abstract：:A protein-cleaving catalyst highly selective for a disease-related protein can be used as a catalytic drug. As the first protein-cleaving catalyst selective for a protein substrate, a catalyst for myoglobin (Mb) was designed by attaching the Cu(II) or Co(III) complex of cyclen to a binding site searched by a combinato...

journal_title：Bioorganic & medicinal chemistry

authors： Jeon JW,Son SJ,Yoo CE,Hong IS,Suh J

更新日期：2003-07-03 00:00:00

abstract：:The synthesis of a neoglycopeptide building block is described. The key step is a cycloaddition where the chemistry is orthogonal to standard glycosyl transfer methodology. Also described is some exploratory chemistry of the building block. ...

journal_title：Bioorganic & medicinal chemistry

authors： Bartolozzi A,Li B,Franck RW

更新日期：2003-07-03 00:00:00

abstract：:N-[(18)F]Fluoroethyl-4-piperidyl acetate ([(18)F]FEtP4A) was synthesized and evaluated as a PET tracer for imaging brain acetylcholinesterase (AchE) in vivo. [(18)F]FEtP4A was previously prepared by reacting 4-piperidyl acetate (P4A) with 2-[(18)F]fluoroethyl bromide ([(18)F]FEtBr) at 130 degrees C for 30 min in 37% r...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang MR,Furutsuka K,Maeda J,Kikuchi T,Kida T,Okauchi T,Irie T,Suzuki K

更新日期：2003-06-12 00:00:00

abstract：:Mycothiol (MSH, 1-D-myo-inosityl 2-(N-acetyl-L-cysteinyl)amido-2-deoxy-alpha-D-glucopyranoside) is the principal low molecular weight thiol in actinomycetes. The enzyme 1-D-myo-inosityl 2-N-acetamido-2-deoxy-alpha-D-glucopyranoside deacetylase (AcGI deacetylase) is involved in the biosynthesis of MSH and forms the fre...

journal_title：Bioorganic & medicinal chemistry

authors： Nicholas GM,Eckman LL,Kovác P,Otero-Quintero S,Bewley CA

更新日期：2003-06-12 00:00:00

abstract：:A series of 2-sec-amino-3H-quinazolin-4-ones (4a-p) and 4-sec-amino-2-chloroquinazolines (5a-b) have been synthesized by nucleophilic substitution reaction of 2-chloro-4(3H)-quinazolones (3) and 2,4-dichloroquinazolines (2) with amines, respectively. Most of the synthesized compounds were evaluated for antihyperglycem...

journal_title：Bioorganic & medicinal chemistry

authors： Ram VJ,Farhanullah,Tripathi BK,Srivastava AK

更新日期：2003-05-29 00:00:00

abstract：:We have surveyed the utility of Beckmann rearrangement for the conversion of indanones into carbostyrils. Initial attempts at the conversion of 6-methoxy indanone oxime under classical conditions resulted in the formation of the two unusual products: 2-sulfonyloxyindanone and the dimeric product. This unusual rearrang...

journal_title：Bioorganic & medicinal chemistry

authors： Torisawa Y,Nishi T,Minamikawa Ji

更新日期：2003-05-15 00:00:00

abstract：:1,4,7-Trisubstituted isoquinolines were designed, synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2. The 1-benzyloxyphenyl-dihydroisoquinoline and -isoquinoline derivatives were found to exhibit better activity against falcipain-2 than their corresponding 1-hydr...

journal_title：Bioorganic & medicinal chemistry

authors： Batra S,Sabnis YA,Rosenthal PJ,Avery MA

更新日期：2003-05-15 00:00:00

abstract：:To clarify the structure-activity relationships of flavonoids for nitric oxide (NO) production inhibitory activity, we examined the inhibitory effects of 73 flavonoids on NO production in lipopolysaccharide-activated mouse peritoneal macrophages. Among those flavonoids, apigenin (IC(50)=7.7 microM), diosmetin (8.9 mic...

