Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree!

abstract：:Two new C(29) sterols with a cyclopropane ring at C-25 and C-26, petrosterol-3,6-dione (1) and 5alpha,6alpha-epoxy-petrosterol (2), along with petrosterol (3), were isolated from the Vietnamese marine sponge Ianthella sp. The structures of the new compounds were elucidated by comprehensive spectroscopic analyses. Comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Nguyen HT,Chau VM,Tran TH,Phan VK,Hoang TH,Nguyen TD,Nguyen XN,Tai BH,Hyun JH,Kang HK,Kim YH

更新日期：2009-08-15 00:00:00

abstract：:The discovery of a series of novel and orally efficacious type II calcimimetics, developed from the lead compound 1, is described herein. Compound 22 suppressed plasma PTH levels relative to vehicle when dosed orally in a rat pharmacodynamic model. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Harrington PE,St Jean DJ Jr,Clarine J,Coulter TS,Croghan M,Davenport A,Davis J,Ghiron C,Hutchinson J,Kelly MG,Lott F,Lu JY,Martin D,Morony S,Poon SF,Portero-Larragueta E,Reagan JD,Regal KA,Tasker A,Wang M,Yang Y,

更新日期：2010-09-15 00:00:00

abstract：:Effect of a series of 1-phenylthioureas 1a-k and 1,3-disubstituted thioureas 2a-k were evaluated against melanin formation in melanoma B16 cell line and mushroom tyrosinase. Inhibitory activity of tyrosinase of 1-phenylthioureas 1a-k is parallel to their melanogenic inhibition. Thus, the melanogenic inhibition in mela...

journal_title：Bioorganic & medicinal chemistry letters

authors： Thanigaimalai P,Lee KC,Sharma VK,Joo C,Cho WJ,Roh E,Kim Y,Jung SH

更新日期：2011-11-15 00:00:00

abstract：:Several unnatural derivatives of narciclasine were prepared in which the C-7 carbon was replaced with nitrogen. The 7-aza derivative and its N-oxide were prepared by the coupling of iodopicolinic acid with a conduramine unit derived chemoenzymatically from bromobenzene. Intramolecular Heck reaction was used to constru...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vshyvenko S,Reisenauer MR,Rogelj S,Hudlicky T

更新日期：2014-09-01 00:00:00

abstract：:Ortho-substituted biphenyl moieties are widely used in drug design. We herein report a successful use of the perpendicular conformation of the alpha-substituted phenylcyclopropyl groups to mimic the aplanar, biologically active conformation of the ortho-substituted biphenyl moieties to achieve structural diversity. Th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Qiao JX,Cheney DL,Alexander RS,Smallwood AM,King SR,He K,Rendina AR,Luettgen JM,Knabb RM,Wexler RR,Lam PY

更新日期：2008-07-15 00:00:00

abstract：:The discovery of a novel class of HCV inhibitors is described. The new amidinourea compounds were designed as isosteric analogues of the antiviral drug moroxydine. The two derivatives 11g and 11h showed excellent HCV inhibition activity and viability and proved to inhibit a step(s) of the RNA replication. The new comp...

journal_title：Bioorganic & medicinal chemistry letters

authors： Magri A,Reilly R,Scalacci N,Radi M,Hunter M,Ripoll M,Patel AH,Castagnolo D

更新日期：2015-11-15 00:00:00

abstract：:Tuberculosis (TB) continues to remain one of the most threatening diseases in the world. With the emergence of multi-drug resistant (MDR) and extensively drug resistant (XDR) strains, the need to develop new therapies is dire. The syntheses of a focused library of hydroxamates and hydroxamic acids is described, as wel...

journal_title：Bioorganic & medicinal chemistry letters

authors： Majewski MW,Cho S,Miller PA,Franzblau SG,Miller MJ

更新日期：2015-11-01 00:00:00

abstract：:An α-carbonic anhydrase (CA, EC 4.2.1.1) isolated from the living fossil sponge Astrosclera willeyana, Astrosclerin, was investigated for its inhibition profile with simple inorganic anions, complex anions and other small molecules known to interact with these zinc enzymes. Astrosclerin is a catalytically highly effic...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ohradanova A,Vullo D,Pastorekova S,Pastorek J,Jackson DJ,Wörheide G,Supuran CT

更新日期：2012-02-01 00:00:00

abstract：:A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Skerlj R,Bridger G,Zhou Y,Bourque E,McEachern E,Langille J,Harwig C,Veale D,Yang W,Li T,Zhu Y,Bey M,Baird I,Sartori M,Metz M,Mosi R,Nelson K,Bodart V,Wong R,Fricker S,Mac Farland R,Huskens D,Schols D

