Enzymatic syntheses of 6-(4H-selenolo[3,2-b]pyrrolyl)-L-alanine, 4-(6H-selenolo[2,3-b]pyrrolyl)-L-alanine, and 6-(4H-furo[3,2-b]pyrrolyl-L-alanine.

abstract：:Tylophorine B exhibits pronounced cytotoxicity and antitumor activity. In order to survey the structure selectivity to DNA afforded by tylophorine B, we have synthesized a variety of duplex, bulge- and hairpin-containing oligodeoxyribonucleotides. Their binding to tylophorine B has been assayed by fluorescence spectro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xi Z,Zhang R,Yu Z,Ouyang D,Huang R

更新日期：2005-05-16 00:00:00

abstract：:Inhibition of Eg5 represents a novel approach for the treatment of cancer. Here, we report the synthesis and structure-activity relationship of S-trityl-L-cysteine (STLC) derivatives as Eg5 inhibitors. Some of these derivatives such as 4f demonstrated enhanced inhibitory activity against Eg5 and induced mitotic arrest...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ogo N,Oishi S,Matsuno K,Sawada J,Fujii N,Asai A

更新日期：2007-07-15 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 use of doxorubicin (DOX) in the treatment of solid tumors is limited by cardiotoxicity essentially due to oxidative stress generation. The aim of this study was to identify coumarin derivatives displaying a protective antioxidant activity without affecting DOX antitumoral efficiency. A set of eighteen coumarinic d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Beillerot A,Domínguez JC,Kirsch G,Bagrel D

更新日期：2008-02-01 00:00:00

abstract：:Cross-linkage of the branches of poly(ethylenimine) (PEI) suppresses flexibility of the polymer as revealed by decreased affinity of the amino groups on PEI backbone towards proton or Ni(II) ion. The cross-linkage improves ability of the PEI derivative equipped with beta-cyclodextrin to deacylate an ester containing t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Suh J,Noh YS

更新日期：1998-06-02 00:00:00

abstract：:S1P receptors (S1PR1-5) are a group of GPCRs activated by a high affinity binding with S1P that have important roles in the regulation of the immune system. A potent S1PR agonist FTY720 is an immunomodulator used to treat multiple sclerosis and several 'second generation' drugs are under clinical development. Subtype-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hur W,Rosen H,Gray NS

更新日期：2017-01-01 00:00:00

abstract：:Herein we report 6-ethoxy-6-oxo-5-(2-phenylhydrazono) hexanoic acid and 3-(2-carboxyethyl)-1H-indole-2-carboxylic acid derivatives as synthetically accessible leads for human kynurenine aminotransferase-I (KAT-I) inhibitors. In total, 12 compounds were synthesized and their biological activities were determined using ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Akladios FN,Nadvi NA,Park J,Hanrahan JR,Kapoor V,Gorrell MD,Church WB

更新日期：2012-02-15 00:00:00

abstract：:Several imidazole-based cyclohexyl amides were identified as potent CB-1 antagonists, but they exhibited poor oral exposure in rodents. Incorporation of a hydroxyl moiety on the cyclohexyl ring provided a dramatic improvement in oral exposure, together with a ca. 10-fold decrease in potency. Further optimization provi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Smith RA,Fathi Z,Achebe F,Akuche C,Brown SE,Choi S,Fan J,Jenkins S,Kluender HC,Konkar A,Lavoie R,Mays R,Natoli J,O'Connor SJ,Ortiz AA,Su N,Taing C,Tomlinson S,Tritto T,Wang G,Wirtz SN,Wong W,Yang XF,Ying S,

更新日期：2007-05-15 00:00:00

abstract：:Coibamide A is a highly potent antiproliferative cyclic depsipeptide, which was originally isolated from a Panamanian marine cyanobacterium. In this study, the synthesis of coibamide A has been investigated using Fmoc-based solid-phase peptide synthesis followed by the cleavage of the resulting linear peptide from the...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nabika R,Suyama TL,Hau AM,Misu R,Ohno H,Ishmael JE,McPhail KL,Oishi S,Fujii N

更新日期：2015-01-15 00:00:00

abstract：:SB-216763 is a novel, potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor with an IC(50) value of 34 nM. [(11)C]SB-216763 (3-(2,4-dichlorophenyl)-4-(1-[(11)C]methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione), a new potential PET agent for imaging of GSK-3, was first designed and synthesized in 20-30% decay cor...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang M,Gao M,Miller KD,Sledge GW,Hutchins GD,Zheng QH

