Copper dipicolinates as peptidomimetic ligands for the Src SH2 domain.

abstract：:The strategy and SAR studies that led to the discovery of a novel potent and orally available 5-lipoxygenase (5-LO) inhibitor 3-(4-fluorophenyl)-6-({4-[(1S)-1-hydroxy-1-(trifluoromethyl)propyl]-1H-1,2,3-triazol-1-yl}methyl)-1-benzothiophene-2-carboxamide ((S)-2l or MK-5286) were described. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li L,Berthelette C,Chateauneuf A,Ouellet M,Sturino CF,Wang Z

更新日期：2010-12-15 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：:Sphingosine-1-phosphate (S1P) is an important regulator of a wide variety of biological processes acting as an endogenous ligand to EDG/S1P receptors. In an effort to establish structure-activity relationship between EDG/S1P and ligands, we report herein homology modeling study of EDG-1/S1P(1), syntheses of S1P analog...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lim HS,Park JJ,Ko K,Lee MH,Chung SK

更新日期：2004-05-17 00:00:00

abstract：:The discovery of 2-acylamino-2-phenylethyl disodium phosphates and as structurally novel inhibitors of TNF-alpha production is reported. Structure-activity relationships (SARs) are also discussed. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Matsui T,Kondo T,Nishita Y,Itadani S,Nakatani S,Omawari N,Sakai M,Nakazawa S,Ogata A,Ohno H,Obata T,Nakai H,Toda M

更新日期：2002-03-25 00:00:00

abstract：:Ganglioside GM1 mimics including (R)-2-hydroxy-3-cyclohexylpropionic acid or (R)-2-hydroxy-3-phenylpropionic acid as replacements for NeuAc are stronger cholera toxin binders than the parent ligand 2, which includes (R)-2-hydroxy-propionic acid. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Arosio D,Baretti S,Cattaldo S,Potenza D,Bernardi A

更新日期：2003-11-03 00:00:00

abstract：:Alkaline phosphatase (AP) isozymes are present in a wide range of species from bacteria to man and are capable of dephosphorylation and transphosphorylation of a wide spectrum of substrates in vitro. In humans, four AP isozymes have been identified-one tissue-nonspecific (TNAP) and three tissue-specific-named accordin...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ardecky RJ,Bobkova EV,Kiffer-Moreira T,Brown B,Ganji S,Zou J,Pass I,Narisawa S,Iano FG,Rosenstein C,Cheltsov A,Rascon J,Hedrick M,Gasior C,Forster A,Shi S,Dahl R,Vasile S,Su Y,Sergienko E,Chung TDY,Kaunitz J,H

更新日期：2014-02-01 00:00:00

abstract：:We have synthesized and evaluated a series of 1,4-disubstituted-triazole derivatives for inhibition of the rat Na(V)1.6 sodium channel isoform, an isoform thought to play an important role in controlling neuronal firing. Starting from a series of 2,4(1H)-diarylimidazoles previously published, we decided to extend the ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Rivara M,Patel MK,Amori L,Zuliani V

更新日期：2012-10-15 00:00:00

abstract：:2,6-Diamino-4,N-diarylpyridines were identified as potent, isoform selective inhibitors of the enzymatic activity of lysophosphatidic acid acyltransferase-beta (LPAAT-beta). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hong F,Hollenback D,Singer JW,Klein P

更新日期：2005-11-01 00:00:00

abstract：:Here we present a proof-of-concept study, combining two known antimicrobial agents into a hybrid structure in order to develop an emergent cationic detergent-like interaction with the bacterial membrane. Six amphiphilic conjugates were prepared by copper (I)-catalyzed 1,3-dipolar cycloaddition between a neomycin B-der...

journal_title：Bioorganic & medicinal chemistry letters

authors： Findlay B,Zhanel GG,Schweizer F

更新日期：2012-02-15 00:00:00

abstract：:A stereoselective synthesis of dinucleoside boranophosphates by using nucleoside 3'-oxazaphospholidine derivatives is described. The diastereoselectivity of the internucleotidic bond formation reactions varied with the nucleobase used. (Rp)- and (Sp)-dithymidine boranophosphates were synthesized with excellent diaster...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wada T,Maizuru Y,Shimizu M,Oka N,Saigo K

