Eicosapentaenoic-acid-derived isoprostanes: synthesis and discovery of two major isoprostanes.

abstract：:We report the first synthesis of the C-terminally spermine-conjugated stapled peptide-based inhibitors of the p53-Mdm2 interaction. Subsequent biological, biophysical and cellular uptake assays with the spermine-conjugated stapled peptides revealed that spermine conjugation minimally affects biological activity while ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Muppidi A,Li X,Chen J,Lin Q

更新日期：2011-12-15 00:00:00

abstract：:Fast atom bombardment mass spectrometry that can directly analyze lysophospholipids was used to quantitatively determine the kinetics of phospholipase A2. This method is 1250 times more sensitive than the colorimetric assay. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Isomura S,Ito K,Haruna M

更新日期：1999-02-08 00:00:00

abstract：:A series of pyrazinones were prepared and evaluated as potential CRF(1)R PET imaging agents. Optimization of their CRF(1)R binding potencies and octanol-phosphate buffer phase distribution coefficients are discussed herein. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Denhart DJ,Zuev D,Ditta JL,Hartz RA,Ahuja VT,Mattson RJ,Huang H,Mattson GK,Zueva L,Nielsen JM,Kozlowski ES,Lodge NJ,Bronson JJ,Macor JE

更新日期：2013-04-01 00:00:00

abstract：:Nitric oxide (NO), a mediator of various physiological and pathophysiological processes, is synthesized by three isozymes of nitric oxide synthase (NOS). Potential candidate clinical drugs should be devoid of inhibitory activity against endothelial NOS (eNOS), since eNOS plays an important role in maintaining normal b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Le Bourdonnec B,Leister LK,Ajello CA,Cassel JA,Seida PR,O'Hare H,Gu M,Chu GH,Tuthill PA,DeHaven RN,Dolle RE

更新日期：2008-01-01 00:00:00

abstract：:A series of 114 SIRT inhibitor candidates was assembled using 'click chemistry', by reacting two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in the presence of Cu(I) catalyst. Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tatum PR,Sawada H,Ota Y,Itoh Y,Zhan P,Ieda N,Nakagawa H,Miyata N,Suzuki T

更新日期：2014-04-15 00:00:00

abstract：:Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Stark H,Ligneau X,Sadek B,Ganellin CR,Arrang JM,Schwartz JC,Schunack W

更新日期：2000-10-16 00:00:00

abstract：:Several boronic acids were screened for their ability to bind to diols. 3-methoxycarbonyl-5-nitrophenyl boronic acid bound to both a catechol dye as well as fructose with a comparable affinity to that of an ortho-methylamino substituted boronic acid. This work suggests a greater role for appropriately functionalized e...

journal_title：Bioorganic & medicinal chemistry letters

authors： Mulla HR,Agard NJ,Basu A

更新日期：2004-01-05 00:00:00

abstract：:We have synthesized 3 analogs of the dopamine D2 receptor (D2 DR) antagonist spiperone that can be conjugated to streptavidin-coated quantum dots via a pegylated biotin derivative. Using fluorescent imaging we demonstrate that substitution on the spiro position is tolerated, whilst the length and rigidity of a spacer ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tomlinson ID,Kovtun O,Crescentini TM,Rosenthal SJ

更新日期：2019-04-15 00:00:00

abstract：:In this study, we synthesized an Azo-py phosphoramidite, featuring azobenzene and pyrene units, as a novel fluorescent and isomeric (trans- and cis-azobenzene units) material, which we incorporated in an i-motif DNA sequence. We then monitored the structural dynamics and changes in fluorescence as the modified DNA seq...

journal_title：Bioorganic & medicinal chemistry letters

authors： Joo HN,Van Thi Nguyen T,Chae HK,Seo YJ

更新日期：2017-06-01 00:00:00

abstract：:The SAR studies to optimise both potency and rate of clearance in the rat for a series of pyrimidine and pyridine based VLA-4 antagonists are described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Porter JR,Archibald SC,Brown JA,Childs K,Critchley D,Head JC,Hutchinson B,Parton TA,Robinson MK,Shock A,Warrellow GJ,Zomaya A

