Gram-scale synthesis of pinusolide and evaluation of its antileukemic potential.

abstract：:An inibition study of the β-carbonic anhydrase (CA, EC 4.2.1.1) DmBCA from the insect Drosophila melanogaster with sulfonamides and sulfamates is reported. Among the panel of 40 investigated compounds, the best DmBCA inhibitors were the sulfonylated benzenesulfonamides and ethoxzolamide, which showed inhibition consta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Syrjänen L,Parkkila S,Scozzafava A,Supuran CT

更新日期：2014-07-01 00:00:00

abstract：:A novel series of variously substituted N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-arylsulfonamides has been synthesized and assayed for β-Secretase (BACE1) inhibitory activity. BACE1 is a widely recognized drug target for the prevention and treatment of Alzheimer's Disease (AD). The introduction of benzyl substituents ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bertini S,Ghilardi E,Asso V,Minutolo F,Rapposelli S,Digiacomo M,Saccomanni G,Salmaso V,Sturlese M,Moro S,Macchia M,Manera C

更新日期：2017-11-01 00:00:00

abstract：:A series of Incentrom A analogs that inhibit the chromosome segregation process in yeast were synthesized and tested for their effects on chromosome stability and cell proliferation. Pharmacophore and structure-activity relationship of Incentrom A for the anti-yeast activity were established. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee HY,Jung Y,Kim W,Kim JH,Suh MS,Shin SK,Yoon HJ

更新日期：2008-08-15 00:00:00

abstract：:The 3C-like protease (3CL(pro)) of severe acute respiratory syndrome associated coronavirus (SARS-CoV) is vital for SARS-CoV replication and is a promising drug target. Structure based virtual screening of 308307 chemical compounds was performed using the computation tool Autodock 3.0.5 on a WISDOM Production Environm...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen TT,Ryu HJ,Lee SH,Hwang S,Breton V,Rhee JH,Kim D

更新日期：2011-05-15 00:00:00

abstract：:The synthesis and antihypertensive activity of racemates and enantiomers of substituted 2,3,8,8a-tetrahydro-7H-oxazolo[3,2-a]pyridinedicarboxylates have been reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Martín E,Morán A,Martín ML,San Román L,Puebla P,Medarde M,Caballero E,San Feliciano A

更新日期：2000-02-21 00:00:00

abstract：:A non-methionine FT inhibitor lead structure (1) was designed through computer modeling of the peptidomimetic FT inhibitor ABT839. Optimization of this lead resulted in compounds 2e and 2g, with FT IC(50) values of 1.3 and 1.8 nM, GGT IC(50) of 1400 nM, and EC(50) (Ras processing) values of 13 and 11 nM, respectively....

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang GT,Wang X,Wang W,Hasvold LA,Sullivan G,Hutchins CW,O'Conner S,Gentiles R,Sowin T,Cohen J,Gu WZ,Zhang H,Rosenberg SH,Sham HL

更新日期：2005-01-03 00:00:00

abstract：:The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at alpha7 nicotinic receptors. Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584, were found to lack high affinity at the alpha7 nicotinic receptor. Quinuclidine analogues (1 and 2) of tropiset...

journal_title：Bioorganic & medicinal chemistry letters

authors： Macor JE,Gurley D,Lanthorn T,Loch J,Mack RA,Mullen G,Tran O,Wright N,Gordon JC

更新日期：2001-02-12 00:00:00

abstract：:A series of potent arenavirus inhibitors sharing a benzimidazole core were previously reported by our group. SAR studies were expanded beyond the previous analysis, which involved the attached phenyl rings and methylamino linker portion, to include modifications focused on the benzimidazole core. These changes include...

journal_title：Bioorganic & medicinal chemistry letters

authors： Burgeson JR,Moore AL,Gharaibeh DN,Larson RA,Cerruti NR,Amberg SM,Hruby DE,Dai D

更新日期：2013-02-01 00:00:00

abstract：:A series of gibberellin based molecules were designed and synthesized. Gibberellin derivatives bearing two alpha,beta-unsaturated ketone units showed strong anticancer activities in MTT assay towards a number of human cancer cell lines including HT29, A549, HepG2 and MKN28. The most potent gibberellin derivative (comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen J,Sun Z,Zhang Y,Zeng X,Qing C,Liu J,Li L,Zhang H

更新日期：2009-09-15 00:00:00

abstract：:A new series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates 1-3 were synthesized through an efficient conversion of 2-pivaloyl-4-oxo-6-ethynylpyrido[2,3-d]pyrimidine 5 to the corresponding 4-amino analog 7 via the activated 1,2,4-triazole intermediate 6. Compound 7 was used as the key intermediate for the pre...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gossett LS,Habeck LL,Shackelford KA,Mendelsohn LG,Gates SB,Worzalla JF,Self TD,Theobald KS,Andis SL,Schultz RM,Shih C

