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：:The synthesis and SAR of a novel series of non-nucleoside pyridopyrimidine inhibitors of the enzyme adenosine kinase (AK) are described. It was found that pyridopyrimidines with a broad range of medium and large non-polar substituents at the 5-position potently inhibited AK activity. A narrower range of analogues was ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cowart M,Lee CH,Gfesser GA,Bayburt EK,Bhagwat SS,Stewart AO,Yu H,Kohlhaas KL,McGaraughty S,Wismer CT,Mikusa J,Zhu C,Alexander KM,Jarvis MF,Kowaluk EA

更新日期：2001-01-08 00:00:00

abstract：:The application of a novel solid-phase synthesis of 2,3-disubstituted indoles utilizing a carbamate indole linker is described resulting in the identification of the novel, high-affinity, selective h5-HT2A antagonist 19. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Smith AL,Stevenson GI,Lewis S,Patel S,Castro JL

更新日期：2000-12-18 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：:New derivatives of L-thiocitrulline were prepared and assayed as inhibitors of the three isoforms of nitric oxide synthase. These compounds demonstrated weak inhibitory activity against the NOS isoforms and these results directly support a recently described model of the L-arginine binding site of NOS. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ware RW Jr,King SB

更新日期：2000-12-18 00:00:00

abstract：:The synthesis and in vitro Class III antiarrhythmic activity of several 4-aroyl (and aryl)-1-aralkylpiperazine and piperidine derivatives are described. Among several potent compounds identified in the series, RWJ-28810 (3), with its EC20 of 3 nM, ranks as one of the most potent (in vitro) compounds reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kanojia RM,Salata JJ,Kauffman J

更新日期：2000-12-18 00:00:00

abstract：:Several benzocyclobutacarbazol derivatives were synthesized and evaluated for their potential cytotoxic properties. A number of these compounds exhibited significant antiproliferative activity with concomitant interaction with the cell cycle and represent a new class of potential anticancer agents. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Graf-Christophe S,Kuehm-Caubère C,Renard P,Pfeiffer B,Pierré A,Léonce S,Caubère P

更新日期：2000-12-04 00:00:00

abstract：:A polyphemusin peptide analogue, T22 ([Tyr(5,12), Lys7]-polyphemusin II), and its shortened potent analogues, T134 (des-[Cys(8,13), Tyr(9,12)]-[D-Lys10, Pro11, L-citrulline16]-T22 without C-terminal amide) and T140 [[L-3-(2-naphthyl)alanine3]-T134], strongly inhibit the T-cell line-tropic (T-tropic) HIV-1 infection th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tamamura H,Omagari A,Oishi S,Kanamoto T,Yamamoto N,Peiper SC,Nakashima H,Otaka A,Fujii N

更新日期：2000-12-04 00:00:00

abstract：:A new family of bioactive bromotyrosine derivatives, termed mololipids, was recently isolated from a Hawaiian sponge, but could not be resolved into individual components by chromatography. To complete their structural characterization and better understand structure-activity relationships, the first pure samples of d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Schoenfeld RC,Lumb JP,Fantini J,Ganem B

更新日期：2000-12-04 00:00:00

abstract：:4-Deacetoxyagosterol A was synthesized from ergosterol by utilizing reductive regioselective epoxy cleavage as a key reaction. This synthesized congener of agosterol A, a spongean MDR-modulator. showed similar MDR-modulating activity against KB CV-60 cells overexpressing MRP. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Murakami N,Sugimoto M,Morita M,Akiyama S,Kobayashi M

更新日期：2000-11-20 00:00:00

abstract：:A new cytotoxic oxysterol, 16beta-hydroxy-5alpha-cholestane-3,6-dione was isolated from the red alga Jania rubens. Its structure was established by spectroscopic method. The ID50 value was 0.5 microg/mL. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ktari L,Blond A,Guyot M

更新日期：2000-11-20 00:00:00

abstract：:The stereoselective synthesis and biological activity of NPS 1407 (4a), (S)-(-)-3-amino-1,1-bis(3-fluorophenyl)butane, a potent, stereoselective antagonist of the NMDA receptor, are described. The racemate (4) was found to be active at the NMDA receptor in an in vitro assay, prompting the synthesis of the individual s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Moe ST,Smith DL,DelMar EG,Shimizu SM,Van Wagenen BC,Balandrin MF,Chien YE,Raszkiewicz JL,Artman LD,White HS,Mueller AL