更新日期：2002-06-17 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：: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：:Pretomanid (PA-824) is an important nitroimidazole antitubercular agent in late stage clinical trials. However, pretomanid is limited by poor solubility and high protein binding, which presents opportunities for improvement in its physiochemical properties. Conversely, the oxazolidinone linezolid has excellent physico...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rakesh,Bruhn DF,Scherman MS,Singh AP,Yang L,Liu J,Lenaerts AJ,Lee RE

更新日期：2016-01-15 00:00:00

abstract：:A catalyst-free synthesis of 6,9-dihydro-[1,3]dioxolo[4,5-g]thieno[3,4-b]quinolin-8(5H)-ones as novel analogues of podophyllotoxins was developed by a three-component reaction of aldehydes, ethyl 2,4-dioxotetrahydrothiophene-3-carboxylate and 3,4-(methylenedioxy)aniline. This methodology not only provides new chemical...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li T,Lu T,Yu C,Yao C

更新日期：2015-04-01 00:00:00

abstract：:Two thermostable α-carbonic anhydrases (α-CAs) isolated from thermophilic Sulfurihydrogenibium spp., namely SspCA (from S. yellowstonensis) and SazCA (from S. azorense), were shown in a previous work to possess interesting complementary properties. SspCA was shown to have an exceptional thermal stability, whereas SazC...

journal_title：Bioorganic & medicinal chemistry letters

authors： De Simone G,Monti SM,Alterio V,Buonanno M,De Luca V,Rossi M,Carginale V,Supuran CT,Capasso C,Di Fiore A

更新日期：2015-05-01 00:00:00

abstract：:The glutamine transporter ASCT2 has been identified as a promising target to inhibit rapid growth of cancer cells. However, ASCT2 pharmacology is not well established. In this report, we performed a systematic structure activity analysis of a series of substituted benzylproline derivatives. Substitutions on the phenyl...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh K,Tanui R,Gameiro A,Eisenberg G,Colas C,Schlessinger A,Grewer C

更新日期：2017-02-01 00:00:00

abstract：:Herein we describe the discovery of a novel series of ATP competitive B-Raf inhibitors via structure based drug design (SBDD). These pyridopyrimidin-7-one based inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimization led to the identification of compound 17, a potent, selective ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ren L,Ahrendt KA,Grina J,Laird ER,Buckmelter AJ,Hansen JD,Newhouse B,Moreno D,Wenglowsky S,Dinkel V,Gloor SL,Hastings G,Rana S,Rasor K,Risom T,Sturgis HL,Voegtli WC,Mathieu S

更新日期：2012-05-15 00:00:00

abstract：:A series of anilinonicotinyl linked pyrazolo[1,5-a]pyrimidine conjugates (6a-x) were synthesized and evaluated for their antiproliferative activity. Some of these conjugates exhibited promising cytotoxic effects in the MCF-7 cell line and among these 6a and 6c exhibited significant effects, apart from G2/M cell cycle ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kamal A,Faazil S,Hussaini SM,Ramaiah MJ,Balakrishna M,Patel N,Pushpavalli SN,Pal-Bhadra M

更新日期：2016-04-15 00:00:00

abstract：:To identify small molecule inhibitors of TNF-α, bioassay- and LC-MS-guided chemical investigation on EtOAc extract of Pseudomonas aeruginosa ABS-36 culture broth (EEPA) was performed, which yielded four proline-based cyclic dipeptides, cyclo(Gly-l-Pro) (1), cyclo(l-Pro-l-Phe) (2), cyclo(trans-4-hydroxy-l-Pro-l-Phe) (3...

journal_title：Bioorganic & medicinal chemistry letters

authors： Khan R,Basha A,Goverdhanam R,Rao PC,Tanemura Y,Fujimoto Y,Begum AS

更新日期：2015-12-15 00:00:00

abstract：:A series of 2-phenyl- or 3-phenyl piperazines, structurally related to DM235 and DM232, two potent nootropic agents, have been prepared and tested in the mouse passive-avoidance test, to assess their ability to revert scopolamine-induced amnesia. Although the newly synthesized molecules were less potent than the paren...

journal_title：Bioorganic & medicinal chemistry letters

authors： Guandalini L,Martino MV,Di Cesare Mannelli L,Bartolucci G,Melani F,Malik R,Dei S,Floriddia E,Manetti D,Orlandi F,Teodori E,Ghelardini C,Romanelli MN