更新日期：2006-06-15 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：:The synthesis and biological evaluation of trans-2,3-dihydroraloxifene, 2, is described. The synthesis proceeds in 8 steps in 20% overall yield. Relative trans 2,3-stereochemistry is definitively established in ester 6, which is converted to the title compound via derivatization, Grignard addition, and deprotection. E...

journal_title：Bioorganic & medicinal chemistry letters

authors： Schmid CR,Glasebrook AL,Misner JW,Stephenson GA

更新日期：1999-04-19 00:00:00

abstract：:Synthesis and biological evaluation of novel and potent cyclohexylamine-based histamine H3 receptor inverse agonists are described. Compounds in this newly identified series exhibited subnanomolar binding affinities for human receptor and no significant interaction with hERG channel. One derivative (10t) demonstrated ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Labeeuw O,Levoin N,Poupardin-Olivier O,Calmels T,Ligneau X,Berrebi-Bertrand I,Robert P,Lecomte JM,Schwartz JC,Capet M

更新日期：2011-09-15 00:00:00

abstract：:Eight monosaccharide analogs of the potent antitumor OSW saponins (2-9) were synthesized. One analog, 2-O-acetyl-alpha-l-arabinopyranoside 3, showed antiproliferative activity against the Jurkat cells (IC(50)=0.078microM) comparable to that of the disaccharide derivative (1). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Tang P,Mamdani F,Hu X,Liu JO,Yu B

更新日期：2007-02-15 00:00:00

abstract：:A new series of triazole compounds possessing a carbon atom in place of a sulfur atom were efficiently synthesized and their in vitro antifungal activities were investigated. The carbon analogs showed excellent in vitro activity against Candida, Cryptococcus, and Aspergillus species. The MICs of compound 1c against C....

journal_title：Bioorganic & medicinal chemistry letters

authors： Uchida T,Somada A,Kagoshima Y,Konosu T,Oida S

更新日期：2008-12-15 00:00:00

abstract：:Spatiotemporal control of protein fluorescence is a powerful tool in tracking protein movements within cells. Here we report an approach to using genetically encoded photo-caged amino acids to control labeling protein tetracysteine tags with biarsenical fluorescein dyes (FlAsH). ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wilkins BJ,Yang X,Cropp TA

更新日期：2009-08-01 00:00:00

abstract：:Telomeric G-rich single-stranded DNA can adopt a G-tetraplex structure which has been shown to inhibit telomerase activity. We have examined benzoindoloquinolines derivatives for their ability to stabilize an intramolecular G-quadruplex. The increase in T(m) value of the G-quadruplex was associated with telomerase inh...

journal_title：Bioorganic & medicinal chemistry letters

authors： Alberti P,Schmitt P,Nguyen CH,Rivalle C,Hoarau M,Grierson DS,Mergny JL

更新日期：2002-04-08 00:00:00

abstract：:HIV integrase catalyzes the integration of HIV DNA copy into the host cell DNA, which is essential for the production of progeny viruses. L-Chicoric acid and dicaffeoylquinic acids, isolated from plants, are well known potent inhibitors of HIV integrase. The common structural features of these inhibitors are caffeic a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee JY,Yoon KJ,Lee YS

更新日期：2003-12-15 00:00:00

abstract：:A series of substituted indoles were examined as selective inhibitors of tropomyosin-related kinase receptor A (TrkA), a therapeutic target for the treatment of pain. An SAR optimization campaign based on ALIS screening lead compound 1 is reported. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hurzy DM,Henze DA,Cabalu TD,Narayan K,Heller A,Cooke AJ

更新日期：2017-06-15 00:00:00

abstract：:Design, synthesis, and SAR of 7-oxopyrrolopyridine-derived DPP4 inhibitors are described. The preferred stereochemistry of these atropisomeric biaryl analogs has been identified as Sa. Compound (+)-3t, with a K(i) against DPP4, DPP8, and DPP9 of 0.37 nM, 2.2, and 5.7 μM, respectively, showed a significant improvement ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang W,Devasthale P,Wang A,Harrity T,Egan D,Morgan N,Cap M,Fura A,Klei HE,Kish K,Weigelt C,Sun L,Levesque P,Li YX,Zahler R,Kirby MS,Hamann LG

