16Beta-hydroxy-5alpha-cholestane-3,6-dione, a novel cytotoxic oxysterol from the red alga Jania rubens.

abstract：:N-Phthaloyl 3-amino-3-arylpropionic acid analogs of thalidomide that are potent inhibitors of tumor necrosis factor-alpha are reported. These compounds were found to be potent inhibitors of phosphodiesterase 4. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Muller GW,Shire MG,Wong LM,Corral LG,Patterson RT,Chen Y,Stirling DI

更新日期：1998-10-06 00:00:00

abstract：:Taspase1 is a threonine protease responsible for cleaving MLL (Mixed-Lineage Leukemia) to achieve proper HOX gene expression. Subsequent studies identified additional Taspase1 substrates including Transcription Factor IIA (TFIIA) and Drosophila HCF. Taspase1 is essential for cell proliferation and is overexpressed in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JT,Chen DY,Yang Z,Ramos AD,Hsieh JJ,Bogyo M

更新日期：2009-09-01 00:00:00

abstract：:Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic beta-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARalpha, PPARgamma and PPARbeta/(d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parmenon C,Guillard J,Caignard DH,Hennuyer N,Staels B,Audinot-Bouchez V,Boutin JA,Dacquet C,Ktorza A,Viaud-Massuard MC

更新日期：2008-03-01 00:00:00

abstract：:A novel series of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists are described. The series was designed to address the suboptimal PK (pharmacokinetic) and off-target profile of a class of N-aryl-benzo-[1,4]-oxazepine-4-carboxamides, represented by 1, that were identified from a high-throughput screen of the Me...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wilson JE,Kurukulasuriya R,Sinz C,Lombardo M,Bender K,Parker D,Sherer EC,Costa M,Dingley K,Li X,Mitelman S,Tong S,Bugianesi R,Ehrhardt A,Priest B,Ratliff K,Ujjainwalla F,Nargund R,Hagmann WK,Edmondson S

更新日期：2016-06-15 00:00:00

abstract：:Benz[b]oxepines 4a-g and 12-oxobenzo[c]phenanthridines 5a-d were designed and synthesized as constrained forms of 3-arylisoquinolines through an intramolecular radical cyclization reaction. Radical cyclization of O-vinyl compounds preferentially led to the 7-endo-trig cyclization pathway to the benz[b]oxepines and 12-...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee SH,Van HT,Yang SH,Lee KT,Kwon Y,Cho WJ

更新日期：2009-05-01 00:00:00

abstract：:A verbenachalcone derivative was synthesized and shown to protect N2a cells from caspase induction caused by serum starvation and to enhance the effect of NGF on neurite outgrowth in PC12 cells. As an initial investigation of the compound's mechanism(s) of action, we performed differential gene expression profiling in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yeh LA,Padmanaban D,Ho P,Xing X,Rowley P,Morse LJ,Jensen RV,Cuny GD

更新日期：2005-02-15 00:00:00

abstract：:An imbalance between bone resorption by osteoclasts and bone formation by osteoblasts can cause bone loss and bone-related disease. In a previous search for natural products that increase osteogenic activity, we found that 5,6-dehydrokawain (1) from Alpinia zerumbet promotes osteoblastogenesis. In this study, we synth...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumagai M,Nishikawa K,Mishima T,Yoshida I,Ide M,Koizumi K,Nakamura M,Morimoto Y

更新日期：2017-06-01 00:00:00

abstract：:The structures of the uracil and thiouracils were examined using NMR spectroscopy and crystal structure data when available. The relationships between the extent of polarization and the C5-C6 bond length as well as the H5-H6 coupling constants were probed. It was found that the bond length and coupling constants corre...

journal_title：Bioorganic & medicinal chemistry letters

authors： Huang S,Gronert S,Wu W

更新日期：2011-11-01 00:00:00

abstract：:The study by the molecular orbital theory displayed that morphine and lysine make two types of the interactions between them: type (A) by three hydrogen bondings and type (B) by one hydrogen bonding accompanied with a proton transfer. The stabilization energies were 45.3 and 34.9 kcal/mol for type (A) and type (B), re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nakai S,Yoneda F

更新日期：2001-06-04 00:00:00

abstract：:Novel Leu-enkephalin (Leu-Enk) (1) analogs possessing various types of alpha-substituted serine instead of its glycine residue in the position 2 were synthesized via an efficient O,N-migration method. The binding characteristics of the synthetic analogs using Chinese hamster ovary (CHO) cells expressed cloned rat mu-,...

journal_title：Bioorganic & medicinal chemistry letters

authors： Horikawa M,Shigeri Y,Yumoto N,Yoshikawa S,Nakajima T,Ohfune Y

更新日期：1998-08-04 00:00:00

abstract：:Selective metabotropic glutamate receptor 2 (mGluR2) inhibitors have been demonstrated to show therapeutic effects by improving alleviating symptoms of schizophrenic patients in clinical studies. Herein we report the synthesis and preliminary evaluation of a 11C-labeled positron emission tomography (PET) tracer origin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kumata K,Zhang Y,Ogawa M,Kurihara Y,Mori W,Hu K,Fujinaga M,Nengaki N,Zhang MR