更新日期：2011-01-01 00:00:00

abstract：:Non peptide products have been found to show nanomolar binding and functional affinities at the human tachykinin NK-2 receptor. The new antagonists do not possess stereogenic centers and their thermal behaviour in solution is featured by a peculiar set of conformational stereoisomers. A macroscopic viewpoint is prefer...

journal_title：Bioorganic & medicinal chemistry letters

authors： Altamura M,Canfarini F,Catalioto RM,Guidi A,Pasqui F,Renzetti AR,Triolo A,Maggi CA

更新日期：2002-10-21 00:00:00

abstract：:Three new (1-3) and one known (4) bioactive terpenoids were isolated from the seeds of Silybum marianum based on the investigation to get new NO inhibitors. Their structures were determined by extensive NMR (1D and 2D NMR) and MS spectroscopic data, and the absolute configurations were identified by experimental and c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qin NB,Li SG,Yang XY,Gong C,Zhang XY,Wang J,Li DH,Guo YQ,Li ZL,Hua HM

更新日期：2017-05-15 00:00:00

abstract：:In a recent paper, [Arienti, K. L.; Brunmark, A.; Axe, F. U.; McClure, K. M.; Lee, A.; Blevitt, J.; Neff, D. K.; Huang, L.; Crawford, S.; Chennagiri, R. P.; Karlsson, L.; Brietenbucher, J. G. J. Med. Chem.2005, 48, 1873], we described the discovery of a class of benzimidazole chk2 kinase inhibitors, exemplified by com...

journal_title：Bioorganic & medicinal chemistry letters

authors： McClure KJ,Huang L,Arienti KL,Axe FU,Brunmark A,Blevitt J,Breitenbucher JG

更新日期：2006-04-01 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：:To design artificial restriction enzymes, synthetic catalytic centers that effectively hydrolyze linear double-stranded polydeoxyribonucleotides are needed. The Co(III) complex of cyclen (CoCyc) attached to polystyrene derivatives hydrolyzes linearized pUC18 DNA with half-lives as short as 30 min at 25 degrees C. The ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jeung CS,Song JB,Kim YH,Suh J

更新日期：2001-12-03 00:00:00

abstract：:The efflux transporter protein P-glycoprotein (P-gp) is capable of affecting the central distribution of diverse neurotherapeutics, including opioid analgesics, through their active removal from the brain. P-gp located at the blood brain barrier has been implicated in the development of tolerance to opioids and demons...

journal_title：Bioorganic & medicinal chemistry letters

authors： Metcalf MD,Rosicky AD,Hassan HE,Eddington ND,Coop A,Cunningham CW,Mercer SL

更新日期：2014-08-01 00:00:00

abstract：:High potency pyrazole-based noncovalent inhibitors of human cathepsin S (CatS) were developed by modification of the benzo-fused 5-membered ring heterocycles found in earlier series of CatS inhibitors. Although substitutions on this heterocyclic framework had a moderate impact on enzymatic potency, dramatic effects on...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wei J,Pio BA,Cai H,Meduna SP,Sun S,Gu Y,Jiang W,Thurmond RL,Karlsson L,Edwards JP

更新日期：2007-10-15 00:00:00

abstract：:A series of steroid-polyamine conjugates were synthesized and evaluated for their antimicrobial activity. This study was focused on the effect of stereochemistry at the C-3 and C-5 of steroids and types of polyamine at C-3 on activity against various human pathogens. All the conjugates exhibited strong antimicrobial a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kim HS,Khan SN,Jadhav JR,Jeong JW,Jung K,Kwak JH

更新日期：2011-07-01 00:00:00

abstract：:HER2 overexpression is associated with aggressive breast cancer with high recurrence rate and poor patient prognosis. Treatment of HER2 overexpressing patients with the HER2 targeting therapy trastuzumab results in acquired resistance within a year. The HER2/EGFR dual kinase inhibitor lapatinib was shown to inhibit so...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sridhar J,Sfondouris ME,Bratton MR,Nguyen TL,Townley I,Klein Stevens CL,Jones FE

更新日期：2014-01-01 00:00:00

abstract：:A novel dendritic molecule with nine chlorambucil (CBL) residues on the surface and a maleimide moiety at the core terminus was synthesized using a convergent synthetic methodology. This molecule is ready for attachment to single-chain Fv antibodies (scFvs) to form antibody-multidrug immunoconjugates in an effort to s...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sun C,Wirsching P,Janda KD

