1-Benzazepin-2-one calcium channel blockers--VI. Receptor-binding model and possible relationship to desmethoxyverapamil.

abstract：:A series of (2E,2'E)-1,1'-(3-hydroxy-5-methylbiphenyl-2,6-diyl)-bis(3-pheylprop-2-ene-1-ones (5-33) were prepared by the reaction of 1,3-diacetyl biphenyls (1-4) with different aldehydes in presence of catalytic amount of solid KOH in ethanol in excellent yields. The compounds were evaluated for anticancer activity ag...

journal_title：Bioorganic & medicinal chemistry

authors： Sharma A,Chakravarti B,Gupt MP,Siddiqui JA,Konwar R,Tripathi RP

更新日期：2010-07-01 00:00:00

abstract：:A labeling probe containing a pyrenecarboxamide-tethered modified DNA base, (Py)U, has been developed for fluorometric detection of RNA poly(A) tracts, in which the fluorescence emission intensity was controlled by the microstructural change around (Py)U caused by binding with the target RNA. ...

journal_title：Bioorganic & medicinal chemistry

authors： Tanaka K,Okamoto A

更新日期：2008-01-01 00:00:00

abstract：:The Thermotoga maritima aldolase gene has been cloned into a T7 expression vector and overexpressed in Escherichia coli. The preparation yields 470 UL(-1) of enzyme at a specific activity of 9.4 U mg(-1). During retroaldol cleavage of KDPG, the enzyme shows a k(cat) that decreases with decreasing temperature. A more t...

journal_title：Bioorganic & medicinal chemistry

authors： Griffiths JS,Wymer NJ,Njolito E,Niranjanakumari S,Fierke CA,Toone EJ

更新日期：2002-03-01 00:00:00

abstract：:Highly chemo- and regioselective de-esterification has been observed in the deacetylation of peracetylated enolic forms of polyphenolic benzyl phenyl ketones by lipase from porcine pancreas (PPL) suspended in tetrahydrofuran (THF). The enzyme selectively deacetylates the enolic acetoxy over the phenolic acetoxy group(...

journal_title：Bioorganic & medicinal chemistry

authors： Parmar VS,Pati HN,Azim A,Kumar R,Himanshu,Bisht KS,Prasad AK,Errington W

更新日期：1998-01-01 00:00:00

abstract：:5-Lipoxygenase (5-LO) and microsomal prostaglandin E₂ synthase (mPGES)-1 are key enzymes in the biosynthesis of leukotrienes and prostaglandin (PG)E₂, respectively, and are considered as valuable targets for the treatment of inflammatory diseases. Here, we present the identification of 2-mercaptohexanoic acid derivati...

journal_title：Bioorganic & medicinal chemistry

authors： Greiner C,Zettl H,Koeberle A,Pergola C,Northoff H,Schubert-Zsilavecz M,Werz O

更新日期：2011-06-01 00:00:00

abstract：:Paraoxonase1 (PON1) is a HDL bound enzyme and many of the anti-atherogenic properties of HDL are attributed to PON1. The enzyme precise mechanism of protective action and its endogenous substrate remain elusive. PON1 hydrolyzes organophosphates, arylesters and lactones, whereas the lactones activity is assumed as the ...

journal_title：Bioorganic & medicinal chemistry

authors： Tavori H,Khatib S,Aviram M,Vaya J

更新日期：2008-08-01 00:00:00

abstract：:The permeability of dipeptide derivatives containing tryptophans and indole derivatives through Caco-2 cells was used as an in vitro intestinal absorption model in order to clarify structural factors which influence their intestinal epithelial permeation and metabolism. Most peptide derivatives were hydrolysed not onl...

journal_title：Bioorganic & medicinal chemistry

authors： Ano R,Kimura Y,Urakami M,Shima M,Matsuno R,Ueno T,Akamatsu M

更新日期：2004-01-02 00:00:00

abstract：:To investigate the effect of elongating base-pair (bp) recognition sequences, we synthesized N-methylpyrrole-N-methylimidazole (PI) polyamide conjugates with eight-bp recognition (3-5). The DNA alkylating activities of conjugates 3-5 were evaluated by high-resolution denaturing polyacrylamide gel electrophoresis with ...