更新日期：2015-04-15 00:00:00

abstract：:In an effort to expand the spectrum of antibacterial activity associated with piperidin-4-one derivatives, we have synthesized two series of 3-carboxyethyl-2,6-diphenyl-4-hydroxy-Delta(3)-tetrahydropyridine derivatives bearing diversified heterocyclic and aromatic systems at the nitrogen atom through acetyl (6-18) and...

journal_title：Bioorganic & medicinal chemistry letters

authors： Aridoss G,Amirthaganesan S,Jeong YT

更新日期：2010-04-01 00:00:00

abstract：:A series of Sordarin derivatives bearing alkyl substituted tetrahydrofuran rings fused to C3'-C4' bond of the sugar moiety have been prepared and their antifungal properties evaluated. Most of them show remarkable antifungal activity against Candida spp and Cryptococcus neoformans. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bueno JM,Chicharro J,Fiandor JM,Gómez de las Heras F,Huss S

更新日期：2002-07-08 00:00:00

abstract：:Small molecule JAK inhibitors have been demonstrated efficacy in rheumatoid arthritis, inflammatory bowel disease, and psoriasis with the approval of several drugs. Aiming to develop potent JAK1/2 inhibitors, two series of triazolo [1,5-a] pyridine derivatives were designed and synthesized by various strategies. The p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lu K,Wu W,Zhang C,Liu Z,Xiao B,Yuan Z,Li A,Chen D,Zhai X,Jiang Y

更新日期：2020-07-15 00:00:00

abstract：:The rational design, syntheses and evaluation of potent sulfonamidopyrrolidin-2-one-based factor Xa inhibitors incorporating aminoindane and phenylpyrrolidine P4 motifs are described. These series delivered highly potent anticoagulant compounds with excellent oral pharmacokinetic profiles; however, significant time de...

journal_title：Bioorganic & medicinal chemistry letters

authors： Young RJ,Adams C,Blows M,Brown D,Burns-Kurtis CL,Chan C,Chaudry L,Convery MA,Davies DE,Exall AM,Foster G,Harling JD,Hortense E,Irvine S,Irving WR,Jackson S,Kleanthous S,Pateman AJ,Patikis AN,Roethka TJ,Senger S,

更新日期：2011-03-15 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：: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：:N-13C-methyl-deoxynojirimycin was synthesized and used in isotope-edited NMR studies to probe the binding site of an alpha-glucosidase. Results from this analysis led to the design and preparation of a novel alpha-glucosidase inhibitor, N-glycyl deoxynojirimycin. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hines JV,Chang H,Gerdeman MS,Warn DE

更新日期：1999-05-03 00:00:00

abstract：:A new halicyclamine derivative, tetradehydrohalicyclamine B (1), was isolated from the marine sponge Acanthostrongylophora ingens, along with halicyclamine B (2) as proteasome inhibitors. Compound 1 is the second example found to have a pyridinium ring in the halicyclamine family. Although the relative configuration o...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kato H,El-Desoky AH,Takeishi Y,Nehira T,Angkouw ED,Mangindaan REP,de Voogd NJ,Tsukamoto S

更新日期：2019-01-01 00:00:00

abstract：:In an effort to better understand the conformational preferences that inform the biological activity of naltrexone and related naltrexol derivatives, a new synthesis of the restricted analog 3-OBn-6β,14-epoxymorphinan 4 is described. 4 was synthesized starting from naltrexone in 50% overall yield, proceeding through t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Martin DJ,FitzMorris PE,Li B,Ayestas M,Sally EJ,Dersch CM,Rothman RB,Deveau AM

更新日期：2012-11-15 00:00:00

abstract：:A series of novel 1,3-benzodiazapine based D1 antagonists was designed according to the understanding of pharmacophore models derived from SCH 23390 (1b), a potent and selective D1 antagonist. The new design features an achiral cyclic-amidine that maintains desired basicity. Solid phase synthesis was developed for SAR...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu Z,Sun ZY,Ye Y,McKittrick B,Greenlee W,Czarniecki M,Fawzi A,Zhang H,Lachowicz JE

更新日期：2009-09-01 00:00:00