Development of novel tail-modified anandamide analogs.

abstract：:Pinusolide (1), a known platelet-activating factor (PAF) receptor binding antagonist, was synthesized from lambertianic acid (2), a labdane-type diterpene readily accessible in multigram quantities from the Siberian pine tree. It was shown that 1 not only decreases the proliferation activity of tumor cells at relative...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shults EE,Velder J,Schmalz HG,Chernov SV,Rubalova TV,Gatilov YV,Henze G,Tolstikov GA,Prokop A

更新日期：2006-08-15 00:00:00

abstract：:A new triterpenoid saponin, julibroside J(28) (1), was isolated from the stem bark of Albizia julibrissin Durazz (Leguminosae) by using chromatographic method. The structure of 1 was established by spectroscopic methods. 1 displayed significant antitumor activity in vitro against PC-3M-1E8, Bel-7402, and HeLa cancer c...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liang H,Tong WY,Zhao YY,Cui JR,Tu GZ

更新日期：2005-10-15 00:00:00

abstract：:A photoresponsive RNA aptamer to hemin was selected in vitro from a random sequence library of RNAs with azobenzene residues. The aptamer bound to hemin under visible light irradiation and was released by ultraviolet light. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu M,Jinmei H,Abe H,Ito Y

更新日期：2010-05-01 00:00:00

abstract：:A series of potent dual JAK1/3 inhibitors have been developed from a moderately selective JAK3 inhibitor. Substitution at the C6 position of the pyrrolopyridazine core with aryl groups provided exceptional biochemical potency against JAK1 and JAK3 while maintaining good selectivity against JAK2 and Tyk2. Translation t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hynes J Jr,Wu H,Kempson J,Duan JJ,Lu Z,Jiang B,Stachura S,Tokarski JS,Sack JS,Khan JA,Lippy JS,Zhang RF,Pitt S,Shen G,Gillooly K,McIntyre K,Carter PH,Barrish JC,Nadler SG,Salter-Cid LM,Fura A,Schieven GL,Pitts

更新日期：2017-07-15 00:00:00

abstract：:A homology model of the nicotinic acid receptor GPR109A was constructed based on the X-ray crystal structure of bovine rhodopsin. An HTS hit was docked into the homology model. Characterization of the binding pocket by a grid-based surface calculation of the docking model suggested that a larger hydrophobic body plus ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Deng Q,Frie JL,Marley DM,Beresis RT,Ren N,Cai TQ,Taggart AK,Cheng K,Carballo-Jane E,Wang J,Tong X,Waters MG,Tata JR,Colletti SL

更新日期：2008-09-15 00:00:00

abstract：:A unique chromism-based assay technique (CHROBA) using photochromic spiropyran-containing peptides has been firstly established for detection of protein kinase A-catalyzed phosphorylation. The alternative method has advantages that avoid isolation and/or immobilization of kinase substrates to remove excess reagents in...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tomizaki KY,Jie X,Mihara H

更新日期：2005-03-15 00:00:00

abstract：:Pinostrobin (5-hydroxy-7-methoxyflavanone) obtained in relatively large amounts from fingerroot (Boesenbergia pandurata) was converted to its C-6 and C-8 prenylated derivatives. The Mitsunobu reaction, europium(III)-catalyzed Claisen-Cope rearrangement, and Claisen reaction coupled with cross-metathesis were used as t...

journal_title：Bioorganic & medicinal chemistry letters

authors： Poerwono H,Sasaki S,Hattori Y,Higashiyama K

更新日期：2010-04-01 00:00:00

abstract：:A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives were synthesized via converting the readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and then reacting with different substituted amines. The molecular struct...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rambabu D,Mulakayala N,Ismail,Kumar KR,Kumar GP,Mulakayala C,Kumar CS,Kalle AM,Rao MV,Oruganti S,Pal M

更新日期：2012-11-01 00:00:00

abstract：:A novel conjugate of Hoechst 33258, pyrene and neomycin was synthesized and examined for its binding and stabilization of A-T rich DNA duplexes using spectroscopic and viscometric techniques. The conjugate, containing three well known ligands that bind nucleic acids albeit in different binding modes, was found to sign...

journal_title：Bioorganic & medicinal chemistry letters

authors： Willis B,Arya DP

更新日期：2009-09-01 00:00:00

abstract：:Cu(II) complexes with 4,6-di(tert-butyl)-2-aminophenol (I) and 2-anilino-4,6-di(tert-butyl)phenol (II) have been synthesized and characterized by means of elemental analysis, TG/DTA, FT-IR, UV-vis, ESR, and conductance measurements. The compounds I and II can coordinate in their singly deprotonated forms and behave as...

