Synthesis of potent taxoids for tumor-specific delivery using monoclonal antibodies.

abstract：:The structure-activity relationship and the synthesis of novel N-[(3S)-pyrrolidin-3-yl]benzamides as dual serotonin and noradrenaline monoamine reuptake inhibitors (SNRI) is described. Preferred compound 9 aka PF-184,298 is a potent SNRI with good selectivity over dopamine reuptake inhibition (DRI), good in vitro meta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wakenhut F,Allan GA,Fish PV,Fray MJ,Harrison AC,McCoy R,Phillips SC,Ryckmans T,Stobie A,Westbrook D,Westbrook SL,Whitlock GA

更新日期：2009-09-01 00:00:00

abstract：:A series of 5-aminomethylquinoxaline-2,3-diones have been identified as potent and selective AMPA antagonists. Some of these compounds are also active at the glycine-binding site of the NMDA receptors. A number of these novel, water-soluble quinoxaline-2,3-dione derivatives display protective effects in the electrosho...

journal_title：Bioorganic & medicinal chemistry letters

authors： Auberson YP,Bischoff S,Moretti R,Schmutz M,Veenstra SJ

更新日期：1998-01-06 00:00:00

abstract：:Gram positive (Bacillus cereus, B. subtilis), Gram negative (Pseudomonas aeruginosa, Escherichia coli) bacteria, and Candida albicans as a representative of fungi were used for screening the in vitro antimicrobial activity of diarylamines in the 2,3,5-trimethylbenzo[b]thiophene series bearing different substituents, s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ferreira IC,Calhelha RC,Estevinho LM,Queiroz MJ

更新日期：2004-12-06 00:00:00

abstract：:The design and synthesis of new 1alpha,25-dihydroxy-19-norvitamin D(3) analogues 3a-c, which have an amide bond in the molecule instead of the diene, are described. The A-ring moiety was constructed by a (3S,5S)-3,5-dihydroxypiperidine derivative (9, 11, or 13) prepared from D-mannose, and a CD-ring carboxylic acid 16...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suhara Y,Kittaka A,Ono K,Kurihara M,Fujishima T,Yoshida A,Takayama H

更新日期：2002-12-16 00:00:00

abstract：:Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X(7) receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and selective at the P2X(7) receptor in both human and rodent. Compound (entry 31) exhibited oral efficacy...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matasi JJ,Brumfield S,Tulshian D,Czarnecki M,Greenlee W,Garlisi CG,Qiu H,Devito K,Chen SC,Sun Y,Bertorelli R,Geiss W,Le VD,Martin GS,Vellekoop SA,Haber J,Allard ML

更新日期：2011-06-15 00:00:00

abstract：:5-Hydroxyalkyl-4-phenylpyridines have been identified as a novel class of glucagon antagonists with potential utility for the treatment of diabetes. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure-activity relationships led to the discovery of a potent antago...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ladouceur GH,Cook JH,Doherty EM,Schoen WR,MacDougall ML,Livingston JN

更新日期：2002-02-11 00:00:00

abstract：:Structure-based design and synthesis of the 3,4'-bispyridinylethylene series led to the discovery of 3-isoquinolinylpyridine 13a as a potent PKB/Akt inhibitor with an IC(50) of 1.3nM against Akt1. Compound 13a shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li Q,Woods KW,Thomas S,Zhu GD,Packard G,Fisher J,Li T,Gong J,Dinges J,Song X,Abrams J,Luo Y,Johnson EF,Shi Y,Liu X,Klinghofer V,Des Jong R,Oltersdorf T,Stoll VS,Jakob CG,Rosenberg SH,Giranda VL

更新日期：2006-04-01 00:00:00

abstract：:Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D(3)/D(2) compound (1) led to a series of new piperazine derivatives having affinity to both dopamine D(3) and D(2) receptors. Several members of this group showed excellent pharmacokinetic and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Agai-Csongor E,Domány G,Nógrádi K,Galambos J,Vágó I,Keserű GM,Greiner I,Laszlovszky I,Gere A,Schmidt E,Kiss B,Vastag M,Tihanyi K,Sághy K,Laszy J,Gyertyán I,Zájer-Balázs M,Gémesi L,Kapás M,Szombathelyi Z

更新日期：2012-05-15 00:00:00

abstract：:Cyclic azobenzene carboxylic acid was synthesized using a shortened route. After reaction with D-threolinol, the resulting cyclic azobenzene-D-threolinol (cAB-Thr) building block was transformed into the corresponding DMTr-protected phosphoramidite, and incorporated into oligodeoxynucleotides at various positions and ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Eljabu F,Dhruval J,Yan H