journal_title：Bioorganic & medicinal chemistry

authors： Matsuda H,Morikawa T,Ando S,Toguchida I,Yoshikawa M

更新日期：2003-05-01 00:00:00

abstract：:Expanding the scope of substrate specificity and stereoselectivity is of current interest in enzyme catalysis. Using error-prone PCR for in vitro directed evolution, the Neu5Ac aldolase from Escherichia coli has been altered to improve its catalytic activity toward enantiomeric substrates including N-acetyl-L-mannosam...

journal_title：Bioorganic & medicinal chemistry

authors： Wada M,Hsu CC,Franke D,Mitchell M,Heine A,Wilson I,Wong CH

更新日期：2003-05-01 00:00:00

abstract：:Glucoconjugated tri and tetra(meta-hydroxyphenyl)chlorins have been synthesized in order to explore how glucoconjugation of the macrocycle affects the photoactivity of the molecule. Internalization processes, photosensitizing efficacy of TPC(m-O-GluOH)(3) and TPC(m-O-GluOH)(4), in HT29 human adenocarcinoma cells have ...

journal_title：Bioorganic & medicinal chemistry

authors： Laville I,Figueiredo T,Loock B,Pigaglio S,Maillard P,Grierson DS,Carrez D,Croisy A,Blais J

更新日期：2003-04-17 00:00:00

abstract：:Seven new nitrogen heterocycle porphyrins, 5,10,15,20-tetra[4-(N-pyrrolidinyl)phenyl]porphine (TBPPH(2)), 5,10,15,20-tetra[4-(4'-ethylpiperazinyl)phenyl]porphine (TEPPH(2)), 5,10,15,20-tetra [4-(4'-butylpiperazinyl)phenyl]porphine (TUPPH(2)), 5,10,15,20-tetra[4-(4'-heptylpiperazinyl) phenyl]porphine (THPPH(2)), 5-[4-(...

journal_title：Bioorganic & medicinal chemistry

authors： Guo CC,Li HP,Zhang XB

更新日期：2003-04-17 00:00:00

abstract：:Protein tyrosine phosphatases (PTPs) are important in the regulation of signal transduction processes. Certain enzymes of this class are considered as potential therapeutic targets in the treatment of a variety of diseases such as diabetes, inflammation, and cancer. However, many PTP inhibitors identified to date are ...

journal_title：Bioorganic & medicinal chemistry

authors： Huang P,Ramphal J,Wei J,Liang C,Jallal B,McMahon G,Tang C

更新日期：2003-04-17 00:00:00

abstract：:Arylamine N-acetyltransferases (NATs) catalyse the acetylation of arylamine, arylhydrazine and arylhydroxylamine substrates by acetyl Coenzyme A. NAT has been discovered in a wide range of eukaryotic and prokaryotic species. Although prokaryotic NATs have been implicated in xenobiotic metabolism, to date no endogenous...

journal_title：Bioorganic & medicinal chemistry

authors： Brooke EW,Davies SG,Mulvaney AW,Pompeo F,Sim E,Vickers RJ

更新日期：2003-04-03 00:00:00

abstract：:N-terminal-blocked and N-terminal-free pseudotripeptide Gly-Gly and Gly-Pro derivatives of 5-aminolevulinic acid (ALA) esters were synthesized as potential specific substrates for cellular peptidases and precursors for the production of the photosensitizer protoporphyrin IX (PpIX). These precursors were evaluated usin...

journal_title：Bioorganic & medicinal chemistry

authors： Berger Y,Ingrassia L,Neier R,Juillerat-Jeanneret L

更新日期：2003-04-03 00:00:00

abstract：:A series of anilides and phenyl esters of piperidine-3-carboxylic acid (nipecotic acid) were synthesized and tested for the ability to inhibit aggregation of human platelet rich-plasma triggered by adenosine 5'-diphosphate (ADP) and adrenaline. As a rule, amides were about two times more active than the corresponding ...