journal_title：Bioorganic & medicinal chemistry letters

authors： Loginova NV,Koval'chuk TV,Zheldakova RA,Osipovich NP,Sorokin VL,Polozov GI,Ksendzova GA,Glushonok GK,Chernyavskaya AA,Shadyro OI

更新日期：2006-10-15 00:00:00

abstract：:Novel dihydropyrazole sulfonamide derivatives (30-56) were designed, synthesized, and evaluated for their biological activities as COX-1 and COX-2 inhibitors. In vitro biological evaluation against three human tumor cell lines revealed that most target compounds showed antiproliferative activities. Among the compounds...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chen Z,Wang ZC,Yan XQ,Wang PF,Lu XY,Chen LW,Zhu HL,Zhang HW

更新日期：2015-05-01 00:00:00

abstract：:Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD-deficient variant of human Jurkat T cells treated with TNF-alpha. 5-(1H-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1H-indol-3-ylmethyl)hydantoins were found to be p...

journal_title：Bioorganic & medicinal chemistry letters

authors： Teng X,Degterev A,Jagtap P,Xing X,Choi S,Denu R,Yuan J,Cuny GD

更新日期：2005-11-15 00:00:00

abstract：:We report a dimerization strategy to enhance the antibacterial potency of an otherwise weak cationic amphiphilic polyproline helical (CAPH) peptide. Overall, the dimeric CAPHs were more active against Escherichia coli and Staphylococcus aureus than the monomeric counterpart, reaching up to a 60-fold increase in potenc...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hernandez-Gordillo V,Geisler I,Chmielewski J

更新日期：2014-01-15 00:00:00

abstract：:Potent cyclin dependent kinase inhibitors were prepared using parallel synthesis methodology. Treating advanced intermediate 2 with a variety of hydrazides in DMSO at 80 degrees C for 30 min gave the desired acylsemicarbazides in good to excellent yield. Several compounds were active against cdk4/D1 and cdk2/E in the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nugiel DA,Vidwans A,Dzierba CD

更新日期：2004-11-15 00:00:00

abstract：:To improve the DNA hydrolytic activity of the zinc finger nuclease, we have created a new artificial zinc finger nuclease (ZWH4) by connecting two distinct zinc finger domains possessing different types of Zn(II) binding sites (Cys(2)His(2)- and His(4)-types). The overall fold of ZWH4 is similar to that of the wild-ty...

journal_title：Bioorganic & medicinal chemistry letters

authors： Negi S,Umeda Y,Masuyama S,Kano K,Sugiura Y

更新日期：2009-05-15 00:00:00

abstract：:A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with the nature of the ortho substituents of the benzamide ring, and reductions in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Varnes JG,Xiong H,Forst JM,Holmquist CR,Ernst GE,Frietze W,Dembofsky B,Andisik DW,Palmer WE,Hinkley L,Steelman GB,Wilkins DE,Tian G,Jonak G,Potts WM,Wang X,Brugel TA,Alhambra C,Wood MW,Veale CA,Albert JS

更新日期：2018-04-01 00:00:00

abstract：:A series of 1-adamantanecarboxamides was synthesized and examined for their potency as a selective 5-HT2 receptor antagonist. We found (S)-N-[1-[2-(4-fluorophenyl)ethyl]pyrrolidin-3-yl]-1-adamantane carboxamide hydrochloride hydrate (10-(S), Y-39241) to have a high affinity and selectivity for 5-HT2 receptors, and thi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Fujio M,Kuroita T,Sakai Y,Nakagawa H,Matsumoto Y

更新日期：2000-11-06 00:00:00

abstract：:The biosynthetic gene cluster of brassicicene C was identified in Alternaria brassicicola strain ATCC 96836 from genome database search. In vivo and in vitro study clearly revealed the function of Orf8 and Orf6 as a fusicoccadiene synthase and methyltransferase, respectively. The understanding toward the biosynthetic ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Minami A,Tajima N,Higuchi Y,Toyomasu T,Sassa T,Kato N,Dairi T

更新日期：2009-02-01 00:00:00

abstract：:Current biosynthetic methods for producing proteins containing site-specifically incorporated unnatural amino acids are inefficient because the majority of the amino acid goes unused. Here we present a universal approach to improve the efficiency of such processes using condensed Escherichia coli cultures. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Liu J,Castañeda CA,Wilkins BJ,Fushman D,Cropp TA

更新日期：2010-10-01 00:00:00

abstract：:EGF receptor-binding peptides could be found by a peptide screening method using fifteen fluorescent amino acids as fluorescent tags. Of 225 peptides, we found an 8-mer peptide containing a dipeptide unit, Y-F, which was the strongest binding peptide to the EGF receptor. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kitamatsu M,Yamamoto T,Futami M,Sisido M