更新日期：1999-01-04 00:00:00

abstract：:IRAK4 has been identified as potential therapeutic target for inflammatory and autoimmune diseases. Herein we report the identification and initial SAR studies of a new class of pyrazole containing IRAK4 inhibitors designed to expand chemical diversity and improve off target activity of a previously identified series....

journal_title：Bioorganic & medicinal chemistry letters

authors： Hanisak J,Seganish WM,McElroy WT,Tang H,Zhang R,Tsui HC,Fischmann T,Tulshian D,Tata J,Sondey C,Devito K,Fossetta J,Garlisi CG,Lundell D,Niu X

更新日期：2016-09-01 00:00:00

abstract：:Drug design efforts in the emerging 2-aminothiazole-4-carboxamide class of CHK1 inhibitors have uncovered specific combinations of key substructures within the molecule; resulting in significant improvements in cell-based activity while retaining a greater than one hundred-fold selectivity against CDK2. The X-ray crys...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang X,Cheng CC,Fischmann TO,Duca JS,Richards M,Tadikonda PK,Reddy PA,Zhao L,Siddiqui MA,Parry D,Davis N,Seghezzi W,Wiswell D,Shipps GW Jr

更新日期：2013-05-01 00:00:00

abstract：:Synthesis of a symmetrically branched diglycerol (BGL002, involving one iminodiacetic residue) as a G2 dendron, and the tetradecaglycerol (BGL014, involving one iminodiacetic residue) as a G4 dendron, is described. Several members of the BGL family of G2-G4 dendrons were assembled, with G2 bearing four hydroxyl groups...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nemoto H,Ishihara A,Araki T,Katagiri A,Kamiya M,Matsushita T,Hattori H,Mimura Y,Tomoda Y,Yamasaki M

更新日期：2011-08-15 00:00:00

abstract：:Hypolipidemic effects of the newly synthesized 5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione-based fibrates were evaluated in Triton WR-1339 and high-fat diet (HFD)-induced hyperlipidemic mice. Preliminary screening of all the synthesized compounds was done by using an acute model (Triton WR-1339 model), in which compo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen ZZ,Xie YD,Shao LH,Wang QT,Xu YH,Bian XL

更新日期：2018-12-15 00:00:00

abstract：:Alzheimer's disease is characterized by the accumulation of β-amyloid (Aβ) plaques and neurofibrillary tangles (NFTs) in the brain. We previously developed [(18)F]fluoropropylcurcumin ([(18)F]FP-curcumin), which demonstrated excellent binding affinity (K(i)=0.07 nM) for Aβ(1-40) aggregates and good pharmacokinetics in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee I,Yang J,Lee JH,Choe YS

更新日期：2011-10-01 00:00:00

abstract：:A series of methoxycarbonyl group modified nidulalin A analogs were synthesized to improve stability against esterases. The amide derivatives showed cytotoxic activity along with inhibitory activity against DNA topoisomerase II. Among the analogs, amide 9a exhibited antitumor activity in Colon 26 murine tumor model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sato S,Suga Y,Yoshimura T,Nakagawa R,Tsuji T,Umemura K,Andoh T

更新日期：1999-09-20 00:00:00

abstract：:QSAR models represent the relationship of biological activity with either physicochemical parameters or structural indices. QSAR study was performed on some arylpiperazines as 5-HT(1A)/alpha(1)-adrenergic receptor antagonists using E-state indices to identify the pharmacophoric requirements. It was found that some of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Debnath B,Samanta S,Naskar SK,Roy K,Jha T

更新日期：2003-09-01 00:00:00

abstract：:A series of (N-benzyl-N-phenylsulfonamido)alkyl amides were developed from classic and parallel synthesis strategies. Compounds with good in vitro and in vivo γ-secretase activity were identified and described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parker MF,Barten DM,Bergstrom CP,Bronson JJ,Corsa JA,Dee MF,Gai Y,Guss VL,Higgins MA,Keavy DJ,Loo A,Mate RA,Marcin LR,McElhone KE,Polson CT,Roberts SB,Macor JE

更新日期：2012-11-15 00:00:00

abstract：:We have succeeded in the acquisition of DNA aptamers that recognize chitin using in vitro selection. The obtained DNA aptamers have the stem-loop or bulge loop structures with guanine rich loop clusters and the clockwise B-form stems. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fukusaki E,Kato T,Maeda H,Kawazoe N,Ito Y,Okazawa A,Kajiyama S,Kobayashi A

更新日期：2000-03-06 00:00:00

abstract：:p38alpha Mitogen Activated Protein Kinase (MAP kinase) is an intracellular soluble serine threonine kinase. p38alpha kinase is activated in response to cellular stresses, growth factors and cytokines such as interleukin-1 (IL-1) and tumor necrosis factor alpha (TNF-alpha). The central role of p38alpha activation in se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mavunkel BJ,Chakravarty S,Perumattam JJ,Luedtke GR,Liang X,Lim D,Xu YJ,Laney M,Liu DY,Schreiner GF,Lewicki JA,Dugar S

