Molecular design, chemical synthesis, and evaluation of cytosine-carbohydrate hybrids for selective recognition of a single guanine bulged duplex DNA.

abstract：:A novel series of benzenesulfonamides that contain ferrocenyl or ruthenocenyl moieties were synthesized and investigated for their ability to inhibit the enzymatic activity of physiologically relevant carbonic anhydrase (CA) isozymes: hCA I, II and tumour-associated IX (h=human). This manuscript describes the regiosel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Salmon AJ,Williams ML,Innocenti A,Vullo D,Supuran CT,Poulsen SA

更新日期：2007-09-15 00:00:00

abstract：:Sustained proliferative capacity and gene dysregulation are hallmarks of cancer. In mammalian cells, cyclin-dependent kinases (CDKs) control critical cell cycle checkpoints and key transcriptional events in response to extracellular and intracellular signals leading to proliferation. Significant clinical activity for ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sánchez-Martínez C,Lallena MJ,Sanfeliciano SG,de Dios A

更新日期：2019-10-15 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：:Starting with a micromolar lead identified from high-throughput screening, a series of pyrazoles were discovered with significantly improved potency on bacterial methionyl-tRNA synthetase and selectivity over human methionyl-tRNA synthetase. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Finn J,Mattia K,Morytko M,Ram S,Yang Y,Wu X,Mak E,Gallant P,Keith D

更新日期：2003-07-07 00:00:00

abstract：:A new series of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridine compounds have been discovered as potent anaplastic lymphoma kinase (ALK) inhibitors. The 4-hydroxyphenyl in the 6-position of 1H-pyrazolo[3,4-b]pyridine were crucial and a fluorine atom substitution could give promising inhibitory activity. The IC50 of compound 9v...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen C,Pan P,Deng Z,Wang D,Wu Q,Xu L,Hou T,Cui S

更新日期：2019-04-01 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：: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：:Next generation NNRTIs are sought which possess both broad spectrum antiviral activity against key mutant strains and a high genetic barrier to the selection of new mutant viral strains. Pyridones were evaluated as an acyclic conformational constraint to replace the aryl ether core of MK-4965 (1) and the more rigid in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gomez R,Jolly S,Williams T,Tucker T,Tynebor R,Vacca J,McGaughey G,Lai MT,Felock P,Munshi V,DeStefano D,Touch S,Miller M,Yan Y,Sanchez R,Liang Y,Paton B,Wan BL,Anthony N

更新日期：2011-12-15 00:00:00

abstract：:Accumulation of beta-amyloid (Abeta), produced by the proteolytic cleavage of amyloid precursor protein (APP) by beta- and gamma-secretase, is widely believed to be associated with Alzheimer's disease (AD). Research around the high-throughput screening hit (S)-4-chlorophenylsulfonyl isoleucinol led to the identificati...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cole DC,Stock JR,Kreft AF,Antane M,Aschmies SH,Atchison KP,Casebier DS,Comery TA,Diamantidis G,Ellingboe JW,Harrison BL,Hu Y,Jin M,Kubrak DM,Lu P,Mann CW,Martone RL,Moore WJ,Oganesian A,Riddell DR,Sonnenberg-Reine

更新日期：2009-02-01 00:00:00

abstract：:A series of 1-(quinoliloxypropyl)-4-aryl-piperazines has been synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced mesh climbing and stereotypic behaviour in mice. The 8-hydroxyquinoline ether derivative 14 has emerged as an important lead compound showing a potenti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bali A,Malhotra S,Dhir H,Kumar A,Sharma A

更新日期：2009-06-01 00:00:00

abstract：:Human isoprenylcysteine carboxyl methyltransferase (hIcmt) is a promising anticancer target as it is important for the post-translational modification of oncogenic Ras proteins. We herein report the synthesis and biochemical activity of 41 farnesyl-cysteine based analogs versus hIcmt. We have demonstrated that the ami...