更新日期：2000-11-06 00:00:00

abstract：:A series of 1-adamantanecarboxamides was synthesized and examined for their potency as a selective 5-HT2 receptor antagonist. We found (S)-N-[1-[2-(4-fluorophenyl)ethyl]pyrrolidin-3-yl]-1-adamantane carboxamide hydrochloride hydrate (10-(S), Y-39241) to have a high affinity and selectivity for 5-HT2 receptors, and thi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujio M,Kuroita T,Sakai Y,Nakagawa H,Matsumoto Y

更新日期：2000-11-06 00:00:00

abstract：:Identification of a number of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes is described. In the rat microdialysis assay, this series of compounds showed pronounced enhancement of brain acetylcholine release after oral administration. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Y,Chackalamannil S,Hu Z,Clader JW,Greenlee W,Billard W,Binch H,Crosby G,Ruperto V,Duffy RA,McQuade R,Lachowicz JE

更新日期：2000-10-16 00:00:00

abstract：:A short route to pyrimidine locked nucleosides has been developed for their incorporation in triplex forming oligonucleotides (TFO). Compared to oligonucleotides built with standard nucleosides, the modified TFOs containing 3'-endo blocked residues formed, with their corresponding DNA duplexes, more stable triple heli...

journal_title：Bioorganic & medicinal chemistry letters

authors： Savy P,Benhida R,Fourrey JL,Maurisse R,Sun JS

更新日期：2000-10-16 00:00:00

abstract：:A series of 5-[(3,5-bis(trifluoromethyl)phenyl)methoxy]-3-(3,4-dichlorophenyl)-4(Z)- (methoxyimino)pentyl-1-piperazines was prepared and their affinity for the NK1 and NK2 receptors investigated. Compounds 7f, 10o, 10r, and 10s were found to be our most potent inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ting PC,Lee JF,Anthes JC,Shih NY,Piwinski JJ

更新日期：2000-10-16 00:00:00

abstract：:Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Stark H,Ligneau X,Sadek B,Ganellin CR,Arrang JM,Schwartz JC,Schunack W

更新日期：2000-10-16 00:00:00

abstract：:Novel and artificial anthraquinone-carbohydrate hybrids were designed and synthesized, and found to effectively cleave DNA under irradiation with a long wavelength UV light and also exhibit cytotoxicity against HeLa S3 cells. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Toshima K,Maeda Y,Ouchi H,Asai A,Matsumura S

更新日期：2000-10-02 00:00:00

abstract：:New analogues of the venerable antimalarial drug primaquine have been synthesized and bioassayed in vivo against Pneumocystis carinii, a life-threatening infection common among immunosuppressed patients. Two of these new compounds are significantly more active than primaquine itself, and provide new information for fu...

journal_title：Bioorganic & medicinal chemistry letters

authors： Goodwin TE,Boylan CJ,Current WL,Byrd JC,Edwards CB,Fuller DA,Green JL,Larocca CD,Raney KD,Ross AS,Tucker WA

更新日期：2000-10-02 00:00:00

abstract：:A series of 4beta-arylamino-4'-O-demethylepipodophyllotoxins and 4beta-arylaminoepipodophyllotoxins have been synthesized with significant stereoselectivity and improved yields by employing the methanesulphonic acid/sodium iodide reagent system. Compounds NPF. W-68 and other DNA topoisomerase II inhibitors are prepare...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamal A,Laxman N,Ramesh G

更新日期：2000-09-18 00:00:00

abstract：:We have described herein the syntheses of three novel series of aromatic ring containing pseudomycin side-chain analogues. Preliminary biological evaluations of these analogues clearly indicate that it is possible to synthesize rigid pseudomycin side-chain analogues without compromising in vitro antifungal activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jamison J,Levy S,Sun X,Zeckner D,Current W,Zweifel M,Rodriguez M,Turner W,Chen SH

