Synthesis and DNA-cleaving activity of lactenediynes conjugated with DNA-complexing moieties.

abstract：:Novel quinazolin- and benzothiazol-6-yloxyacetamides show excellent in vivo activity against the three economically most important Oomycete pathogens Phytophthora infestans, Plasmopara viticola and Pythium ultimum. They are polar analogs of known quinolin-6-yloxyacetamides, which are not active against the soil-borne ...

journal_title：Bioorganic & medicinal chemistry

authors： Beaudegnies R,Quaranta L,Murphy Kessabi F,Lamberth C,Knauf-Beiter G,Fraser T

更新日期：2016-02-01 00:00:00

abstract：:A series of 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives was synthesized and 13 of them were selected by the National Cancer Institute (NCI) and evaluated for their in vitro anticancer activity. Seven of the investigated compounds, 3i, 3j, 3k, 3o, 3p, 3q, and 3r, displayed high a...

journal_title：Bioorganic & medicinal chemistry

authors： Aboraia AS,Abdel-Rahman HM,Mahfouz NM,El-Gendy MA

更新日期：2006-02-15 00:00:00

abstract：:A novel class of N-substituted tetrahydropyridine derivatives was found to have multiple kinetic mechanisms of monoamine oxidase A inhibition. Eleven structurally similar tetrahydropyridine derivatives were synthesized and evaluated as inhibitors of MAO-A and MAO-B. The most potent MAO-A inhibitor in the series, 2,4-d...

journal_title：Bioorganic & medicinal chemistry

authors： Wichitnithad W,O'Callaghan JP,Miller DB,Train BC,Callery PS

更新日期：2011-12-15 00:00:00

abstract：:The discovery of the first class of potent glucose-6-phosphatase catalytic site inhibitors, substituted 4,5,6,7-tetrahydrothieno[3,2-c]- and -[2,3-c]pyridines, is described. Optimisation of this series involved solution phase combinatorial synthesis and very potent compounds were prepared with IC50 values down to 140 ...

journal_title：Bioorganic & medicinal chemistry

authors： Madsen P,Lundbeck JM,Jakobsen P,Varming AR,Westergaard N

更新日期：2000-09-01 00:00:00

abstract：:Purinergic receptors, also known as purinoceptors, are ligand gated membrane ion channels involved in many cellular functions. Among all identified purinergic receptors, P2X₇ subform is unique since it induces the caspase activity, cytokine secretion, and apoptosis. The distribution of P2X₇ receptors, and the need of ...

journal_title：Bioorganic & medicinal chemistry

authors： Mehta N,Kaur M,Singh M,Chand S,Vyas B,Silakari P,Bahia MS,Silakari O

更新日期：2014-01-01 00:00:00

abstract：:Posttranslational modification of proteins with ubiquitin and ubiquitin-like modifiers such as SUMO can be reverted by specific proteases, also referred to as deubiquitinases and isopeptidases, most of which are cysteine-dependent. We have found that the replacement of the conserved C-terminal glycine with propargylam...

journal_title：Bioorganic & medicinal chemistry

authors： Sommer S,Weikart ND,Linne U,Mootz HD

更新日期：2013-05-01 00:00:00

abstract：:The pH-rate profile for the hydrolysis of 3'-phosphoadenosine 5'-phosphosulfate (PAPS) in aqueous solution has been measured. Comparison with other data suggests that hydrolysis occurs by almost complete unimolecular elimination of sulfur trioxide, with weak involvement of a molecule of water in the transition state. ...

journal_title：Bioorganic & medicinal chemistry

authors： Bedford CT,Kirby AJ,Logan CJ,Drummond JN

更新日期：1995-02-01 00:00:00

abstract：:Many therapeutically-relevant protein-protein interactions (PPIs) have been reported that feature a helix and helix-binding cleft at the interface. Given this, different approaches to disrupting such PPIs have been developed. While short peptides (<15 amino acids) typically do not fold into a stable helix, researchers...