更新日期：2020-12-01 00:00:00

abstract：:The highly selective agonists of the A(3) adenosine receptor (AR), Cl-IB-MECA (2-chloro-N(6)-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine), and its 4'-thio analogue, were successfully converted into selective antagonists simply by appending a second N-methyl group on the 5'-uronamide position. The 2-chloro-5'-(N,N-d...

journal_title：Bioorganic & medicinal chemistry letters

authors： Gao ZG,Joshi BV,Klutz AM,Kim SK,Lee HW,Kim HO,Jeong LS,Jacobson KA

更新日期：2006-02-01 00:00:00

abstract：:Novel, low brain penetrant, orally bioavailable CB1 receptor agonists were designed starting from a mature lead series of potent brain penetrant CB1 receptor agonists. Increasing the calculated polar surface area was found to be a good strategy for reducing brain penetration whilst retaining drug-like properties. This...

journal_title：Bioorganic & medicinal chemistry letters

authors： Adam JM,Clark JK,Davies K,Everett K,Fields R,Francis S,Jeremiah F,Kiyoi T,Maidment M,Morrison A,Ratcliffe P,Prosser A,Schulz J,Wishart G,Baker J,Boyce S,Campbell R,Cottney JE,Deehan M,Martin I

更新日期：2012-04-15 00:00:00

abstract：:The stereospecific synthesis of two all-syn-EPA-derived isoprostanes (iPs), 5-epi-8,12-iso-iPF(3alpha)-VI 17 and 8,12-iso-iPF(3alpha)-VI 18, has been accomplished. These two synthetic probes have been used to discover and identify their presence in human urine. The eventual quantitative measurement of these two iPs ma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chang CT,Patel P,Kang N,Lawson JA,Song WL,Powell WS,FitzGerald GA,Rokach J

更新日期：2008-10-15 00:00:00

abstract：:Based on the favorable antiviral profiles of 4'-substituted nucleosides, novel 1-(2'-deoxy-2'-fluoro-4'-C-ethynyl-beta-D-arabinofuranosyl)-uracil (1a), -thymine (1b), and -cytosine (2) analogs were synthesized. Compounds 1b and 2 exhibited potent anti-HIV-1 activity with IC(50) values of 86 and 1.34 nM, respectively, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang Q,Li Y,Song C,Qian K,Chen CH,Lee KH,Chang J

更新日期：2010-07-15 00:00:00

abstract：:Amiodarone (Cordarone, Wyeth-Ayerst Pharmaceuticals) is a clinically available drug used to treat a wide variety of cardiac arrhythmias. We report here the synthesis and characterization of a panel of potential amiodarone metabolites that have significant structural similarity to thyroid hormone and its metabolites th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Snead AN,Miyakawa M,Tan ES,Scanlan TS

更新日期：2008-11-15 00:00:00

abstract：:Two (99m)Tc/Re complexes based on flavone and aurone were tested as potential probes for imaging β-amyloid plaques using single photon emission computed tomography. Both (99m)Tc-labeled derivatives showed higher affinity for Aβ(1-42) aggregates than did (99m)Tc-BAT. In sections of brain tissue from an animal model of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ono M,Ikeoka R,Watanabe H,Kimura H,Fuchigami T,Haratake M,Saji H,Nakayama M

更新日期：2010-10-01 00:00:00

abstract：:A series of compounds originally derived from the vascular endothelial growth factor receptor tyrosine kinase inhibitor, SU5416, was synthesized and evaluated. The most potent compound in this series, compound 7, structurally resembles the potent anti-microtubule agent Combretastatin A-4, inhibited tubulin polymerizat...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li PK,Xiao Z,Hu Z,Pandit B,Sun Y,Sackett DL,Werbovetz K,Lewis A,Johnsamuel J

更新日期：2005-12-15 00:00:00

abstract：:Novel phenol bis-Mannich adducts were identified as IL-2 expression inhibitors in a T cell proliferation screening assay. Analogues of the lead compound were prepared through parallel synthesis and a highly selective IL-2 inhibitor was discovered that provided a suitable compound for further optimization. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Geng B,Fleming PR,Umlauf S,Lin A,Pallai PV

更新日期：2002-03-11 00:00:00

abstract：:In the past half century research efforts have defined a critical role for angiogenesis in tumor growth and metastasis. We previously reported that inhibition of a novel target, ENOX1, by a (Z)-2-benzylindol-3-ylmethylene) quinuclidin-3-ol, suppressed tumor angiogenesis. The present study was undertaken in order to es...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkateswaran A,Reddy YT,Sonar VN,Muthusamy V,Crooks PA,Freeman ML,Sekhar KR