journal_title：Bioorganic & medicinal chemistry

authors： de Candia M,Summo L,Carrieri A,Altomare C,Nardecchia A,Cellamare S,Carotti A

更新日期：2003-04-03 00:00:00

abstract：:Glucuronide derivatives of CBI-bearing CC-1065 analogues have been synthesized, and their cytotoxicities tested against U937 leukemia cells. The new compounds show potent antitumor activity in vitro. Compounds 1 and 2, and their corresponding glucuronides 3 and 4 have IC(50) values of 0.6, 0.1, 1.4 and 0.6 nM, respect...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Y,Yuan H,Wright SC,Wang H,Larrick JW

更新日期：2003-04-03 00:00:00

abstract：:The Maillard reaction is a complex network of reactions that has been shown to result in the non-enzymatic crosslinking of proteins. Recent attention has focussed on the role of alpha-dicarbonyl compounds as important in vivo contributors to protein crosslinking but, despite extensive research, the molecular mechanism...

journal_title：Bioorganic & medicinal chemistry

authors： Meade SJ,Miller AG,Gerrard JA

更新日期：2003-03-20 00:00:00

abstract：:Thymidylate synthase (TS) (EC 2.1.1.45), an enzyme involved in the DNA synthesis of both prokaryotic and eukaryotic cells, is a potential target for the development of anticancer and antinfective agents. Recently, we described a series of phthalein and naphthalein derivatives as TS inhibitors. These compounds have str...

journal_title：Bioorganic & medicinal chemistry

authors： Ghelli S,Rinaldi M,Barlocco D,Gelain A,Pecorari P,Tondi D,Rastelli G,Costi MP

更新日期：2003-03-20 00:00:00

abstract：:A new asymmetric cyanine dye has been synthesised and its interaction with different DNA has been investigated. In this dye, BEBO, the structure of the known intercalating cyanine dye BO has been extended with a benzothiazole substituent. The resulting crescent-shape of the molecule is similar to that of the well-know...

journal_title：Bioorganic & medicinal chemistry

authors： Karlsson HJ,Lincoln P,Westman G

更新日期：2003-03-20 00:00:00

abstract：:There is considerable interest in developing dopamine transporter (DAT) inhibitors as potential therapies for the treatment of cocaine abuse. We report herein our pharmacophore-based discovery and molecular modeling-assisted rational design of 2,3-disubstituted quinuclidines as potent DAT inhibitors with a novel chemi...

journal_title：Bioorganic & medicinal chemistry

authors： Sakamuri S,Enyedy IJ,Zaman WA,Tella SR,Kozikowski AP,Flippen-Anderson JL,Farkas T,Johnson KM,Wang S

更新日期：2003-03-20 00:00:00

abstract：:The methanolic extract of the roots of Saussurea lappa CLARKE, a Chinese medicinal herb Saussureae Radix, was found to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-activated mouse peritoneal macrophages. Among the constituents from the methanolic extract, two sesquiterpene lactones (costunolide and...

journal_title：Bioorganic & medicinal chemistry

authors： Matsuda H,Toguchida I,Ninomiya K,Kageura T,Morikawa T,Yoshikawa M

更新日期：2003-03-06 00:00:00

abstract：:Amido derivatives 10-18 of the corresponding oxyamines were synthesised as melatoninergic ligands by the reaction of hydroxyphtalimide with the halogeno derivatives or the corresponding alcohols using Mitsunobu reaction conditions. The affinity of the compounds for chicken brain melatonin receptors and recombinant hum...

journal_title：Bioorganic & medicinal chemistry

authors： Pégurier C,Morellato L,Chahed E,Andrieux J,Nicolas JP,Boutin JA,Bennejean C,Delagrange P,Langlois M,Mathé-Allainmat M