更新日期：2010-10-15 00:00:00

abstract：:Selective inhibitors of protein tyrosine phosphatases (PTPases) are of great interest as therapeutic agents and research tools. Several phenylalanine derivatives (1, 2) designed as phosphotyrosine mimetics or irreversible active site inhibitors were successfully synthesized, then incorporated into a combinatorial libr...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan Z,Kahn M,Qabar M,Urban J,Kim HO,Blaskovich MA

更新日期：2003-06-16 00:00:00

abstract：:The first example of dual inhibitors for matrix metalloproteinase (MMP) and cathepsin is described. An appropriate alignment of peptide-parts and two different specific functional groups in one molecule led to the discovery of a potent dual inhibitor (3a). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yamamoto M,Ikeda S,Kondo H,Inoue S

更新日期：2002-02-11 00:00:00

abstract：:Two types of P1-P3-linked macrocyclic renin inhibitors containing the hydroxyethylene isostere (HE) scaffold just outside the macrocyclic ring have been synthesized. An aromatic or aliphatic substituent (P3sp) was introduced in the macrocyclic ring aiming at the S3 subpocket (S3sp) in order to optimize the potency. A ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sund C,Belda O,Wiktelius D,Sahlberg C,Vrang L,Sedig S,Hamelink E,Henderson I,Agback T,Jansson K,Borkakoti N,Derbyshire D,Eneroth A,Samuelsson B

更新日期：2011-01-01 00:00:00

abstract：:Phosphorodiamidate morpholino oligonucleotides (PMOs) have been extensively applied in antisense strategies for gene regulation because of their high stability in serum and low toxicity. However, chain elongation of PMOs requires long reaction time because few efficient methods have been developed for the formation of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Harakawa T,Tsunoda H,Ohkubo A,Seio K,Sekine M

更新日期：2012-02-01 00:00:00

abstract：:In this study, we report three novel naturally occurring compounds, blapsins A (1) and B (2), and blapsamide (3) from the ethanol extract of the stink beetle, Blaps japanensis. The structures of these compounds were determined using spectroscopic methods. Compound 3 is a phenolic compound bearing a formamido group in ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yan YM,Dai HQ,Du Y,Schneider B,Guo H,Li DP,Zhang LX,Fu H,Dong XP,Cheng YX

更新日期：2012-06-15 00:00:00

abstract：:A new class of NO-donor phenol derivatives is described. The products were obtained by joining appropriate phenols with either nitrooxy or 3-phenylsulfonylfuroxan-4-yloxy moieties. All the compounds proved to inhibit the ferrous salt/ascorbate induced lipidic peroxidation of membrane lipids of rat hepatocytes. They we...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cena C,Boschi D,Tron GC,Chegaev K,Lazzarato L,Di Stilo A,Aragno M,Fruttero R,Gasco A

更新日期：2004-12-20 00:00:00

abstract：:The use of a tri-substituted acylhydrazine as an isostere of a tertiary amide was explored in a series of HCV NS5B thumb site II inhibitors. Direct replacement generated an analog with similar conformational and physicochemical properties. The series was extended to produce compounds with potent binding affinities and...

journal_title：Bioorganic & medicinal chemistry letters

authors： Canales E,Carlson JS,Appleby T,Fenaux M,Lee J,Tian Y,Tirunagari N,Wong M,Watkins WJ

更新日期：2012-07-01 00:00:00

abstract：:By performing RNA-targeted structure-activity relationship studies, we discovered a novel peptidomimetic containing squaryldiamide as a potential bioisostere replacement for guanidine that binds transactivation responsive RNA with high affinity. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee CW,Cao H,Ichiyama K,Rana TM

更新日期：2005-10-01 00:00:00

abstract：:Novel analogues of the angiotensin I-converting enzyme (ACE) inhibitor keto-ACE were synthesized via a facile Horner-Emmons olefination of a phosphonoketone precursor with ethyl glyoxylate. Introduction of a bulky aromatic tryptophan at the P(2)(') position of keto-ACE resulted in a significant increase in C-domain-se...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nchinda AT,Chibale K,Redelinghuys P,Sturrock ED

更新日期：2006-09-01 00:00:00

abstract：:A new class of PARP-1 inhibitors, namely substituted fused uracil derivatives were synthesised. Starting from a derivative with an IC(50)=2microM the chemical optimisation program led to compounds with more than a 100-fold increase in potency (IC(50)<20nM). Additionally, physicochemical and pharmacokinetic properties ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Steinhagen H,Gerisch M,Mittendorf J,Schlemmer KH,Albrecht B

更新日期：2002-11-04 00:00:00