更新日期：2000-09-18 00:00:00

abstract：:Novel L- and D-configuration dioxolane 5-azacytosine and 6-azathymine nucleosides have been synthesized and evaluated for biological activity. (-)-(2S,4S)-1-[2-(Hydroxymethyl)-1,3-dioxolan-4-yl]-5-azacytosine (6) showed significant activity against HBV, whereas the D-configuration analogue (14) has been found to exhib...

journal_title：Bioorganic & medicinal chemistry letters

authors： Luo MZ,Liu MC,Mozdziesz DE,Lin TS,Dutschman GE,Gullen EA,Cheng YC,Sartorelli AC

更新日期：2000-09-18 00:00:00

abstract：:Cocaine binds into beta-cyclodextrin, but not detectably into alpha- or gamma-cyclodextrin, in water solution. NMR studies indicate the geometry of the complex, which is confirmed by molecular mechanics calculations and binding studies on cocaine analogues and cyclodextrin dimers. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nesna N,Lou J,Breslow R

更新日期：2000-09-04 00:00:00

abstract：:A series of substituted 2-aminopyridines was prepared and evaluated as inhibitors of human nitric oxide synthases (NOS). 4,6-Disubstitution enhanced both potency and specificity for the inducible NOS with the most potent compound having an IC50 of 28 nM. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hagmann WK,Caldwell CG,Chen P,Durette PL,Esser CK,Lanza TJ,Kopka IE,Guthikonda R,Shah SK,MacCoss M,Chabin RM,Fletcher D,Grant SK,Green BG,Humes JL,Kelly TM,Luell S,Meurer R,Moore V,Pacholok SG,Pavia T,Williams H

更新日期：2000-09-04 00:00:00

abstract：:The effect of 2,3 modifications on the antibacterial activity of ketolides was evaluated by introducing substituents in position 2 and converting the C-1, C-2, C-3 beta-keto-ester into stable 2,3 enol-ether or 2,3 anhydro derivatives. Introduction of a fluorine in C-2 is beneficial with regard to the overall antibacte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Denis A,Bretin F,Fromentin C,Bonnet A,Piltan G,Bonnefoy A,Agouridas C

更新日期：2000-09-04 00:00:00

abstract：:A new method for the synthesis of 2'-O-methyl-2-thiouridine (s2Um) found in thermophilic bacterial tRNA was developed. Structural properties of s2Um and s2Um(p)U were studied by using 1H NMR spectroscopy. A modified nonaribonucleotide (RNA*: 5'-CGUUs2UmUUGC-3') was synthesized to study the base-recognition ability of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shohda K,Okamoto I,Wada T,Seio K,Sekine M

更新日期：2000-08-21 00:00:00

abstract：:A new glucuronylated prodrug of nornitrogen mustard, incorporating the same spacer group as the doxorubicin prodrug HMR 1826, has been prepared. Upon exposure to E. coli beta-glucuronidase, fast hydrolysis occurs but a lower cytotoxicity against LoVo cancer cells is observed compared to the nornitrogen mustard alone. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Papot S,Combaud D,Bosslet K,Gerken M,Czech J,Gesson JP

更新日期：2000-08-21 00:00:00

abstract：:Caffeoylglucosides, which have a glucose ring as a central linker, were synthesized from methyl D-glucosides, and their anti-HIV-1 activities were tested. Among them, four dicaffeoylglucosides (IC50 = 29.1+/-35.1 microM), 6a, 6b, 9b and 10b, showed HIV-1 integrase inhibitory activity as potent as L-chicoric acid. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim SN,Lee JY,Kim HJ,Shin CG,Park H,Lee YS

更新日期：2000-08-21 00:00:00

abstract：:A series of alpha1a receptor antagonists derived from a 4-aryl-3,4-dihydropyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to picomolar range along with high selectivity was obtained. In vivo efficacy in a prostate contraction model in rats was observed with a few derivatives. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nantermet PG,Barrow JC,Selnick HG,Homnick CF,Freidinger RM,Chang RS,O'Malley SS,Reiss DR,Broten TP,Ransom RW,Pettibone DJ,Olah T,Forray C

更新日期：2000-08-07 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：:Practical, asymmetric total syntheses of the title phospholipids from a readily available myo-inositol derivative as well as short chain and cross-linkable aminoether analogues are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Falck JR,Krishna UM,Capdevila JH

