abstract：:Modified guanosine monophosphates have been employed to introduce various functional groups onto RNA 5'-ends. Applications of modified RNA 5'-ends include the generation of functionalized RNA libraries for in vitro selection of catalytic RNAs, the attachment of photoaffinity-tags for mapping RNA-protein interactions o...

journal_title：Bioorganic & medicinal chemistry

authors： Sengle G,Jenne A,Arora PS,Seelig B,Nowick JS,Jäschke A,Famulok M

更新日期：2000-06-01 00:00:00

abstract：:A molecular modeling study using Comparative Molecular Field Analysis (CoMFA) was undertaken to develop a predictive model for combretastatin binding to the colchicine binding site of tubulin. Furthermore, we examined the potential contribution of lipophilicity (log P) and molecular dipole moment and were unable to co...

journal_title：Bioorganic & medicinal chemistry

authors： Brown ML,Rieger JM,Macdonald TL

更新日期：2000-06-01 00:00:00

abstract：:Several analogues of cirazoline (2), a selective alpha1-adrenoreceptor agonist, were prepared and their pharmacological profiles studied. Although at the alpha1-adrenoreceptor all the compounds displayed a significant agonist activity, at the alpha2-adrenoreceptor they showed either agonist or antagonist activity depe...

journal_title：Bioorganic & medicinal chemistry

authors： Pigini M,Quaglia W,Gentili F,Marucci G,Cantalamessa F,Franchini S,Sorbi C,Brasili L

更新日期：2000-05-01 00:00:00

abstract：:A set of oligo-1,3-thiazolecarboxamide derivatives able to interact with the minor groove of nucleic acids was synthesized. These oligopeptides contained different numbers of thiazole units presenting dimethylaminopropyl or EDTA moieties on the C-terminus, and aminohexanoyl or EDTA moieties on the N-terminus. The inhi...

journal_title：Bioorganic & medicinal chemistry

authors： Ryabinin VA,Zakharova OD,Yurchenko EY,Timofeeva OA,Martyanov IV,Tokarev AA,Belanov EF,Bormotov NI,Tarrago-Litvak L,Andreola ML,Litvak S,Nevinsky GA,Sinyakov AN

更新日期：2000-05-01 00:00:00

abstract：:Twenty-four hydrophobic dicarboxylic acids are described which were evaluated as inhibitors of 14 kDa human platelet phospholipase A2 (HP-PLA2). In general, biarylacetic acid derivatives were found to be more active than biaryl acids or biarylpropanoic acids. More potent inhibitors were obtained when hydrophobic group...

journal_title：Bioorganic & medicinal chemistry

authors： Springer DM,Luh BY,Bronson JJ,McElhone KE,Mansuri MM,Gregor KR,Nettleton DO,Stanley PL,Tramposch KM

更新日期：2000-05-01 00:00:00

abstract：:Various D-fructose analogues modified at C-1 or C-6 positions were synthesized from D-glucose by taking advantage of the Amadori rearrangement or using the aldol condensation between dihydroxyacetone phosphate and appropriate aldehyde catalyzed by fructose 1,6-diphosphate aldolase from rabbit muscle. The affinities of...

journal_title：Bioorganic & medicinal chemistry

authors： Azéma L,Bringaud F,Blonski C,Périé J

更新日期：2000-04-01 00:00:00

abstract：:(R)- and (S)-Hippuryl-alpha-methylphenylalanine [(R)- and (S)-Hipp-alpha-MePhe] and (S)-hippuryl-alpha-methylphenyllactic acid [(S)-Hipp-alpha-MeOPhe] were synthesized and evaluated as substrates for carboxypeptidase A (CPA) in an effort to shed further light on the catalytic mechanism of the enzyme. The rate of CPA-c...

journal_title：Bioorganic & medicinal chemistry

authors： Lee M,Kim DH

更新日期：2000-04-01 00:00:00

abstract：:Due to the capability of peptidyl derivatives of araC to behave as prodrugs of this antimetabolite, and because of the well known biological properties of peptide T and its analogues (in particular that of targeting CD4+ cells), new peptide T-araC conjugates were prepared and tested in vitro for antiproliferative acti...

journal_title：Bioorganic & medicinal chemistry

authors： Manfredini S,Marastoni-M,Tomatis R,Durini E,Spisani S,Pani A,Marceddu T,Musiu C,Marongiu ME,La Colla P

更新日期：2000-03-01 00:00:00

abstract：:A series of hydroxamates was prepared by reaction of alkyl/arylsulfonyl halides with N-2-chlorobenzyl-L-alanine, followed by conversion of the COOH moiety to the CONHOH group, with hydroxylamine in the presence of carbodiimides. Other structurally related compounds were obtained by reaction of N-2-chlorobenzyl-L-alani...