更新日期：2011-11-15 00:00:00

abstract：:Herein, we report the design and synthesis of the novel 12-membered non-antibiotic macrolide (8R,9S)-8,9-dihydro-6,9-epoxy-8,9-anhydropseudoerythromycin A (EM900), which was found to be a potent anti-inflammatory and/or immunomodulatory agent, capable of promoting monocyte to macrophage differentiation. This molecule ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sugawara A,Sueki A,Hirose T,Nagai K,Gouda H,Hirono S,Shima H,Akagawa KS,Omura S,Sunazuka T

更新日期：2011-06-01 00:00:00

abstract：:Four stereoisomeric hybrids of the polyketide natural products callystatin A and leptomycin B have been prepared by parallel synthetic routes involving chiral allenylstannane methodology. Like their natural counterparts, these hybrids exhibit nanomolar levels of cytotoxicity toward HCT-116 human colon cancer cells. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Marshall JA,Mikowski AM,Bourbeau MP,Schaaf GM,Valeriote F

更新日期：2006-01-15 00:00:00

abstract：:Structural features of the substituted 4-piperidinyl urea analogs 1, responsible for the H3 antagonist activity, have been identified. Structure-activity relationship of the H3 receptor affinity, hERG ion channel inhibitory activity and their separation is described. Preliminary pharmacokinetic evaluation of the compo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Berlin M,Lee YJ,Boyce CW,Wang Y,Aslanian R,McCormick KD,Sorota S,Williams SM,West RE Jr,Korfmacher W

更新日期：2010-04-01 00:00:00

abstract：:Thirteen new 2-pyrazoline derivatives bearing benzenesulfonamide moiety (2a-m) were synthesized by condensing appropriate chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride and tested for anticancer and anti-inflammatory actions. According to the protocol of the National Cancer Institute (NCI) in vitro diseas...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bashir R,Ovais S,Yaseen S,Hamid H,Alam MS,Samim M,Singh S,Javed K

更新日期：2011-07-15 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：:We herein report the discovery of four series of fused 5,6-bicyclic heterocycles as γ-secretase modulators. Synthesis and SAR of these series are discussed. These compounds represent a new class of γ-secretase modulators that demonstrate moderate to good in vitro potency in inhibiting Aβ(42) production. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qin J,Dhondi P,Huang X,Mandal M,Zhao Z,Pissarnitski D,Zhou W,Aslanian R,Zhu Z,Greenlee W,Clader J,Zhang L,Cohen-Williams M,Jones N,Hyde L,Palani A

更新日期：2011-01-15 00:00:00

abstract：:A series of 2-phenylbenzofuran derivatives with a diphenylmethylcarbamoyl group at the 5 or 6 position of the benzofuran ring were synthesized and evaluated for rat and human testosterone 5 alpha-reductase inhibitory activities in vitro. They had inhibitory activities against both enzymes and the 6-carbamoyl derivativ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ishibashi K,Nakajima K,Sugioka Y,Sugiyama M,Hamada T,Horikoshi H,Nishi T

更新日期：1998-03-17 00:00:00

abstract：:The fruits of Cudrania tricuspidata (Carr.) Bur. (Moraceae) significantly inhibited pancreatic lipase, which plays a key role in fat absorption. Optimization of extraction conditions with minimum pancreatic lipase activity and maximum yield was determined using response surface methodology with three-level-three-facto...

journal_title：Bioorganic & medicinal chemistry letters

authors： Jeong JY,Jo YH,Lee KY,Do SG,Hwang BY,Lee MK

更新日期：2014-05-15 00:00:00

abstract：:A series of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones were synthesized and evaluated for their in vitro anti-filarial activity. To pre-assess the anti-filarial behavior of synthesized compounds (V(a-f)) on a structural basis, automated docking studies were carried out with Molecular Design Sui...

journal_title：Bioorganic & medicinal chemistry letters

authors： Chhajed SS,Manisha P,Bastikar VA,Animeshchandra H,Ingle VN,Upasani CD,Wazalwar SS

更新日期：2010-06-15 00:00:00

abstract：:Radicicol and geldanamycin are potent inhibitors of the Hsp90 protein folding machinery, which is an emerging target for the development of cancer chemotherapeutics. However, radicicol is inactive in vivo and geldanamycin suffers from its redox-active behavior that produces toxicity unrelated to Hsp90 inhibition. It w...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang M,Shen G,Blagg BS

更新日期：2006-05-01 00:00:00