journal_title：Bioorganic & medicinal chemistry

authors： Tennyson RL,Walker SN,Ikeda T,Harris RS,McNaughton BR

更新日期：2018-03-15 00:00:00

abstract：:Electronic parameters (molecular electrostatic potential MEP, charge distribution on the nitrogen atoms, dipole moment mu and ionization potential IP) were calculated by semiempirical quantum chemistry methods for 2 sets (X = H and m-CF3, the syn- and anti-rotamers of the latter being considered separately) of the 6-a...

journal_title：Bioorganic & medicinal chemistry

authors： Karolak-Wojciechowska J,Lange J,Kwiatkowski W,Gniewosz M,Plenkiewicz J

更新日期：1994-08-01 00:00:00

abstract：:Tea catechins, an important class of polyphenols, have been shown to have wide spectrum of antitumor activity believed to be due mainly to their antioxidative effect. In this study, the radical scavenging behavior of catechins on 2,2-diphenyl-1-picrylhydrazyl (DPPH) was studied. Two reaction products of (+)-catechin, ...

journal_title：Bioorganic & medicinal chemistry

authors： Sang S,Cheng X,Stark RE,Rosen RT,Yang CS,Ho CT

更新日期：2002-07-01 00:00:00

abstract：:To establish the role of the ferrocenyl moiety in the antiplasmodial activity of ferroquine, compounds in which this moiety is replaced by the corresponding ruthenium-based moieties were synthesized and evaluated. In both the sensitive (D10) and resistant (K1) strains of Plasmodium falciparum, ruthenoquine analogues s...

journal_title：Bioorganic & medicinal chemistry

authors： Blackie MA,Beagley P,Croft SL,Kendrick H,Moss JR,Chibale K

更新日期：2007-10-15 00:00:00

abstract：:A series of 3-amino-benzo[d]isoxazole-/3-aminoindazole-based compounds were designed, synthesized and pharmacologically evaluated as tyrosine kinase c-Met inhibitors. The SAR study was conducted leading to identification of nine compounds (8d, 8e, 12, 28a-d, 28h and 28i) with IC50s less than 10nM against c-Met. Compou...

journal_title：Bioorganic & medicinal chemistry

authors： Jiang X,Liu H,Song Z,Peng X,Ji Y,Yao Q,Geng M,Ai J,Zhang A

更新日期：2015-02-01 00:00:00

abstract：:The four stereoisomeric 1,5-dideoxy-1,5-iminopentitols with D-arabino-(D-lyxo-) (3), ribo- (9), L-lyxo (L-arabino-) (13) and xylo-(18) configurations were synthesized. The corresponding aldonolactones (1, 7 and 11) or aldonic acid ester (15b) having a leaving group at C-5 gave by reaction with aqueous ammonia, the 5-a...

journal_title：Bioorganic & medicinal chemistry

authors： Godskesen M,Lundt I,Madsen R,Winchester B

更新日期：1996-11-01 00:00:00

abstract：:Here we report on a novel fluorescent analog of phenytoin as a potential inhibitor of neuropathic pain with potential use as an imaging agent. Compound 2 incorporated a heptyl side chain and dansyl moiety onto the parent compound phenytoin and produced greater displacement of BTX from sodium channels and greater funct...

journal_title：Bioorganic & medicinal chemistry

authors： Walls TH,Grindrod SC,Beraud D,Zhang L,Baheti AR,Dakshanamurthy S,Patel MK,Brown ML,MacArthur LH

更新日期：2012-09-01 00:00:00

abstract：:Sphingolipids are ubiquitous and abundant components of all eukaryotic and some prokaryotic organisms. Sphingolipids show a large structural variety not only between the different species, but also within an individual cell. This variety is not limited to alterations in the polar headgroups of e.g. glycosphingolipids,...