journal_title：Bioorganic & medicinal chemistry

authors： Scozzafava A,Supuran CT

更新日期：2000-03-01 00:00:00

abstract：:Novel benzimidazole derivatives were synthesized and their pharmacological activities were examined. These compounds showed a good suppressive action on histamine release from rat peritoneal mast cells produced by antigen-antibody reaction, an antagonistic action on guinea pig ileum contraction caused by histamine, an...

journal_title：Bioorganic & medicinal chemistry

authors： Nakano H,Inoue T,Kawasaki N,Miyataka H,Matsumoto H,Taguchi T,Inagaki N,Nagai H,Satoh T

更新日期：2000-02-01 00:00:00

abstract：:We have exhibited successful and rapid screening of DNA-binding peptide ligands from solid-phase library beads with the use of the target DNA-conjugated magnetic beads. The target duplex DNA (3) has a polyether linker between two complementary sequences (T4A3G-ether linker-CT3A4) and is stable in the duplex form durin...

journal_title：Bioorganic & medicinal chemistry

authors： Alam MR,Maeda M,Sasaki S

更新日期：2000-02-01 00:00:00

abstract：:Avermectin B1a (1) is a potent anthelmintic, insecticide, miticide and chloride channel activator on interaction with a specific nerve membrane site analyzed by binding assays with [3H]1. Candidate photoaffinity probes were prepared replacing the dioleandrosyl substituent with potential isosteric esters and ethers app...

journal_title：Bioorganic & medicinal chemistry

authors： Tsukamoto Y,Cole LM,Casida JE

更新日期：2000-01-01 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 DNA helix destabilizing activity of a series of cyclobisintercaland compounds (CBIs) has been evaluated by measuring their ability to displace a 32P-labelled oligonucleotide primer (17-mer) hybridized to the single stranded DNA of M13. This destabilizing activity appears to be strongly dependent on the cyclic stru...

journal_title：Bioorganic & medicinal chemistry

authors： Teulade-Fichou MP,Fauquet M,Baudoin O,Vigneron JP,Lehn JM

更新日期：2000-01-01 00:00:00

abstract：:The synthesis of a new minimum steric perturbing proxyl nitroxide, which is a derivative of glycerol and contains a stearic acid moiety, has been carried out. Its localization in model membrane L-alpha-dipalmitoyl phosphatidyl choline (DPPC) was ascertained with the help of ESR, DSC, 1H and 31P NMR techniques. The nit...

journal_title：Bioorganic & medicinal chemistry

authors： Katoch R,Trivedi GK,Phadke RS

更新日期：1999-12-01 00:00:00

abstract：:The molecular structure of 2alpha-hydroxyneoanisatin, a positional isomer of the potent neurotoxin anisatin, was determined by X-ray crystallographic analysis. This compound and four further seco-prezizaane type sesquiterpene lactones previously isolated from Illicium floridanum, which represent different structural t...

journal_title：Bioorganic & medicinal chemistry

authors： Schmidt TJ,Okuyama E,Fronczek FR

更新日期：1999-12-01 00:00:00

abstract：:Naphthalene melatoninergic ligands with alkyl groups (Me, Et, Pr, Bz) in the beta position of the ethylamido chain were synthesised. The affinity of the compounds for chicken brain melatonin receptors was evaluated using 2-[125I]-iodomelatonin as the radioligand. An increase in the affinity was observed with the beta-...

journal_title：Bioorganic & medicinal chemistry

authors： Mathé-Allainmat M,Le Gall M,Jellimann C,Andrieux J,Langlois M

更新日期：1999-12-01 00:00:00

abstract：:The use of methanethiosulfonates as thiol-specific modifying reagents in the strategy of combined site-directed mutagenesis and chemical modification allows virtually unlimited opportunities for creating new protein surface environments. As a consequence of our interest in electrostatic manipulation as a means of tail...

journal_title：Bioorganic & medicinal chemistry

authors： Davis BG,Khumtaveeporn K,Bott RR,Jones JB

更新日期：1999-11-01 00:00:00

abstract：:The biochemically unique structures of sugar residues in the outer cell wall of Mycobacterium tuberculosis (MTB) make the pathways for their biosynthesis and utilization attractive targets for the development of new and selective anti-tubercular agents. A cell-free assay system for galactosyltransferase activity using...

journal_title：Bioorganic & medicinal chemistry

authors： Pathak AK,Besra GS,Crick D,Maddry JA,Morehouse CB,Suling WJ,Reynolds RC

更新日期：1999-11-01 00:00:00

abstract：:By the introduction of various amide surrogates, novel pseudopeptides corresponding to a membrane active depsipeptide were synthesized and their native characteristics compared with that of the peptide. The pseudopeptides had more resistance to serum proteases than the peptide and similar antimicrobial activities to t...