更新日期：2015-12-01 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：:Germinal center kinase-like kinase (GLK, also known as MAP4K3) has been hypothesized to have an effect on key cellular activities, including inflammatory responses. GLK is required for activation of protein kinase C-θ (PKCθ) in T cells. Controlling the activity of T helper cell responses could be valuable for the trea...

journal_title：Bioorganic & medicinal chemistry letters

authors： May-Dracka TL,Arduini R,Bertolotti-Ciarlet A,Bhisetti G,Brickelmaier M,Cahir-McFarland E,Enyedy I,Fontenot JD,Hesson T,Little K,Lyssikatos J,Marcotte D,McKee T,Murugan P,Patterson T,Peng H,Rushe M,Silvian L,Spilker K

更新日期：2018-06-01 00:00:00

abstract：:A new acylphenol, malabaricone E (1) together with the known malabaricones A-C (2-4), maingayones A and B (5 and 6) and maingayic acid B (7) were isolated from the ethyl acetate extract of the fruits of Myristica cinnamomea King. Their structures were determined by 1D and 2D NMR techniques and LCMS-IT-TOF analysis. Co...

journal_title：Bioorganic & medicinal chemistry letters

authors： Abdul Wahab SM,Sivasothy Y,Liew SY,Litaudon M,Mohamad J,Awang K

更新日期：2016-08-01 00:00:00

abstract：:The thrombin receptor (PAR-1) is activated by alpha-thrombin to stimulate various cell types, including platelets, through the tethered-ligand sequence SFLLRN. Macrocyclic peptide analogues of SFLLRN were synthesized and evaluated in vitro. In general, the compounds were much less potent in inducing platelet aggregati...

journal_title：Bioorganic & medicinal chemistry letters

authors： McComsey DF,Hecker LR,Andrade-Gordon P,Addo MF,Maryanoff BE

更新日期：1999-01-18 00:00:00

abstract：:A series of new voltage-gated sodium channel blockers were prepared based on the screening lead succinic diamide BPBTS. Replacement of the succinimide linker with the more rigid cyclic 1,2-trans-diamide linker was well tolerated. N-Methylation on the biphenylsulfonamide side of the amide moiety significantly reduced t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shao PP,Ok D,Fisher MH,Garcia ML,Kaczorowski GJ,Li C,Lyons KA,Martin WJ,Meinke PT,Priest BT,Smith MM,Wyvratt MJ,Ye F,Parsons WH

更新日期：2005-04-01 00:00:00

abstract：:Novel triazolopyrimidine acylsulfonamides class of antimycobacterial agents, which are mycobacterial acetohydroxyacid synthase (AHAS) inhibitors were designed by hybridization of known AHAS inhibitors such as sulfonyl urea and triazolopyrimidine sulfonamides. This Letter describes the synthesis and SAR studies of this...

journal_title：Bioorganic & medicinal chemistry letters

authors： Patil V,Kale M,Raichurkar A,Bhaskar B,Prahlad D,Balganesh M,Nandan S,Shahul Hameed P

更新日期：2014-05-01 00:00:00

abstract：:The reaction of methoxypoly(ethylene glycol)-4-nitrophenyl carbonate with amphotericin B has been used to prepare a new conjugate of amphotericin B (mPEG-AmB). A preliminary screening of in vitro antifungal activity has suggested that mPEG-AmB possesses a similar effect and a similar spectrum of activity as the conven...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sedlák M,Buchta V,Kubicová L,Simůnek P,Holcapek M,Kasparová P

更新日期：2001-11-05 00:00:00

abstract：:Inhibition of the newest isoform of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), CA XV, with a series of phenols was investigated. Murine CA XV showed an inhibition profile by phenols distinct of those of the cytosolic human isoforms CA I and II. Phenol and some of its 2-, 3-, and 4-substituted derivatives i...

journal_title：Bioorganic & medicinal chemistry letters

authors： Innocenti A,Hilvo M,Scozzafava A,Parkkila S,Supuran CT

更新日期：2008-06-15 00:00:00

abstract：:Two series of 5-phenyl furocoumarin derivatives were designed and prepared based on our previous research. All new compounds were characterized by (1)H NMR, (13)C NMR and mass spectra. Furthermore, they were screened for their vasodilatory activity on the mesenteric artery of Sprague-Dawley rats, and they all presente...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang C,Wang T,Huang L,Lu W,Zhang J,He H

更新日期：2016-01-15 00:00:00

abstract：:A novel fluorescein-based fluorescent probe for nitroxyl (HNO) based on the reductive Staudinger ligation of HNO with an aromatic phosphine was prepared. This probe reacts with HNO derived from Angeli's salt and 4-bromo Piloty's acid under physiological conditions without interference by other biological redox species...