更新日期：2003-09-15 00:00:00

abstract：:The synthesis and antioxidant activity of oligo(ethylene glycol)-modified manganese salen complexes are reported. Their SOD activities were similar and 2- to 3-fold more potent than the standard compound EUK-134. Their catalase-like activity was lower than that of EUK-134 in the initial conversion rate; however, some ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Park W,Lim D

更新日期：2009-02-01 00:00:00

abstract：:The esterase, phosphatase, and sulfatase activities of carbonic anhydrase (CA, EC 4.2.1.1) isozymes, CA I, II, and XIII with 4-nitrophenyl esters as substrates was investigated. These enzymes show esterase activity with 4-nitrophenyl acetate as substrate, with second order rate constants in the range of 753-7706M(-1)s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Innocenti A,Scozzafava A,Parkkila S,Puccetti L,De Simone G,Supuran CT

更新日期：2008-04-01 00:00:00

abstract：:The reduced activation of PPARs has a positive impact on cancer cell growth and viability in multiple preclinical tumor models, suggesting a new therapeutic potential for PPAR antagonists. In the present study, the benzothiazole amides 2a-g were synthesized and their activities on PPARs were investigated. Transactivat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ammazzalorso A,De Lellis L,Florio R,Laghezza A,De Filippis B,Fantacuzzi M,Giampietro L,Maccallini C,Tortorella P,Veschi S,Loiodice F,Cama A,Amoroso R

更新日期：2019-08-15 00:00:00

abstract：:Systematic SAR studies of the different regioisomers and homologues of the spiro(indane-1,4-piperidine) moiety in the growth hormone secretagogue L-162,752 are presented. Among them, spiro(3H-1-benzopyran-2,3-piperidine) was found to afford secretagogues with low nanomolar in vitro activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yang L,Morriello G,Prendergast K,Cheng K,Jacks T,Chan WW,Schleim KD,Smith RG,Patchett AA

更新日期：1998-01-06 00:00:00

abstract：:Elevated triglycerides (TG) contribute towards increased risk for cardiovascular disease. Lipoprotein lipase (LPL) is an enzyme that is responsible for the metabolism of core triglycerides of very-low density lipoproteins (VLDL) and chylomicrons in the vasculature. In this study, we explored the structure-activity rel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Geldenhuys WJ,Caporoso J,Leeper TC,Lee YK,Lin L,Darvesh AS,Sadana P

更新日期：2017-01-15 00:00:00

abstract：:A 70% EtOH extract from the bark of Syringareticulata has shown significant antioxidant activity. Chemical study on the extract resulted in the isolation of seventeen compounds (1-17), including a novel oleoside-type secoiridoid glucoside, reticuloside (1), and the structures were elucidated on the basis of extensive ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bi X,Li W,Sasaki T,Li Q,Mitsuhata N,Asada Y,Zhang Q,Koike K

更新日期：2011-11-01 00:00:00

abstract：:Amino-1,2,5-trideoxy-2,5-imino-D-mannitol was fluorescently tagged by reaction with dansyl chloride at N-1 or by attachment of a dansyl amide bearing spacer to this centre. Compounds obtained are highly potent inhibitors of beta-glucosidase exhibiting Ki values in the single figure nanomolar range. The 1-N-dansyl subs...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hermetter A,Scholze H,Stütz AE,Withers SG,Wrodnigg TM

更新日期：2001-05-21 00:00:00

abstract：:We report the design, synthesis, and structure-activity relationship (SAR) of a series of novel pyrido[2,3-d]pyrimidin-7-one compounds as potent Abl kinase inhibitors. We evaluate their specificity profile against a panel of human recombinant kinases, as well as their biological profile toward a panel of well-characte...

journal_title：Bioorganic & medicinal chemistry letters

authors： Antczak C,Veach DR,Ramirez CN,Minchenko MA,Shum D,Calder PA,Frattini MG,Clarkson B,Djaballah H

更新日期：2009-12-15 00:00:00

abstract：:Starting from our previously identified novel c-Met kinase inhibitors bearing 1H-imidazo[4,5-h][1,6]naphthyridin-2(3H)-one scaffold, a global structural exploration was conducted to furnish an optimal binding motif for further development, directed by the enzyme inhibitory mechanism. First round SAR study picked two i...

journal_title：Bioorganic & medicinal chemistry letters

authors： An XD,Liu H,Xu ZL,Jin Y,Peng X,Yao YM,Geng M,Long YQ

更新日期：2015-02-01 00:00:00

abstract：:O6-Benzylguanine (O6-BG) is a substrate of O6-methylguanine-DNA methyltransferase (MGMT), which is involved in drug resistance of chemotherapy in the majority of glioblastoma multiform. For clinical diagnosis, it is hoped that the MGMT expression level could be determined by a noninvasive method to understand the deta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Koyama H,Ikenuma H,Toda H,Kondo G,Hirano M,Kato M,Abe J,Yamada T,Wakabayashi T,Ito K,Natsume A,Suzuki M

更新日期：2017-05-01 00:00:00