journal_title：Bioorganic & medicinal chemistry

authors： Takagaki T,Bando T,Kitano M,Hashiya K,Kashiwazaki G,Sugiyama H

更新日期：2011-10-01 00:00:00

abstract：:The synthesis of 9-(β-d-1,3-dioxolan-4-yl)2,6-diaminopurine nucleoside phosphoramidate prodrugs as well as various 2-amino-6-carbamoylpurine dioxolane derivatives and their phosphoramidates prodrugs is reported. Their ability to block HIV and HBV replication along with their cytotoxicity toward HepG2, human lymphocyte...

journal_title：Bioorganic & medicinal chemistry

authors： Cho JH,Bondana L,Detorio MA,Montero C,Bassit LC,Amblard F,Coats SJ,Schinazi RF

更新日期：2014-12-01 00:00:00

abstract：:Microsomal prostaglandin E(2) synthase-1 (mPGES-1) has been recognized as novel, promising drug target for anti-inflammatory and anticancer drugs. mPGES-1 catalyzes the synthesis of the inducible prostaglandin E(2) in response to pro-inflammatory stimuli, rendering this enzyme extremely interesting in drug discovery p...

journal_title：Bioorganic & medicinal chemistry

authors： De Simone R,Bruno I,Riccio R,Stadler K,Bauer J,Schaible AM,Laufer S,Werz O

更新日期：2012-08-15 00:00:00

abstract：:The design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors, which possess new templates instead of a cyclohexane ring, are described. The mode of interaction with the enzyme is discussed based on the structure-activity relationship (SAR) data obtained for the synthesized inhibitors. Fu...

journal_title：Bioorganic & medicinal chemistry

authors： Ochiai H,Odagaki Y,Ohtani T,Ishida A,Kusumi K,Kishikawa K,Yamamoto S,Takeda H,Obata T,Kobayashi K,Nakai H,Toda M

更新日期：2004-10-01 00:00:00

abstract：:A tetracyclic, conformationally constrained analogue of delta8-THC (2) has been synthesized in which a two carbon bridge exists between C2 and C2'. Two conceptually related syntheses of 2 are described, both of which employ 5,7-dimethoxy-4-oxo-1,2,3,4-tetrahydronaphthoic acid (11) as starting material. This substrate ...

journal_title：Bioorganic & medicinal chemistry

authors： Huffman JW,Yu S

更新日期：1998-12-01 00:00:00

abstract：:Positron emission tomography (PET) using fluorine-18 (18F)-labeled 2-nitroimidazole radiotracers has proven useful for assessment of tumor oxygenation. However, the passive diffusion-driven cellular uptake of currently available radiotracers results in slow kinetics and low tumor-to-background ratios. With the aim to ...

journal_title：Bioorganic & medicinal chemistry

authors： Wanek T,Kreis K,Križková P,Schweifer A,Denk C,Stanek J,Mairinger S,Filip T,Sauberer M,Edelhofer P,Traxl A,Muchitsch VE,Mereiter K,Hammerschmidt F,Cass CE,Damaraju VL,Langer O,Kuntner C

更新日期：2016-11-01 00:00:00

abstract：:In our previous work, a series of 2-amino-3,4-dihydroquinazoline derivativesusing an electron acceptor group was reported to be potent T-type calcium channel blockers and exhibit strong cytotoxic effects against various cancerous cell lines. To investigate the role of the guanidine moiety in the 2-amino-3,4-dihydroqui...

journal_title：Bioorganic & medicinal chemistry

authors： Nam Y,Ryu KD,Jang C,Moon YH,Kim M,Ko D,Chung KS,Gandini MA,Lee KT,Zamponi GW,Lee JY