更新日期：2010-12-15 00:00:00

abstract：:A graftable LDV (Leu-Asp-Val) peptidomimetic molecule (B-c) has been prepared from 3-(5-amino-2-hydroxy)phenyl-propionic acid, as alpha(4)beta(1) (VLA-4) integrin ligand. For that purpose, the mechanism of 3-(4-azidophenyl)propionic acid rearrangement has been revisited. Activation of Durapore DVPP-hydrophilic membran...

journal_title：Bioorganic & medicinal chemistry letters

authors： Momtaz M,Rerat V,Gharbi S,Gérard E,Pourcelle V,Marchand-Brynaert J

更新日期：2008-02-01 00:00:00

abstract：:A dumbbell-shaped circular oligonucleotide containing topoisomerase I-binding sites and two mismatched base pairs in its sequence has been designed and synthesized. Our further studies demonstrate that this particularly designed oligonucleotide displays an IC(50) value of 9 nM in its inhibition on the activity of huma...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li X,Tao Ng MT,Wang Y,Liu X,Li T

更新日期：2007-09-01 00:00:00

abstract：:Novel pyrano[4,3-b]pyran-5(4H)-one based small molecules were designed as potential inhibitors of sirtuins (i.e., yeast sir2, a homolog of human SIRT1). Elegant synthesis of these compounds was performed via a multi-step sequence consisting of MCR, Sandmeyer type iodination, Sonogashira type coupling followed by iodoc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nakhi A,Rahman MS,Archana S,Kishore R,Seerapu GP,Kumar KL,Haldar D,Pal M

更新日期：2013-07-15 00:00:00

abstract：:A series of pyrimidine benzamide-based thrombopoietin receptor agonists is described. The lead molecule contains a 2-amino-5-unsubstituted thiazole, a group that has been associated with idiosyncratic toxicity. The potential for metabolic oxidation at C-5 of the thiazole, the likely source of toxic metabolites, was re...

journal_title：Bioorganic & medicinal chemistry letters

authors： Reiter LA,Subramanyam C,Mangual EJ,Jones CS,Smeets MI,Brissette WH,McCurdy SP,Lira PD,Linde RG,Li Q,Zhang F,Antipas AS,Blumberg LC,Doty JL,Driscoll JP,Munchhof MJ,Ripp SL,Shavnya A,Shepard RM,Sperger D,Thomasco LM

更新日期：2007-10-01 00:00:00

abstract：:A novel neurokinin-1 receptor antagonist, (+/-)-(1R( *),3S( *),4S( *),5S( *))-4-[(N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-3-phenyl-2-aza-7-oxabicyclo[3.3.0]octane (1), was synthesized stereoselectively using Padwa's intramolecular 1,3-dipolar cycloaddition methodology as the key step. Compound (+/-)-1 showed high...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shishido Y,Ito F,Morita H,Ikunaka M

更新日期：2007-12-15 00:00:00

abstract：:The concept of sequential cytotoxicity, which states that successive chemical attacks on cellular constituents can be more deleterious to neoplasms than normal cells, was evaluated using a series of 3,5-bis(benzylidene)-1-diethylphosphono-4-oxopiperidines 1 and related phosphonic acids 2, which were screened against a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Das S,Das U,Sakagami H,Hashimoto K,Kawase M,Gorecki DK,Dimmock JR

更新日期：2010-11-15 00:00:00

abstract：:A series of 1-isoquinolinylguanidines are shown to be potent inhibitors of uPA with selectivity over tPA and plasmin. Potency is enhanced by the presence of a 4-halo and a 7-aryl substituent, particularly when substituted by a 3-carboxylic acid group. Compound 13j (UK-356,202) combines excellent potency and selectivit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Barber CG,Dickinson RP,Fish PV

更新日期：2004-06-21 00:00:00

abstract：:In this study, 5-methylmellein (5-MM) loaded bovine serum albumin nanoparticles (BSA NPs) were developed using desolvation technique. The developed nanoparticles were characterized for their mean particle size, polydispersity, zeta potential, loading efficiency, X-ray diffractometry (XRD), differential scanning calori...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arora D,Kumar A,Gupta P,Chashoo G,Jaglan S

更新日期：2017-12-01 00:00:00

abstract：:To obtain modulators for reducing mitochondrial damage by the inhibition of Aβ oligomer formation, 2-phenylbenzofuran derivatives were designed and prepared. Their inhibitory activity against Aβ fibril formation was screened using ThT fluorescence assay, and the effect of derivatives on mitochondrial function was eval...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee YS,Kim HY,Youn HM,Seo JH,Kim Y,Shin KJ

更新日期：2013-11-01 00:00:00

abstract：:We have recently reported that the elaboration of the N-substituent in the δ opioid receptor (DOR) antagonist naltrindole (NTI) enabled the regulation of the DOR activities from full inverse agonists to weak partial agonists. The investigations of amide-type NTI derivatives revealed that N-phenylacetyl and N-dihydroci...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujii H,Uchida Y,Shibasaki M,Nishida M,Yoshioka T,Kobayashi R,Honjo A,Itoh K,Yamada D,Hirayama S,Saitoh A

更新日期：2020-06-15 00:00:00