journal_title：Bioorganic & medicinal chemistry

authors： Saied EM,Le TL,Hornemann T,Arenz C

更新日期：2018-08-07 00:00:00

abstract：:Eight novel 2-(2,6-dioxopiperidin-3-yl)phthalimidine EM-12 dithiocarbamates 9 and 10, N-substituted 3-(phthalimidin-2-yl)-2,6-dioxopiperidines 11-14 and 3-substituted 2,6-dioxopiperidines 16 and 18 were synthesized as tumor necrosis factor-α (TNF-α) synthesis inhibitors. Synthesis involved utilization of a novel conde...

journal_title：Bioorganic & medicinal chemistry

authors： Luo W,Yu QS,Salcedo I,Holloway HW,Lahiri DK,Brossi A,Tweedie D,Greig NH

更新日期：2011-07-01 00:00:00

abstract：:Synthesis of [(11)C]celecoxib, a selective COX-2 inhibitor, and [(11)C]SC-62807, a major metabolite of celecoxib, were achieved and the potential of these PET probes for assessing the function of drug transporter in biliary excretion was evaluated. The synthesis of [(11)C]celecoxib was achieved in one-pot by reacting ...

journal_title：Bioorganic & medicinal chemistry

authors： Takashima-Hirano M,Takashima T,Katayama Y,Wada Y,Sugiyama Y,Watanabe Y,Doi H,Suzuki M

更新日期：2011-05-01 00:00:00

abstract：:This study measured the antiplasmodial activity of nine zinc-dipicolylamine (ZnDPA) complexes against three strains of Plasmodium falciparum, the causative parasite of malaria. Growth inhibition assays showed significant activity against all tested strains, with 50% inhibitory concentrations between 5 and 600nM and al...

journal_title：Bioorganic & medicinal chemistry

authors： Rice DR,de Lourdes Betancourt Mendiola M,Murillo-Solano C,Checkley LA,Ferdig MT,Pizarro JC,Smith BD

更新日期：2017-05-15 00:00:00

abstract：:Reverse chemical proteomics using T7 phage display is a powerful technique for identifying cellular receptors of biologically active small molecules. However, to date this method has generally been limited to cDNA libraries constructed from mRNA isolated from eukaryotes. In this paper, we describe the construction of ...

journal_title：Bioorganic & medicinal chemistry

authors： Piggott AM,Kriegel AM,Willows RD,Karuso P

更新日期：2009-10-01 00:00:00

abstract：:While hemoglobin is one of the most well characterized proteins due to its function in oxygen transport, few additional properties of hemoglobin have been described. While screening serum samples for novel antimicrobial factors, it was found that intact hemoglobin tetramers, including that from human, exhibited consid...

journal_title：Bioorganic & medicinal chemistry

authors： Parish CA,Jiang H,Tokiwa Y,Berova N,Nakanishi K,McCabe D,Zuckerman W,Xia MM,Gabay JE

更新日期：2001-02-01 00:00:00

abstract：:The role of novel triazine derivatives against oxidative stress exerted by hydrogen peroxide on differentiated rat pheochromocytoma (PC12) cell line was examined and a consistent protection from H(2)O(2)-induced cell death, associated with a marked reduction in caspase-3 activation, was observed. Moreover, activation ...

journal_title：Bioorganic & medicinal chemistry

authors： Irannejad H,Amini M,Khodagholi F,Ansari N,Tusi SK,Sharifzadeh M,Shafiee A

更新日期：2010-06-15 00:00:00

abstract：:Aryl diketoacids (ADK) and their bioisosteres are among the most promising HIV-1 integrase (IN) inhibitors. Previously, we designed a series of ADK dimers as a new class of IN inhibitors that were hypothesized to target two divalent metal ions on the active site of IN. Herein we present a further structure-activity re...

journal_title：Bioorganic & medicinal chemistry

authors： Zeng LF,Jiang XH,Sanchez T,Zhang HS,Dayam R,Neamati N,Long YQ

更新日期：2008-08-15 00:00:00

abstract：:Peptidomimetic compounds possessing a caprolactam ring constraint were prepared and evaluated as interleukin-1beta converting enzyme (ICE) inhibitors. The caprolactam ring was used to constrain the P3 region of our inhibitors. This strategy proved to be effective for the synthesis of ICE inhibitors, maintaining key hy...