更新日期：2020-06-01 00:00:00

abstract：:In this Letter, we investigated the binding properties towards nucleic acids of a thymine-functionalized oligolysine, composed of nucleobase-bearing amino acid moieties and underivatized l-lysine residues alternate in the backbone. The basic nucleopeptide proved to be well soluble in water and able to interact with bo...

journal_title：Bioorganic & medicinal chemistry

authors： Roviello GN,Musumeci D,D'Alessandro C,Pedone C

更新日期：2014-02-01 00:00:00

abstract：:Three soft drug analogs and a metabolite of methatropine based on phenylsuccinic structural moiety were synthesized and tested for activity. In an in vivo assay, the soft drugs were found to be two orders of magnitude less potent than methatropine while the carboxylate metabolite was found to be one order of magnitude...

journal_title：Bioorganic & medicinal chemistry

authors： Hammer RH,Gunes E,Kumar GN,Wu WM,Srinivasan V,Bodor NS

更新日期：1993-09-01 00:00:00

abstract：:In the light of known HDAC inhibitors, 33 carboxylic acid derivatives were tested to understand the structural requirements for HDAC inhibition activity. Several modifications were applied to develop the structure-activity relationships of carboxylic acid HDAC inhibitors. HDAC inhibition activities were investigated i...

journal_title：Bioorganic & medicinal chemistry

authors： Bora-Tatar G,Dayangaç-Erden D,Demir AS,Dalkara S,Yelekçi K,Erdem-Yurter H

更新日期：2009-07-15 00:00:00

abstract：:Diflumetorim is a member of pyrimidinamine fungicides that possess excellent antifungal activities. Nevertheless, as reported that the activity of diflumetorim to corn rust (Puccinia sorghi) was not ideal (EC50 = 53.26 mg/L). Herein, a series of novel pyrimidinamine derivatives containing phenyl-thiazole/oxazole moiet...

journal_title：Bioorganic & medicinal chemistry

authors： Yan Z,Liu A,Ou Y,Li J,Yi H,Zhang N,Liu M,Huang L,Ren J,Liu W,Hu A

更新日期：2019-08-01 00:00:00

abstract：:Borrelidin A (1) is produced by several species of Streptomyces and within its bioactive scaffold, the vinylic nitrile moiety is essential for activity. We report herein newly discovered members of the borrelidin family, borrelidin F (2), borrelidin G (3), borrelidin H (4) and borrelidin I (5); all were isolated from ...

journal_title：Bioorganic & medicinal chemistry

authors： Sun J,Shao J,Sun C,Song Y,Li Q,Lu L,Hu Y,Gui C,Zhang H,Ju J

更新日期：2018-05-01 00:00:00

abstract：:Pin1 (Protein interacting with NIMA1) is a cis-trans isomerase and promotes the amide bond rotation of phosphoSer/Thr-Pro motifs in its substrates. Inhibition of Pin1 might be a novel strategy for developing anticancer agents. Herein, a series of pyrimidine derivatives were synthesized and their Pin1 inhibitory activi...

journal_title：Bioorganic & medicinal chemistry

authors： Cui G,Jin J,Chen H,Cao R,Chen X,Xu B

更新日期：2018-05-01 00:00:00

abstract：:We synthesized the biotinylated chondroitin sulfate tetrasaccharides CS-CC [-3)βGalNAc6S(1-4)βGlcA(1-]2 and CS-DD [-3)βGalNAc6S(1-4)βGlcA2S(1-]2 which possess sulfate groups at O-6 of GalNAc and an additional sulfate group at O-2 of GlcA, respectively. We also analyzed interactions among CS-CC and CS-DD and the antibo...

journal_title：Bioorganic & medicinal chemistry

authors： Matsushita K,Nakata T,Takeda-Okuda N,Nadanaka S,Kitagawa H,Tamura JI

更新日期：2018-03-01 00:00:00

abstract：:Two new series of new compounds containing a 6-amino-substituted group or 6-acrylamide-substituted group linked to a 4-anilinoquinazoline nucleus have been discovered as potential EGFR inhibitors. These compounds proved efficient effects on antiproliferative activity and EGFR-TK inhibitory activity. Especially, N(6)-(...