journal_title：Bioorganic & medicinal chemistry

authors： Oh JE,Hong SY,Lee KH

更新日期：1999-11-01 00:00:00

abstract：:Protozoan parasites are unable to synthesize purines de novo and must rely on purine salvage pathways for their requirements. Nucleoside hydrolases, which are not found in mammals, function as key enzymes in purine salvage in protozoa. Inhibition of these enzymes may disrupt purine supply and specific inhibitors are p...

journal_title：Bioorganic & medicinal chemistry

authors： Furneaux RH,Schramm VL,Tyler PC

更新日期：1999-11-01 00:00:00

abstract：:Combinatorial biocatalysis, based on a principle of the combinatorial use of biosynthetic steps rather than the combinatorial use of reagents, offers a complementary approach to combinatorial chemistry, which, used individually or in connection with synthetic organic transformations, provides access to analogues not r...

journal_title：Bioorganic & medicinal chemistry

authors： Krstenansky JL,Khmelnitsky Y

更新日期：1999-10-01 00:00:00

abstract：:The beta-amino acid, (S)-ethyl-3-amino-4-pentynoate, is a chiral synthon used in the synthesis of xemilofiban hydrochloride, an anti-platelet agent. A biocatalytic approach was developed to resolve (R)- and (S)-enantiomers of ethyl 3-amino-4-pentynoate in enantiomerically pure form employing the enzyme Penicillin acyl...

journal_title：Bioorganic & medicinal chemistry

authors： Topgi RS,Ng JS,Landis B,Wang P,Behling JR

更新日期：1999-10-01 00:00:00

abstract：:To assist in the development of technetium-based radiopharmaceuticals that are useful for the diagnostic imaging of steroid receptor-positive breast tumors, we have synthesized a series of small-sized metal chelates according to 'n + 1' mixed-ligand, thioether-carbonyl and organometallic designs. In these preliminary ...

journal_title：Bioorganic & medicinal chemistry

authors： Wüst F,Skaddan MB,Leibnitz P,Spies H,Katzenellenbogen JA,Johannsen B

更新日期：1999-09-01 00:00:00

abstract：:3- And 4-imidazol-1-yl-methyl substituted biphenyl compounds (named as meta- and para-substituted compounds) were synthesized bearing additional substituents in 3'-/4'-position as inhibitors of P450 17 (17alpha-hydroxylase-C17,20-lyase). P450 17 is the key enzyme of androgen biosynthesis. Its inhibition is a novel the...

journal_title：Bioorganic & medicinal chemistry

authors： Wachall BG,Hector M,Zhuang Y,Hartmann RW

更新日期：1999-09-01 00:00:00

abstract：:A number of 5-aminosubstituted 20(S)-camptothecin analogues were prepared via semi-synthesis starting from 20(S)-camptothecin and 9-methoxy 20(S)-camptothecin. In vitro anti-cancer activity of these analogues was determined using 60 human tumor cell line assay. Although water solubility of most of these compounds was ...

journal_title：Bioorganic & medicinal chemistry

authors： Subrahmanyam D,Sarma VM,Venkateswarlu A,Sastry TV,Kulakarni AP,Rao DS,Reddy KV

更新日期：1999-09-01 00:00:00

abstract：:Synthesis and antitumor activity of goniofufurone analogues 15, 16, 17, 33, and 46 is reported. Key step in the synthesis is Pd (II) mediated oxidative cyclisation of vinyl-(hydroxy) furans 18, 19 to the corresponding lactols 32, 43. Cytotoxicities of 15, 16, 17, 33, and 46 tested against six human cancer cell lines a...

journal_title：Bioorganic & medicinal chemistry

authors： Mereyala HB,Gadikota RR,Joe M,Arora SK,Dastidar SG,Agarwal S

更新日期：1999-09-01 00:00:00

abstract：:The enzyme 17alpha-hydroxylase/17,20-lyase (P-450(17alpha) has recently become the focus of research into the fight against hormone dependent prostate cancer. However, the specific nature of this enzyme, in particular, the dual role of its active site, remains unknown. In our drive to elucidate further information reg...

journal_title：Bioorganic & medicinal chemistry

authors： Ahmed S

更新日期：1999-08-01 00:00:00

abstract：:Gabaculine (5-amino-1,3-cyclohexadienylcarboxylic acid, 1), a naturally occurring neurotoxin isolated from Streptomyces toyocaenis, has been shown to be a mechanism-based inactivator of gamma-aminobutyric acid aminotransferase (GABA-AT) (Rando, R. R. Biochemistry 1977, 16, 4604). Inactivation results from reaction of ...

journal_title：Bioorganic & medicinal chemistry

authors： Fu M,Silverman RB

更新日期：1999-08-01 00:00:00

abstract：:Experimental and theoretical physico-chemical methods were used to investigate the interaction between several reversible monoamine oxidase A inhibitors in the oxazolidinone series and the active site of the enzyme. Phenyloxazolidinones include toloxatone and analogues, among which befloxatone was selected as drug can...