journal_title：Bioorganic & medicinal chemistry letters

authors： Miao Z,Reisz JA,Mitroka SM,Pan J,Xian M,King SB

更新日期：2015-01-01 00:00:00

abstract：:Two novel compounds with mannose-derived structure, bearing a tetrazole (compound 3) and a sulfone group (compound 4) in terminal position, have been prepared from methyl α-d-mannopyranoside in reduced number of steps. The angiogenic activity of 3 and 4 has been screened using the chick chorioallantoic membrane (CAM) ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ionescu C,Sippelli S,Toupet L,Barragan-Montero V

更新日期：2016-01-15 00:00:00

abstract：:Starting from a thiazolidin-4-one HTS hit, a novel series of substituted lactams was identified and developed as dual orexin receptor antagonists. In this Letter, we describe our initial efforts towards the improvement of potency and metabolic stability. These investigations delivered optimized lead compounds with CNS...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sifferlen T,Boller A,Chardonneau A,Cottreel E,Hoecker J,Aissaoui H,Williams JT,Brotschi C,Heidmann B,Siegrist R,Gatfield J,Treiber A,Brisbare-Roch C,Jenck F,Boss C

更新日期：2014-02-15 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：:Telomerase and telomere maintenance are emerging targets for the treatment of human cancers. We report here on the targeting of the telomere-telomerase complex with a series of small molecules based on an acridine platform. A series of 3,6-bisamidoacridines with extended 9-anilino sidechains were designed and synthesi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Schultes CM,Guyen B,Cuesta J,Neidle S

更新日期：2004-08-16 00:00:00

abstract：:A series of 9-alkylaminoacridines were synthesized and evaluated for activity against two strains of methicillin-resistant and one strain of methicillin-sensitive Staphylococcus aureus. Results are presented that show a clear structure activity relationship between the N-alkyl chain length and antibacterial activity w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Benoit AR,Schiaffo C,Salomon CE,Goodell JR,Hiasa H,Ferguson DM

更新日期：2014-07-15 00:00:00

abstract：:The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-(S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of dipeptidyl peptidase IV (DPP IV) are reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiao L,Baumann CA,Crysler CS,Ninan NS,Abad MC,Spurlino JC,Desjarlais RL,Kervinen J,Neeper MP,Bayoumy SS,Williams R,Deckman IC,Dasgupta M,Reed RL,Huebert ND,Tomczuk BE,Moriarty KJ

更新日期：2006-01-01 00:00:00

abstract：:A novel series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols, have been discovered by combining virtual and focused screening efforts with design techniques. Synthesis of the two diastereomeric isomers of the molecule followed by chiral resolution of each enantiomer revealed the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim CY,Mahaney PE,McConnell O,Zhang Y,Manas E,Ho DM,Deecher DC,Trybulski EJ

更新日期：2009-09-01 00:00:00

abstract：:The marine alkaloids, longamide B (1), longamide B methyl ester (2), hanishin (3), and a series of non-naturally occurring analogues were synthesized in an efficient manner from inexpensive commercially available dl-aspartic acid dimethyl ester. The cytotoxicities of these natural products (1-3) and their analogues (9...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhao DG,Ma YY,Peng W,Zhou AY,Zhang Y,Ding L,Du Z,Zhang K

更新日期：2016-01-01 00:00:00

abstract：:Recent studies have highlighted a key role in regulating gene transcription, in both eukaryotes and prokaryotes, by enzymes that control the acetylation and deacetylation of histones. In particular, inhibitors of histone deacetylases (HDAC-Is) have been shown effective in controlling the development of many parasites,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Giannini G,Battistuzzi G,Vignola D

更新日期：2015-02-01 00:00:00

abstract：:For further structure-activity relationship (SAR) research of OSW saponins, a cholestane glycoside, namely 3beta, 16beta, 26-trihydroxycholest-5-en-22-one 16-O-(2-O-4-methoxybenzoyl-beta-D-xylopyranosyl)-(1-->3)-2-O-acetyl-alpha-L-arabinopyranoside (1) together with two 1-->4-linked disaccharide analogues (2 and 3) we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng D,Zhou L,Guan Y,Chen X,Zhou W,Chen X,Lei P

更新日期：2010-09-15 00:00:00

abstract：:Selective σ2 ligands continue to be an active target for medications to attenuate the effects of psychostimulants. In the course of our studies to determine the optimal substituents in the σ2-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorop...

journal_title：Bioorganic & medicinal chemistry letters

authors： Motel WC,Healy JR,Viard E,Pouw B,Martin K,Matsumoto RR,Coop A

更新日期：2013-12-15 00:00:00