journal_title：Bioorganic & medicinal chemistry

authors： Xu YY,Li SN,Yu GJ,Hu QH,Li HQ

更新日期：2013-10-01 00:00:00

abstract：:A series of novel anthranilic diamides derivatives (7a-s) containing halogen, trifluoromethyl group and cyano group were designed, synthesized, and characterized by melting point, 1H NMR, 13C NMR and elemental analyses. The bioactivity revealed that most of them showed moderate to excellent activities against oriental...

journal_title：Bioorganic & medicinal chemistry

authors： Liu JB,Li FY,Dong JY,Li YX,Zhang XL,Wang YH,Xiong LX,Li ZM

更新日期：2018-07-23 00:00:00

abstract：:Adenosine A1 receptors are attracting great interest as drug targets for their role in cognitive deficits. Antagonism of the adenosine A1 receptor may offer therapeutic benefits in complex neurological diseases, such as Alzheimer's and Parkinson's disease. The aim of this study was to discover potential selective aden...

journal_title：Bioorganic & medicinal chemistry

authors： Van der Walt MM,Terre'Blanche G

更新日期：2015-10-15 00:00:00

abstract：:A series of new hexadentate and pentadentate chelators were designed and synthesized as chelators of (64)Cu. The new pentadentate and hexadentate chelators contain different types of donor groups and are expected to form neutral complexes with Cu(II). The new chelators were evaluated for complex kinetics and stability...

journal_title：Bioorganic & medicinal chemistry

authors： Sin I,Kang CS,Bandara N,Sun X,Zhong Y,Rogers BE,Chong HS

更新日期：2014-04-15 00:00:00

abstract：:The preparation of a series of novel 6-(beta-D-ribofuranosyl)-2-alkyl/aryl-6H-imidazo[1,2-c]pyrimidin-5-one nucleosides and the 2-nitrile nucleosides, 6-(beta-D-ribofuranosyl)-5-oxo-5,6-dihydro-imidazo[1,2-c]pyrimidine-2-carbonitrile and 2R and 2S isomers of 6-(beta-D-ribofuranosyl)-5-oxo-2,3,5,6-tetrahydro-imidazo[1,...

journal_title：Bioorganic & medicinal chemistry

authors： Kifli N,De Clercq E,Balzarini J,Simons C

更新日期：2004-08-01 00:00:00

abstract：:Vinorine synthase (EC 2.3.1.160) catalyses the acetyl-CoA- or CoA-dependent reversible formation of the alkaloids vinorine (or 11-methoxy-vinorine) and 16-epi-vellosimine (or gardneral). The forward reaction leads to vinorine, which is a direct biosynthetic precursor along the complex pathway to the monoterpenoid indo...

journal_title：Bioorganic & medicinal chemistry

authors： Bayer A,Ma X,Stöckigt J

更新日期：2004-05-15 00:00:00

abstract：:A series of novel combretastatin-A4 analogues in which the cis-olefinic bridge is replaced by an imidazolone-amide were synthesized, and their cytotoxicity and tubulin-polymerization inhibitory activities were evaluated. These compounds appear to be potential tubulin-polymerization inhibitors. Compounds 10, 9b and 9c,...

journal_title：Bioorganic & medicinal chemistry

authors： Li YW,Liu J,Liu N,Shi D,Zhou XT,Lv JG,Zhu J,Zheng CH,Zhou YJ

更新日期：2011-06-01 00:00:00

abstract：:Several analogues of (Z)-8-dodecenyl acetate (1a), the major pheromone component of the Oriental fruit moth, Cydia molesta, with chloroformate and lactone functional groups in place of the acetate moiety, were synthesized and investigated for their biological activity at four evaluation levels, i.e. by electroantennog...

journal_title：Bioorganic & medicinal chemistry

authors： Hoskovec M,Hovorka O,Kalinová B,Koutek B,Streinz L,Svatos A,Sebek P,Saman D,Vrkoc J

更新日期：1996-03-01 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