更新日期：2000-08-07 00:00:00

abstract：:A number of analogues of the recently described compound nematophin were prepared and studied for antibacterial activity. The 2-phenyl derivative was found to exhibit exceptional activity against methicillin resistant Staphylococcus aureus (MRSA) whereas the isosteric benzimidazole analogue was much less active. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kennedy G,Viziano M,Winders JA,Cavallini P,Gevi M,Micheli F,Rodegher P,Seneci P,Zumerle A

更新日期：2000-08-07 00:00:00

abstract：:The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chain aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega ...

journal_title：Bioorganic & medicinal chemistry letters

authors： deLong MA,Amburgey J,Taylor C,Wos JA,Soper DL,Wang Y,Hicks R

更新日期：2000-07-17 00:00:00

abstract：:6-Nitroquipazine has been known as one of the most potent and selective inhibitors of serotonin transporter in vitro and in vivo. Nine derivatives of 6-nitroquipazine were synthesized and tested for their potential abilities to displace [3H]citalopram binding to the rat cortical membranes. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee BS,Chu S,Lee BC,Chi DY,Choe YS,Jeong KJ,Jin C

更新日期：2000-07-17 00:00:00

abstract：:Analogues of BIBP 3226, (R)-N(alpha)-diphenylacetyl-N-(4-hydroxybenzyl)argininamide, were synthesized and investigated for Y1 antagonism (Ca2+-assay, HEL cells) and binding on Y1, Y2 and Y5 receptors. Replacing the benzylamino by a tetrahydrobenzazepinyl group preserves most of the Y1 activity. Combination with a N(G)...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aiglstorfer I,Hendrich I,Moser C,Bernhardt G,Dove S,Buschauer A

更新日期：2000-07-17 00:00:00

abstract：:The syntheses of 7-chloro-4-(substituted amino) quinolines (2-22) and their antifilarial activities are delineated. Some of the screened compounds have shown promising filarial response and sterilization effect on female Acanthocheilonema viteae in rodents. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tewari S,Chauhan PM,Bhaduri AP,Fatima N,Chatterjee RK

更新日期：2000-07-03 00:00:00

abstract：:A series of novel nikkomycin analogue inhibitors of the chitin synthase of fungal cell wall was synthesized and evaluated for their inhibitory activities. Among them, the compound having a phenanthrene group at the terminal amino acid was found to possess strong anti-chitin synthase activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Obi K,Uda J,Iwase K,Sugimoto O,Ebisu H,Matsuda A

更新日期：2000-07-03 00:00:00

abstract：:The synthesis of N-(O,O-diisopropylphosphoryl)-benzyltetrahydroisoquinoline (3) has been achieved in a 'one pot' procedure from imine (2) and diisopropyl-phosphorochloridate (1) generated in situ (POCl3 + iPrOH). Compound 3 is the first benzyltetrahydroisoquinoline derivative found to be a potent inhibitor of mitochon...

journal_title：Bioorganic & medicinal chemistry letters

authors： Andreu I,Cabedo N,Tormo JR,Bermejo A,Mello R,Cortes D

更新日期：2000-07-03 00:00:00

abstract：:Dimethylallyl (DMA) derivatives of a naturally occurring xanthone (decussatin 1) were prepared. Their activity as potential P-glycoprotein inhibitors was monitored by affinity of direct binding and compared to that of corresponding DMA-flavones. Both classes of compounds exhibited the same structure-activity relations...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tchamo DN,Dijoux-Franca MG,Mariotte AM,Tsamo E,Daskiewicz JB,Bayet C,Barron D,Conseil G,Di Pietro A

更新日期：2000-06-19 00:00:00

abstract：:The synthesis and in vitro chemical and enzymatic stability of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine (9) as L-Dopa prodrug are described. Prodrug 9 possesses a good lipophilicity (log P = 2.153 +/- 0.017), is stable in aqueous buffer solutions (pH 1.3 and 7.4), and in 80% rat and human plasma it...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cingolani GM,Di Stefano A,Mosciatti B,Napolitani F,Giorgioni G,Ricciutelli M,Claudi F

更新日期：2000-06-19 00:00:00