更新日期：2011-12-01 00:00:00

abstract：:(R)-Glycerol-monolinoleate 4 and (R)-glycerol-monostearate 5 were isolated from the ethyl acetate extracts of Saururus chinensis roots and (R)- or (S)-fatty acid glycerols 4 and 5 were synthesized for confirming their structures and evaluating their inhibitory activities against Lp-PLA(2). The (R)-4 and (S)-4 exhibite...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee WS,Kim MJ,Beck YI,Park YD,Jeong TS

更新日期：2005-08-01 00:00:00

abstract：:A one step synthesis of fluorescent 8-aryl-(7-deazaguanines) has been accomplished. Probes exhibit blue to green high quantum yield fluorescence in a variety of organic and aqueous solutions, high extinction coefficients, and large Stokes shifts often above 100 nm. The probes are highly cell permeable, and exhibit sta...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dhimitruka I,Eubank TD,Gross AC,Khramtsov VV

更新日期：2015-10-15 00:00:00

abstract：:A new cytotoxic β-carboline alkaloid, 1-methyl-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (1), was isolated from roots of Galianthe thalictroides, together with the alkaloid 1-(hydroxymethyl)-3-(2-hydroxypropan-2-yl)-2-(5-methoxy-9H-β-carbolin-1-yl)-cyclopentanol (2), the anthraquinones 1-...

journal_title：Bioorganic & medicinal chemistry letters

authors： de Oliveira Figueiredo P,Perdomo RT,Garcez FR,de Fatima Cepa Matos M,de Carvalho JE,Garcez WS

更新日期：2014-03-01 00:00:00

abstract：:A Hit-to-Lead optimisation programme was carried out on the high throughput screening hit, the triazolethiol 1, resulting in the discovery of the potent, orally bioavailable triazolethiol CXCR2 receptor antagonist 45. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Baxter A,Bennion C,Bent J,Boden K,Brough S,Cooper A,Kinchin E,Kindon N,McInally T,Mortimore M,Roberts B,Unitt J

更新日期：2003-08-18 00:00:00

abstract：:The iridium(III)-catalyzed ortho-C-H amidation of benzoic acids with sulfonyl azides is described. These transformations allow the facile generation of N-sulfonyl anthranilic acids, which are known as crucial scaffolds found in biologically active molecules. In addition, all synthetic products were evaluated for in vi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Han SH,Suh HS,Jo H,Oh Y,Mishra NK,Han S,Kim HS,Jung YH,Lee BM,Kim IS

更新日期：2017-05-15 00:00:00

abstract：:A urokinase targeting conjugate of 2'-deoxy-5-fluorouridine (5-FUdr) was synthesized and tested for tumor-cell selective cytotoxicity in vitro. The 5-FUdr prodrug 2'-deoxy-5-fluoro-3'-O-(3-carboxypropanoyl)uridine (5-FUdrsuccOH) containing an ester-labile succinate linker was attached to the specific urokinase inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Vine KL,Locke JM,Bremner JB,Pyne SG,Ranson M

更新日期：2010-05-01 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：:During the course of our efforts toward the discovery of human histamine H4 antagonists from a series of 2-aminiopyrimidines, it was noted that a 6-trifluoromethyl group dramatically reduced affinity of the series toward the histamine H4 receptor. This observation was further investigated by synthesizing a series of l...

journal_title：Bioorganic & medicinal chemistry letters

authors： Savall BM,Meduna SP,Venable J,Wei J,Smith RC,Hack MD,Thurmond RL,McGovern P,Edwards JP

更新日期：2014-12-01 00:00:00

abstract：:Benzalacetone synthase (BAS) and chalcone synthase (CHS) are plant-specific type III polyketide synthases (PKSs), sharing 70% amino acid sequence identity and highly homologous overall protein structures. BAS catalyzes the decarboxylative coupling of 4-coumaroyl-CoA with malonyl-CoA to produce the diketide benzalaceto...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shimokawa Y,Morita H,Abe I

更新日期：2010-09-01 00:00:00

abstract：:Benzylidene-2,4-thiazolidinedione derivatives with substitutions at both the ortho and para-positions of the phenyl group were synthesized as PTP1B inhibitors with IC(50) values in a low micromolar range. Compound 18l, the lowest, bore an IC(50) of 1.3 μM. In a peroxisome proliferator-activated receptor-γ (PPAR-γ) pro...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhattarai BR,Kafle B,Hwang JS,Ham SW,Lee KH,Park H,Han IO,Cho H