更新日期：2003-03-06 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：:Structure-activity relationships of 2-phenyl-imidazo[2,1-i]purin-5-ones as ligands for human A(3) adenosine receptors (ARs) were investigated. An ethyl group in the 8-position of the imidazoline ring of 4-methyl-2-phenyl-imidazopurinone leading to chiral compounds was found to increase affinity for human A(3) ARs by s...

journal_title：Bioorganic & medicinal chemistry

authors： Ozola V,Thorand M,Diekmann M,Qurishi R,Schumacher B,Jacobson KA,Müller CE

更新日期：2003-02-06 00:00:00

abstract：:Thiol- or acid-promoted additions of silyl radicals to camptothecin are reported. At 105 degrees C, mixtures of 7-silyl (favored) and 12-silyl camptothecins are formed alongside substantial amounts of recovered camptothecin. At 160 degrees C, 12-silyl isomers are formed preferentially, but the total mass balance is su...

journal_title：Bioorganic & medicinal chemistry

authors： Du W,Kaskar B,Blumbergs P,Subramanian PK,Curran DP

更新日期：2003-02-06 00:00:00

abstract：:Seven new taxanes were isolated from the needles of the Canadian yew: unusual functional groups, positions and/or stereochemical features are described. Their chemical structures were rigorously characterized by detailed high resolution NMR analyses and confirmed by high resolution Fast Atom Bombardment Mass Spectrome...

journal_title：Bioorganic & medicinal chemistry

authors： Shi QW,Sauriol F,Mamer O,Zamir LO

更新日期：2003-01-17 00:00:00

abstract：:Forty-five novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds contain novel cinnamic acid moieties at C-7 that were synthesized using a key Heck reaction followed by nucleophilic aromatic substitution reactions. The most active compound...

journal_title：Bioorganic & medicinal chemistry

authors： Springer DM,Luh BY,Goodrich J,Bronson JJ

更新日期：2003-01-17 00:00:00

abstract：:We have recently reported the discovery of numerous new compounds that are selective inhibitors of all of the subtypes of the adenosine receptor family via a pharmacophore database searching and screening strategy. During the course of this work we made the unexpected discovery of a potent A(2B) receptor antagonist, 4...

journal_title：Bioorganic & medicinal chemistry

authors： Webb TR,Lvovskiy D,Kim SA,Ji Xd,Melman N,Linden J,Jacobson KA

更新日期：2003-01-02 00:00:00

abstract：:Human urotensin II (hU-II; H-Glu-Thr-Pro-Asp-cyclo[Cys-Phe-Trp-Lys-Tyr-Cys]-Val-OH) is a disulfide bridged undecapeptide recently identified as the ligand of an orphan G protein-coupled receptor. hU-II has been described as the most potent vasoconstrictor compound identified to date. With the aim of replacing the disu...

journal_title：Bioorganic & medicinal chemistry

authors： Grieco P,Carotenuto A,Patacchini R,Maggi CA,Novellino E,Rovero P

更新日期：2002-12-01 00:00:00

abstract：:4-Oxalocrotonate tautomerase (4-OT) catalyzes the isomerization of 4-oxalocrotonate, 1, to 2-oxo-3E-hexenedioate, 3, using a general acid/base mechanism that involves a conserved N-terminal proline residue. The P1A and P1G mutants have been shown to catalyze this isomerization but at reduced rates. Analysis of these m...

journal_title：Bioorganic & medicinal chemistry

authors： Brik A,Dawson PE,Keinan E

更新日期：2002-12-01 00:00:00

abstract：:Topological evidences for modelling lipophilicity of a large series of diversed compounds have been provided on the basis of distance-based topological indices. A pool of topological indices along with indicator parameters related to the type of the compounds present in the set of 140 compounds were used for this purp...

