05-01 00:00:00

abstract：:Based on 2-(4-phenoxybenzoyl)-5-hydroxyindole (2), a novel structural class of CaMKII inhibitors were synthesized and further optimized. The strong acidity of the hydroxyl group and the lipophilic group at the 4 and 6-positions were found to be necessary for strong CaMKII inhibition. Compound 25 was identified as a pr...

journal_title：Bioorganic & medicinal chemistry

authors： Komiya M,Asano S,Koike N,Koga E,Igarashi J,Nakatani S,Isobe Y

更新日期：2012-12-01 00:00:00

abstract：:In this study, a number of 2',4'-BNA- and 2',4'-BNA(NC)-modified siRNAs were designed and synthesized. Their thermal stability, nuclease resistance and gene silencing properties against cultured mammalian cells were evaluated and compared with those of natural siRNAs. The 2',4'-BNA- and 2',4'-BNA(NC)-modified siRNAs (...

journal_title：Bioorganic & medicinal chemistry

authors： Abdur Rahman SM,Sato H,Tsuda N,Haitani S,Narukawa K,Imanishi T,Obika S

更新日期：2010-05-15 00:00:00

abstract：:The effects of Brazilian green propolis ethanol extract on Cry j1-induced cys-leukotrienes and histamine release from peripheral leukocytes of patients with allergic rhinitis were investigated. One of the key mechanisms for the anti-allergic properties of the extract was revealed to be the suppression of cys-LTs relea...

journal_title：Bioorganic & medicinal chemistry

authors： Tani H,Hasumi K,Tatefuji T,Hashimoto K,Koshino H,Takahashi S

更新日期：2010-01-01 00:00:00

abstract：:3-D-Quantitative structure--activity relationships of N-(3-acyloxy-2-benzylpropyl)-N'-dihydroxytetrahydro-benzazepine and tetrahydroisoquinoline and N-(3-acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea analogues as potent vanilloid receptor ligands were investigated using the CoMFA and the COMSIA metho...

journal_title：Bioorganic & medicinal chemistry

authors： Kim KH

更新日期：2002-05-01 00:00:00

abstract：:The cellular penetration (CP) activity of functional molecules has attracted significant attention as one of the most promising new approaches for drug delivery. In particular, cell-penetrating peptides (CPPs) have been studied extensively in cellular engineering. Because there have been few large-scale systematic stu...

journal_title：Bioorganic & medicinal chemistry

authors： Usui K,Kikuchi T,Mie M,Kobatake E,Mihara H

更新日期：2013-05-01 00:00:00

abstract：:We report structural studies in aqueous solution on backbone cyclic peptides that possess potent antimicrobial activity specifically against Pseudomonas sp. The peptides target the β-barrel outer membrane protein LptD, which plays an essential role in lipopolysaccharide transport to the outer membrane. The peptide L27...

journal_title：Bioorganic & medicinal chemistry

authors： Schmidt J,Patora-Komisarska K,Moehle K,Obrecht D,Robinson JA

更新日期：2013-09-15 00:00:00

abstract：:An efficient and practical strategy for the synthesis of (3R,4s,5S)-4-(2-hydroxyethyl) piperidine-3,4,5-triol and its N-alkyl derivatives 8a-f, starting from the D-glucose, is reported. The chiral pool methodology involves preparation of the C-3-allyl-α-D-ribofuranodialdose 10, which was converted to the C-5-amino der...

journal_title：Bioorganic & medicinal chemistry

authors： Markad PR,Sonawane DP,Ghosh S,Chopade BA,Kumbhar N,Louat T,Herman J,Waer M,Herdewijn P,Dhavale DD

更新日期：2014-11-01 00:00:00

abstract：:Cytosolic (TrxR1) and mitochondrial (TrxR2) thioredoxin reductases experience pronounced concentration- and time-dependent inhibition when incubated with the two naphthodianthrones hypericin and pseudohypericin. Pseudohypericin turned out to be a quite strong inhibitor of TrxR1 (IC(50)=4.40μM) being far more effective...

journal_title：Bioorganic & medicinal chemistry

authors： Sorrentino F,Karioti A,Gratteri P,Rigobello MP,Scutari G,Messori L,Bindoli A,Chioccioli M,Gabbiani C,Bergonzi MC,Bilia AR