journal_title：Bioorganic & medicinal chemistry letters

authors： Majmudar JD,Hahne K,Hrycyna CA,Gibbs RA

更新日期：2011-05-01 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：:Coxsackievirus and related enteroviruses are important human pathogens that cause various diseases with clinical manifestations ranging from trivial flu-like syndromes to dangerous or even fatal diseases such as myocarditis, meningitis and encephalitis. Here, we report on our continuous SAR study focused on 9-(bicyclo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sála M,De Palma AM,Hřebabecký H,Dejmek M,Dračínský M,Leyssen P,Neyts J,Mertlíková-Kaiserová H,Nencka R

更新日期：2011-07-15 00:00:00

abstract：:We expand the structural requirements and structure-activity relationship of a novel class of non-peptidic aryl-based thrombin inhibitors through exploration of the S1 specificity pocket of thrombin using flexible and constrained amidines. The most active compound of this class is 11 with Ki = 69 nM, which is ca. 15-f...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lu T,Tomczuk B,Bone R,Murphy L,Salemme FR,Soll RM

更新日期：2000-01-03 00:00:00

abstract：:We disclose a new compound class of potent and selective alpha-1A adrenergic receptor antagonists exemplified by the geminally, disubstituted cyclic imide 7. The optimization of lead compounds resulting in the cyclic imide motif is highlighted. The results of in vitro and in vivo studies of selected compounds are pres...

journal_title：Bioorganic & medicinal chemistry letters

authors： DiPardo RM,Patane MA,Newton RC,Price R,Broten TP,Chang RS,Ransom RW,Di Salvo J,Freidinger RM,Bock MG

更新日期：2001-07-23 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：:Triple-negative breast cancer (TNBC) has been reported to be correlated with high expression of proliferation markers as well as constitutive activation of metastasis-relevant signaling pathways. For many years, breast cancer researchers have been investigating specific and effective methods to treat or to control the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen L,Long C,Nguyen J,Kumar D,Lee J

更新日期：2018-02-01 00:00:00

abstract：:The design and synthesis of a new series of c-Jun N-terminal kinase-3 (JNK3) inhibitors with selectivity against JNK1 are reported. The novel series of substituted 2'-anilino-4,4'-bipyridines were designed based on a combination of hits from high throughput screening and X-ray crystal structure information of compound...

journal_title：Bioorganic & medicinal chemistry letters

authors： Swahn BM,Xue Y,Arzel E,Kallin E,Magnus A,Plobeck N,Viklund J

更新日期：2006-03-01 00:00:00

abstract：:Novel imidazole frameworks have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Nitrile 28 possessed attractive CNS drug-like properties with good membrane permeability and no P-pg mediated efflux. 28...

journal_title：Bioorganic & medicinal chemistry letters

authors： Whitlock GA,Brennan PE,Roberts LR,Stobie A

更新日期：2009-06-01 00:00:00

abstract：:Cyclin-dependent kinase 5 (CDK5) is a serine-threonine protein kinase that plays a significant role in neuronal development. In association with p25, CDK5 abnormally phosphorylates a number of cellular targets involved in neurodegenerative disorders. Using active site homology and previous structure-activity relations...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kaller MR,Zhong W,Henley C,Magal E,Nguyen T,Powers D,Rzasa RM,Wang W,Xiong X,Norman MH

更新日期：2009-12-01 00:00:00

abstract：:Structure-based drug design was exploited in the synthesis of 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group with acyclic tertiary amide termini. Optimized hydrophobic contacts of one amide substituent in P4 were complemented by hydrophobici...

journal_title：Bioorganic & medicinal chemistry letters

authors： Young RJ,Campbell M,Borthwick AD,Brown D,Burns-Kurtis CL,Chan C,Convery MA,Crowe MC,Dayal S,Diallo H,Kelly HA,King NP,Kleanthous S,Mason AM,Mordaunt JE,Patel C,Pateman AJ,Senger S,Shah GP,Smith PW,Watson NS,West