journal_title：Bioorganic & medicinal chemistry

authors： Agrawal VK,Singh J,Khadikar PV

更新日期：2002-12-01 00:00:00

abstract：:The activity-structure relationships (ASR) of phenolic compounds as hydroxyl-radical scavengers have mostly been studied and discussed with regard to their iron-chelating and hydrogen-donation properties in Fenton-type system, but extensive elucidation of multiple mechanisms underlying the hydroxyl radical scavenging ...

journal_title：Bioorganic & medicinal chemistry

authors： Cheng Z,Ren J,Li Y,Chang W,Chen Z

更新日期：2002-12-01 00:00:00

abstract：:Compounds from a wide variety of structural classes inhibit HIV-1 integrase. However, a single unified understanding of the relationship between the structures and activities of these compounds still eludes researchers. We report herein the development of QSAR models for integrase inhibition. The genetic function appr...

journal_title：Bioorganic & medicinal chemistry

authors： Yuan H,Parrill AL

更新日期：2002-12-01 00:00:00

abstract：:Various 4-analogues of podophyllotoxin and epipodophyllotoxin were obtained via the formation of the corresponding 4-keto derivatives. Methyloximation of podophyllotoxone, followed by subsequent catalytic hydrogenation, gave stereoselective access to 4-alpha-amino-4-deoxypodophyllotoxin and from there, to the correspo...

journal_title：Bioorganic & medicinal chemistry

authors： Roulland E,Magiatis P,Arimondo P,Bertounesque E,Monneret C

更新日期：2002-11-01 00:00:00

abstract：:The first published synthesis and characterization of a purine-scaffold library of hsp90 inhibitors is presented. The purine-scaffold represents a platform for the creation of easily synthesizable and derivatizable soluble molecules that are amenable for oral administration. The most active compound of the series (71)...

journal_title：Bioorganic & medicinal chemistry

authors： Chiosis G,Lucas B,Shtil A,Huezo H,Rosen N

更新日期：2002-11-01 00:00:00

abstract：:Serine peptidases are a large, well-studied, and medically important class of peptidases. Despite the attention these enzymes have received, details concerning the substrate specificity of even some of the best known enzymes in this class are lacking. One approach to rapidly characterizing substrate specificity for pe...

journal_title：Bioorganic & medicinal chemistry

authors： Furlong ST,Mauger RC,Strimpler AM,Liu YP,Morris FX,Edwards PD

更新日期：2002-11-01 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：:Biological assay guided fractionation of a dichloromethane extract of Synaptolepis kirkii led to the isolation of four new and five known daphnane-type diterpene orthoesters, whose structure was established by spectroscopic data. Full spectroscopic data of the new and known natural products are reported here for the f...

journal_title：Bioorganic & medicinal chemistry

authors： He W,Cik M,Van Puyvelde L,Van Dun J,Appendino G,Lesage A,Van der Lindin I,Leysen JE,Wouters W,Mathenge SG,Mudida FP,De Kimpe N

更新日期：2002-10-01 00:00:00

abstract：:We report the synthesis and biological activity of a series of side-chain-constrained RGD peptides containing the (2S,3R) or (2S,3S) beta-methyl aspartic acid within the RGD sequence. These compounds have been assayed for binding to the integrin receptors alpha(IIb)beta3 and alpha(v)beta3 and the results demonstrate t...

journal_title：Bioorganic & medicinal chemistry

authors： Schabbert S,Pierschbacher MD,Mattern RH,Goodman M

更新日期：2002-10-01 00:00:00

abstract：:The in vitro antitumor activities of 2,6-di-[2-(heteroaryl)vinyl]pyridines versus the standard National Cancer Institute 60 cell lines panel and of 2,6-di-[2-(heteroaryl)vinyl] pyridinium cations versus MCF7 (human mammary carcinoma) and LNCap (prostate carcinoma) cell lines are reported. Antiproliferative effects in ...

journal_title：Bioorganic & medicinal chemistry

authors： Barresi V,Condorelli DF,Fortuna CG,Musumarra G,Scirè S

更新日期：2002-09-01 00:00:00