journal_title：Bioorganic & medicinal chemistry

authors： Wang Y,O'Neil SV,Wos JA,Oppong KA,Laufersweiler MC,Soper DL,Ellis CD,Baize MW,Fancher AN,Lu W,Suchanek MK,Wang RL,Schwecke WP,Cruze CA,Buchalova M,Belkin M,De B,Demuth TP Jr

更新日期：2007-02-01 00:00:00

abstract：:Multidrug-resistant bacterial infections continue to be a rising global health concern. Herein is described the development of a class of novel 2-aminobenzimidazoles with antibiotic activity. These active 2-aminobenzimidazoles retain their antibiotic activity against several strains of multidrug-resistant Staphylococc...

journal_title：Bioorganic & medicinal chemistry

authors： Huigens RW 3rd,Reyes S,Reed CS,Bunders C,Rogers SA,Steinhauer AT,Melander C

更新日期：2010-01-15 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 previously reported the discovery and initial SAR of the [1,7]naphthyridine-3-carbonitriles and quinoline-3-carbonitriles as Tumor Progression Loci-2 (Tpl2) kinase inhibitors. In this paper, we report new SAR efforts which have led to the identification of 4-alkylamino-[1,7]naphthyridine-3-carbonitriles. These...

journal_title：Bioorganic & medicinal chemistry

authors： Kaila N,Green N,Li HQ,Hu Y,Janz K,Gavrin LK,Thomason J,Tam S,Powell D,Cuozzo J,Hall JP,Telliez JB,Hsu S,Nickerson-Nutter C,Wang Q,Lin LL

更新日期：2007-10-01 00:00:00

abstract：:For elucidation of the structural and conformational requirements on the endotoxic and antagonistic activity of lipid A derivatives, we designed and synthesized lipid A analogues containing acidic amino acid residues in place of the non-reducing end phosphorylated glucosamine. Definite switching of the endotoxic or an...

journal_title：Bioorganic & medicinal chemistry

authors： Akamatsu M,Fujimoto Y,Kataoka M,Suda Y,Kusumoto S,Fukase K

更新日期：2006-10-01 00:00:00

abstract：:The blending of key structural features from the purine and pyrimidine nucleobase scaffolds gives rise to a new class of hybrid nucleosides. The purine-pyrimidine hybrid nucleosides can be viewed as either N-3 ribosylated purines or 5,6-disubstituted pyrimidines, thus recognition by both purine- and pyrimidine-metabol...

journal_title：Bioorganic & medicinal chemistry

authors： Sadler JM,Mosley SL,Dorgan KM,Zhou ZS,Seley-Radtke KL

更新日期：2009-08-01 00:00:00

abstract：:A novel series of fluorinated 2-phenylindole derivatives were synthesized and evaluated as β-amyloid imaging probes for PET. The in vitro inhibition assay demonstrated that their binding affinities for Aβ(1-42) aggregates ranged from 28.4 to 1097.8 nM. One ligand was labeled with (18)F ([(18)F]1a) for its high affinit...

journal_title：Bioorganic & medicinal chemistry

authors： Fu H,Yu L,Cui M,Zhang J,Zhang X,Li Z,Wang X,Jia J,Yang Y,Yu P,Jia H,Liu B

更新日期：2013-07-01 00:00:00

abstract：:A type of novel α,β-unsaturated cyclohexanone analogous, which designed based on the curcumin core structure, have been discovered as potential EGFR inhibitors. These compounds exhibit potent antiproliferative activity in two human tumor cell lines (Hep G2 and B16-F10). Among them, compounds I(3) and I(12) displayed t...

journal_title：Bioorganic & medicinal chemistry

authors： Xu YY,Cao Y,Ma H,Li HQ,Ao GZ

更新日期：2013-01-15 00:00:00