更新日期：2011-01-01 00:00:00

abstract：:Valinol is part of numerous pharmaceuticals and has various other important applications. Optically pure valinol (ee >99%) was prepared employing different ω-transaminases from the corresponding prochiral hydroxy ketone. By the choice of the enzyme the (R)- as well as the (S)-enantiomer were accessible. Reductive amin...

journal_title：Bioorganic & medicinal chemistry

authors： Fuchs CS,Simon RC,Riethorst W,Zepeck F,Kroutil W

更新日期：2014-10-15 00:00:00

abstract：:In this study a new set of thiazolo[5,4-d]pyrimidine derivatives was synthesized. These derivatives bear different substituents at positions 2 and 5 of the thiazolopyrimidine core while maintaining a free amino group at position-7. The new compounds were tested for their affinity and potency at human (h) A1, A2A, A2B ...

journal_title：Bioorganic & medicinal chemistry

authors： Varano F,Catarzi D,Falsini M,Vincenzi F,Pasquini S,Varani K,Colotta V

更新日期：2018-07-23 00:00:00

abstract：:A high throughput assay was applied to guide the isolation of a new pancreatic α-amylase inhibitor, dracoflavan B, from the dragon's blood resin from Daemonorops draco. Applying C18 column, we successfully isolated both diastereomers and their structures verified by (1)H NMR spectra in comparison with the literature v...

journal_title：Bioorganic & medicinal chemistry

authors： Toh ZS,Wang H,Yip YM,Lu Y,Lim BJ,Zhang D,Huang D

更新日期：2015-12-15 00:00:00

abstract：:A number of 3,5-bis(benzylidene)-4-piperidones 1 and some N-4-(2-aminoethoxy)phenylcarbonyl analogs 3-6 display excellent in vitro antimycobacterial properties. In particular, 1c and 6d are potent antimycobacterials which are well tolerated in mice and are identified as important lead molecules. The nature of both the...

journal_title：Bioorganic & medicinal chemistry

authors： Das U,Das S,Bandy B,Stables JP,Dimmock JR

更新日期：2008-04-01 00:00:00

abstract：:Syntheses of new glycosylated neutral and cationic porphyrin dimers linked at the meso-position via a flexible hydrocarbon chain are described. A detailed 1H and 13C NMR study allows their complete structural elucidation. The UV-visible, fluorescence and MALDI mass spectra are also presented. Photocytotoxicities of th...

journal_title：Bioorganic & medicinal chemistry

authors： Sol V,Chaleix V,Champavier Y,Granet R,Huang YM,Krausz P

更新日期：2006-12-01 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：:The interaction of organic compounds with apoptosis regulatory proteins is an attractive field of research because of its relevance in the development of new chemotherapeutic agents for cancer treatment. Our group designed four new adamantane thiadiazole derivatives (ATDs). The four ATDs were theoretically tested for ...

journal_title：Bioorganic & medicinal chemistry

authors： Ali AG,Mohamed MF,Abdelhamid AO,Mohamed MS

更新日期：2017-01-01 00:00:00

abstract：:3D-Quantitative structure-activity relationships of 2,4,5- and 2,3,4,5-substituted imidazoles as a novel class of potent and nontoxic modulators of Pgp mediated MDR were investigated using CoMFA and COMSIA approaches. The best CoMFA model obtained from 46 imidazole analogues is a two-component model with the following...

journal_title：Bioorganic & medicinal chemistry

authors： Kim KH

更新日期：2001-06-01 00:00:00

abstract：:There is currently interest in the metabolism of the various compounds which make up the vitamin E family, especially with regards to the possible use of vitamin E metabolites as markers of oxidative stress and adequate vitamin E supply. A number of vitamin E metabolites have been described to date and we have recentl...

journal_title：Bioorganic & medicinal chemistry

authors： Pope SA,Burtin GE,Clayton PT,Madge DJ,Muller DP

更新日期：2001-05-01 00:00:00

abstract：:A series of nitrogen-based 20S-hydroxyl camptothecin ester derivatives were prepared. 3-Aminopropionate of camptothecin was found more cytotoxic in vitro on several human tumor cell lines than 3-amidopropionate of camptothecin. Ester 16 showed best antitumor activity in vivo and in vitro in all esters we prepared. ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang CY,Pan XD,Liu HY,Fu ZD,Wei XY,Yang LX

更新日期：2004-07-01 00:00:00

abstract：:Selective targeting of RNA has become a recent priority in drug design strategies due to the emergence of retroviruses, the need for new antibiotics to counter drug resistance, and our increased awareness of the essential role RNA and RNA structures play in the progression of disease. Most organic compounds known to s...