更新日期：2010-11-15 00:00:00

abstract：:The synthesis and inhibitory activities of 10 potential inhibitors of Pfmrk, a Plasmodium falciparum cyclin-dependent protein kinase, are described. The most potent inhibitor is a 3-phenyl-quinolinone compound with an IC(50) value of 18 microM. It is the first compound reported to inhibit Pfmrk at the micro molar rang...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xiao Z,Waters NC,Woodard CL,Li Z,Li PK

更新日期：2001-11-05 00:00:00

abstract：:A series of novel fusidic acid (FA) derivatives was synthesized by replacing the carboxylic acid group with various ester and amide groups and evaluated in vitro for their antiplasmodial activity against the chloroquine-sensitive NF54 and multidrug-resistant K1 strains of the malarial parasite Plasmodium falciparum. M...

journal_title：Bioorganic & medicinal chemistry letters

authors： Espinoza-Moraga M,Singh K,Njoroge M,Kaur G,Okombo J,De Kock C,Smith PJ,Wittlin S,Chibale K

更新日期：2017-02-01 00:00:00

abstract：:Protein tyrosine phosphatase 1B (PTP1B) is a major negative regulator in insulin- and leptin-signaling cascades as well as a positive regulator in tumorigenesis, and much attention has been paid to PTP1B inhibitors as potential therapies for diabetes, obesity, and cancer. In the present study, the screening of a compo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li W,Li S,Higai K,Sasaki T,Asada Y,Ohshima S,Koike K

更新日期：2013-11-01 00:00:00

abstract：:In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang L,Huang Y,Zhang J,Tong L,Chen Y,Lu W,Huang Q

更新日期：2014-03-15 00:00:00

abstract：:Amino-1,2,5-trideoxy-2,5-imino-D-mannitol was fluorescently tagged by reaction with dansyl chloride at N-1 or by attachment of a dansyl amide bearing spacer to this centre. Compounds obtained are highly potent inhibitors of beta-glucosidase exhibiting Ki values in the single figure nanomolar range. The 1-N-dansyl subs...

journal_title：Bioorganic & medicinal chemistry letters

authors： Hermetter A,Scholze H,Stütz AE,Withers SG,Wrodnigg TM

更新日期：2001-05-21 00:00:00

abstract：:A short route to pyrimidine locked nucleosides has been developed for their incorporation in triplex forming oligonucleotides (TFO). Compared to oligonucleotides built with standard nucleosides, the modified TFOs containing 3'-endo blocked residues formed, with their corresponding DNA duplexes, more stable triple heli...

journal_title：Bioorganic & medicinal chemistry letters

authors： Savy P,Benhida R,Fourrey JL,Maurisse R,Sun JS

更新日期：2000-10-16 00:00:00

abstract：:4-Anilino-3-cyanoquinolines were reported to have irreversible binding to epidermal growth factor receptor kinase (EGFRK) by forming a covalent linkage to C773. Our initial docking studies gave results inconsistent with the in vitro data and showed two different binding modes. To perceive the exact mode of binding of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Akula N,Bhalla J,Sridhar J,Pattabiraman N

更新日期：2004-07-05 00:00:00

abstract：:N6-Substituted adenosine analogues containing cyclic hydrazines or chiral hydroxy (ar)alkyl groups, designed to interact with the S2 and S3 receptor subregions, have been synthesized and their binding to the adenosine A1 and A2A receptors have been investigated. Examples of both types of compounds were found to exhibi...

journal_title：Bioorganic & medicinal chemistry letters

authors： Ha SB,Melman N,Jacobson KA,Nair V

更新日期：1997-12-16 00:00:00

abstract：:A series of sixteen β-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-β-carboline and various aldehydes under basic conditions followed by N2-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Venkataramana Reddy PO,Hridhay M,Nikhil K,Khan S,Jha PN,Shah K,Kumar D

更新日期：2018-05-01 00:00:00

abstract：:Twenty-six new hydrophilic chiral 2-alkoxy-1,4-butanediamine platinum (II) complexes having a seven-membered ring structure between a bidentate carrier ligand and a platinum atom have been synthesized and most of them were evaluated for their in vitro cytotoxicity toward A549 human non-small cell lung carcinoma and HC...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhu H,Cui K,Wang L,Gou S

更新日期：2005-11-15 00:00:00

abstract：:To continue our study of 2-morpholino-benzoxazine based compounds, which show useful activity against PI3K family enzymes or antiplatelet activity, we designed and synthesized a series of linear 6.7-fused, 5,6-angular fused and 7,8-angular fused-aryl-morpholino-naphth-oxazines. The compounds were prepared from substit...

journal_title：Bioorganic & medicinal chemistry letters

authors： Morrison R,Zheng Z,Jennings IG,Thompson PE,Al-Rawi JMA

更新日期：2016-11-15 00:00:00