更新日期：2006-12-01 00:00:00

abstract：:The naturally occurring aporphine alkaloid nantenine, has been shown to antagonize behavioral and physiological effects of MDMA in mice. We have synthesized (+/-)-nantenine via an oxidative cyclization reaction with PIFA and evaluated its binding profile against a panel of CNS targets. To begin to understand the impor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Legendre O,Pecic S,Chaudhary S,Zimmerman SM,Fantegrossi WE,Harding WW

更新日期：2010-01-15 00:00:00

abstract：:Modification of the major insecticide fipronil (1) by replacing three pyrazole substituents (hydrogen for both cyano and amino and trifluoromethyldiazirinyl for trifluoromethylsulfinyl) gives a candidate photoaffinity probe (3) of high potency (IC(50) 2-28 nM) in blocking the chloride channel of Drosophila and human b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sirisoma NS,Ratra GS,Tomizawa M,Casida JE

更新日期：2001-11-19 00:00:00

abstract：:N(tau)-Aryl-histidine derivatives were synthesized using a modified one-step Cu-catalyzed coupling of aryl halides and N-acetylhistidine methyl ester. The latter is much less reactive than imidazole toward aryl halides. p-Chloroiodobenzene coupled with iodine displacement only, whereas m- and p-bromoiodobenzene both g...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yue W,Lewis SI,Koen YM,Hanzlik RP

更新日期：2004-04-05 00:00:00

abstract：:Albocycline (ALB) is a unique macrolactone natural product with potent, narrow-spectrum activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate (VISA), and vancomycin-resistant S. aureus (VRSA) strains (MIC = 0.5-1.0 μg/mL). Described herein is the synthesis and evaluation of a nov...

journal_title：Bioorganic & medicinal chemistry letters

authors： Daher SS,Franklin KP,Scherzi T,Dunman PM,Andrade RB

更新日期：2020-11-01 00:00:00

abstract：:5-Aminolaevulinic acid (ALA) prodrugs have been widely used in photodynamic therapy (PDT) as precursors to the natural photosensitizer, protoporphyrin IX (PpIX). The main disadvantage of this therapy is that ALA is poorly absorbed by cells due to its high hydrophilicity. In order to improve the therapeutical effect an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu CF,Battah S,Kong X,Reeder BJ,Hider RC,Zhou T

更新日期：2015-02-01 00:00:00

abstract：:A novel diamino-substituted hypocrellin derived from hypocrellin B (HB) was synthesized by a mild method. The red absorption of the resulting product was significantly enhanced relative to the parent hypocrellins and any other hypocrellin derivatives, and the active oxygen species generating abilities were enhanced di...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu S,Chen S,Zhang M,Shen T

更新日期：2004-03-22 00:00:00

abstract：:Structures containing the (R)-3-amino-3-methyl piperidine unit as a new pharmacophore moiety have been shown to possess moderate inhibitory activity for DPP-4 with good pharmacokinetics profile. One of these compounds was found to have good oral bioavailability and PK/PD profile in ZF-rat. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nishio Y,Kimura H,Tosaki S,Sugaru E,Sakai M,Horiguchi M,Masui Y,Ono M,Nakagawa T,Nakahira H

更新日期：2010-12-15 00:00:00

abstract：:A novel class of HCV NS5B RNA dependent RNA polymerase inhibitors containing 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H-pyrano[3,4-b]benzofuran scaffolds were designed and synthesized. Optimization of the alkyl substituent in the pyran ring showed preference for an n-propyl group, while 5,8-disubsti...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gopalsamy A,Aplasca A,Ciszewski G,Park K,Ellingboe JW,Orlowski M,Feld B,Howe AY

更新日期：2006-01-15 00:00:00

abstract：:A series of alpha(v)beta(3) antagonists based on a thiophene scaffold were synthesized via two routes and evaluated for in vitro biological activity. We have identified several structurally similar antagonists with different selectivities towards alpha(IIb)beta(3), alpha(v)beta(5) and alpha(5)beta(1) at the cellular l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bubenik M,Meerovitch K,Bergeron F,Attardo G,Chan L

更新日期：2003-02-10 00:00:00