journal_title：Bioorganic & medicinal chemistry

authors： Li K,Fernandez-Saiz M,Rigl CT,Kumar A,Ragunathan KG,McConnaughie AW,Boykin DW,Schneider HJ,Wilson WD

更新日期：1997-06-01 00:00:00

abstract：:A set of new muscarinic antagonists, bridged bicyclic derivatives of 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine (1), was synthesized and tested to evaluate their affinity and selectivity for M(1), M(2), M(3) and M(4) receptor subtypes. The conformational constraint of 1 in a bicyclic structure, and the varia...

journal_title：Bioorganic & medicinal chemistry

authors： Piergentili A,Gentili F,Ghelfi F,Marucci G,Pigini M,Quaglia W,Giannella M

更新日期：2003-09-01 00:00:00

abstract：:A novel series of arylsulfonamide derivatives of (aryloxy)propyl piperidines was designed to obtain potent 5-HT7R antagonists. Among the compounds evaluated herein, 3-chloro-N-{1-[3-(1,1-biphenyl-2-yloxy)2-hydroxypropyl]piperidin-4-yl}benzenesulfonamide (25) exhibited antagonistic properties at 5-HT7R and showed selec...

journal_title：Bioorganic & medicinal chemistry

authors： Canale V,Partyka A,Kurczab R,Krawczyk M,Kos T,Satała G,Kubica B,Jastrzębska-Więsek M,Wesołowska A,Bojarski AJ,Popik P,Zajdel P

更新日期：2017-05-15 00:00:00

abstract：:A detailed investigation of the South China Sea soft coral Sarcophyton trocheliophorum Marenzeller yielded, along with six known terpenes (6-11), the new sarcophytonolides N-R (1-5), whose structures have been elucidated by detailed spectroscopic analysis. Sarcophytonolides N-R are mono- or bicyclic cembranoids charac...

journal_title：Bioorganic & medicinal chemistry

authors： Liang LF,Gao LX,Li J,Taglialatela-Scafati O,Guo YW

更新日期：2013-09-01 00:00:00

abstract：:Phospholipid-linked 'advanced glycation end products' (AGEs) are supposed to play an important role for lipid oxidation in vivo. The identification of the pyrrolecarbaldehyde 1-[2-formyl-5-(hydroxymethyl)-1 H-pyrrol-1-yl]-4,10-dioxo-7-(tetradecanoyloxy)-3,5,9-trioxa- 4lambda5-phosphatricosan-4-olate (7) from model rea...

journal_title：Bioorganic & medicinal chemistry

authors： Lederer MO,Baumann M

更新日期：2000-01-01 00:00:00

abstract：:The synthesis, biological and molecular modeling evaluation of a series of macrocyclic naphthalene diimides is reported. The present investigation expands on the study of structure-activity relationships of prototype compound 2 by constraining the molecule into a macrocyclic structure with the aim of improving its G-q...

journal_title：Bioorganic & medicinal chemistry

authors： Marchetti C,Minarini A,Tumiatti V,Moraca F,Parrotta L,Alcaro S,Rigo R,Sissi C,Gunaratnam M,Ohnmacht SA,Neidle S,Milelli A

更新日期：2015-07-01 00:00:00

abstract：:3'-Deoxy-3'-C-CF3, 2',3'-dideoxy-3'-C-CF3 and 2',3'-unsaturated-3'-C-CF3 nucleoside derivatives of adenosine and cytidine have been synthesized. All these derivatives were prepared by glycosylation of adenine and uracil with a suitable peracylated 3-trifluoromethyl sugar precursor. The resulting protected nucleosides ...

journal_title：Bioorganic & medicinal chemistry

authors： Jeannot F,Gosselin G,Standring D,Bryant M,Sommadossi JP,Giulia Loi A,La Colla P,Mathé C

更新日期：2002-10-01 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：:Several rationally designed analogs of 3-fluoro-2-oxo-3-phenylpropionic acid were chemically synthesized, and the reactions of the hydrate form of these compounds with 4-hydroxyphenylpyruvate dioxygenase from pig liver as inhibitors were examined. Compounds 14a and 14b were found to be potent competitive inhibitors of...

journal_title：Bioorganic & medicinal chemistry

authors： Ling TS,Shiu S,Yang DY

更新日期：1999-07-01 00:00:00