journal_title：Bioorganic & medicinal chemistry

authors： Wouters J,Moureau F,Evrard G,Koenig JJ,Jegham S,George P,Durant F

更新日期：1999-08-01 00:00:00

abstract：:Aminoglycoside antibiotics have recently emerged as an intriguing family of RNA binding molecules and they became leading structures for the design of novel RNA ligands. The demystification of the aminoglycoside-RNA recognition phenomenon is required for the development of superior binders. To explore the existence of...

journal_title：Bioorganic & medicinal chemistry

authors： Michael K,Wang H,Tor Y

更新日期：1999-07-01 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

abstract：:2- and 3-Methyl-4,8-dihydrobenzo[1,2-b:5,4-b']dithiophene-4,8-dione and related derivatives were synthesized and evaluated in vitro by NCI against eight cancer types. Compounds 12-15 showed significant activity against melanoma, NCI-H23 non-small cell lung cancer, and MDA-MB-435 and MDA-N breast cancer cell lines; 2-h...

journal_title：Bioorganic & medicinal chemistry

authors： Chao YH,Kuo SC,Ku K,Chiu IP,Wu CH,Mauger A,Wang HK,Lee KH

更新日期：1999-06-01 00:00:00

abstract：:Beta-carboline-benzoquinolizidine plant alkaloid deoxytubulosine (DTB) was evaluated and assessed for the first time for its biochemical and biological activity employing the biomarker dihydrofolate reductase (DHFR) (5,6,7,8-tetrahydrofolate: NADP+ oxidoreductase, EC 1.5.1.3) as the probe enzyme, a key target in cance...

journal_title：Bioorganic & medicinal chemistry

authors： Rao KN,Venkatachalam SR

更新日期：1999-06-01 00:00:00

abstract：:We report the synthesis of several highly functionalized biotinylated philanthotoxin (PhTX) analogues (7, 8, 10, 13-16) designed on the basis of earlier structure-activity relationship studies. Despite the extensive modifications, the binding to nicotinic acetylcholine receptor (nAChR) is in the low micromolar range a...

journal_title：Bioorganic & medicinal chemistry

authors： Hashimoto M,Liu Y,Fang K,Li HY,Campiani G,Nakanishi K

更新日期：1999-06-01 00:00:00

abstract：:The objective of this brief review is to present an overview of the bioorganic chemistry of cyclic-ADP-ribose (cADPR) with special emphasis on the methodology used for the synthesis of analogues of cADPR. New structural analogues of cADPR can be prepared using either the biomimetic method or ADP-ribosyl cyclase from A...

journal_title：Bioorganic & medicinal chemistry

authors： Zhang FJ,Gu QM,Sih CJ

更新日期：1999-05-01 00:00:00

abstract：:Several aryl substituted C-fucopeptides have been developed as sialyl Lewis X mimetics. Although the compounds have a much simpler structure compared to SLe(x), up to 3-times higher binding affinity toward E-selectin and > 1000 times toward P-selectin was observed. Furthermore, a convenient strategy for generating a n...

journal_title：Bioorganic & medicinal chemistry

authors： Huwe CM,Woltering TJ,Jiricek J,Weitz-Schmidt G,Wong CH

更新日期：1999-05-01 00:00:00

abstract：:In order to determine the function of epinephrine (Epi) in the central nervous system, we have targeted the enzyme that catalyzes the final step in the biosynthesis of Epi, phenylethanolamine N-methyltransferase (PNMT; EC 2.1.1.28). 1,2,3,4-Tetrahydroisoquinolines (THIQs) are inhibitors of this enzyme, but also displa...

journal_title：Bioorganic & medicinal chemistry

authors： Grunewald GL,Caldwell TM,Li Q,Criscione KR

更新日期：1999-05-01 00:00:00

abstract：:Hepatitis A virus (HAV) 3C proteinase is a picornaviral cysteine proteinase that is essential for cleavage of the initially synthesized viral polyprotein precursor to mature fragments and is therefore required for viral replication in vivo. Since the enzyme generally recognizes peptide substrates with L-glutamine at t...

journal_title：Bioorganic & medicinal chemistry

authors： Huang Y,Malcolm BA,Vederas JC

更新日期：1999-04-01 00:00:00

abstract：:Oligosaccharyltransferase (OST) catalyzes the transfer of a branched oligosaccharide from a dolichylpyrophosphate oligosaccharide (Dol-PP-OS) to the asparagine of a nascent polypeptide chain in vivo and peptide substrates in vitro. Here we report the isolation and purification of Dol-PP-OS from bovine pancreas and thy...

journal_title：Bioorganic & medicinal chemistry

authors： Gibbs BS,Coward JK

更新日期：1999-03-01 00:00:00