更新日期：2002-08-19 00:00:00

abstract：:In search for a new antibacterial agent with improved antimicrobial spectrum and potency, we designed and synthesized a series of novel 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones 7a-h by convergent synthesis approach. All the synthesized compounds were assayed for their in-vitro antibacteri...

journal_title：Bioorganic & medicinal chemistry letters

authors： Diwakar SD,Bhagwat SS,Shingare MS,Gill CH

更新日期：2008-08-15 00:00:00

abstract：:Serine/threonine kinase PIM3 is a potential therapeutic target for pancreatic cancer. Here, we describe the evolution of our previous PIM1 inhibitor 1 into PIM3 inhibitor 11 guided by use of the crystal structure of PIM1 as a surrogate to provide a basis for rational modification. Compound 11 potently inhibits PIM3 ki...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nakano H,Hasegawa T,Saito N,Furukawa K,Mukaida N,Kojima H,Okabe T,Nagano T

更新日期：2015-12-15 00:00:00

abstract：:A number of molecular recognition features have been exploited in structure-based design of selective Cathepsin inhibitors. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bethel PA,Gerhardt S,Jones EV,Kenny PW,Karoutchi GI,Morley AD,Oldham K,Rankine N,Augustin M,Krapp S,Simader H,Steinbacher S

更新日期：2009-08-15 00:00:00

abstract：:Analysis of the enantiomers of rosiglitazone in a PPAR gamma binding assay suggests that the (S)-(-)-isomer is responsible for the antidiabetic activity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parks DJ,Tomkinson NC,Villeneuve MS,Blanchard SG,Willson TM

更新日期：1998-12-15 00:00:00

abstract：:This communication describes the high-throughput screen of a diverse library of 50,000 small molecules against Escherichia coli dihydrofolate reductase to detect inhibitors. Sixty-two compounds were identified as having significant inhibitory activity against the enzyme. Secondary screening of these revealed twelve mo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zolli-Juran M,Cechetto JD,Hartlen R,Daigle DM,Brown ED

更新日期：2003-08-04 00:00:00

abstract：:The alpha7 subtype of the nicotinic acetylcholine receptor (nAChR) is the target of studies aimed at identifying features that will lead to the development of selective therapeutics. Five arylidine anabaseines, three with pyridine rings and two with the pyrrole rings, were synthesized in 35-65% yield via aldol condens...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang J,Papke RL,Horenstein NA

更新日期：2009-01-15 00:00:00

abstract：:Macromolecular chelators have potential applications in the medical area, for instance, in treatment of iron overload-related disorders and in the treatment of external infections. In this investigation, several novel iron(III)-selective hydroxypyridinone hexadentate-terminated first and second generation dendrimeric ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhou T,Chen K,Kong LM,Liu MS,Ma YM,Xie YY,Hider RC

更新日期：2018-08-01 00:00:00

abstract：:A new immobilization chemistry for covalent attachment of phosphorylated oligonucleotides on epoxy-activated glass surface via opening of oxirane ring is described. The proposed strategy results in excellent immobilization efficiency, spot homogeneity, and morphology. The constructed microarray was successfully demons...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mahajan S,Kumar P,Gupta KC

更新日期：2006-11-01 00:00:00

abstract：:Cyclic phosphatidic acid (CPA) is a naturally occurring analog of lysophosphatidic acid (LPA) in which the sn-2 hydroxy group forms a five-membered ring with the sn-3 phosphate. Here, we describe the synthesis of R-3-CCPA and S-3-CCPA along with their pharmacological properties as inhibitors of lysophospholipase D/aut...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gupte R,Siddam A,Lu Y,Li W,Fujiwara Y,Panupinthu N,Pham TC,Baker DL,Parrill AL,Gotoh M,Murakami-Murofushi K,Kobayashi S,Mills GB,Tigyi G,Miller DD

更新日期：2010-12-15 00:00:00

abstract：:Kynurenine monooxygenase (KMO) is a potential drug target for treatment of neurodegenerative disorders such as Huntington's and Alzheimer's diseases. We have evaluated substituted kynurenines as substrates or inhibitors of KMO from Cytophaga hutchinsonii. Kynurenines substituted with a halogen at the 5-position are ex...

journal_title：Bioorganic & medicinal chemistry letters

authors： Phillips RS,Anderson AD,Gentry HG,Güner OF,Bowen JP

更新日期：2017-04-15 00:00:00