Syntheses of certain 3-aryl-2-propenoates and evaluation of their cytotoxicity.

abstract：:The induction of conformationally restricted N-(aryl or heteroaryl)-3-azabicyclo[3.1.0]hexane derivatives at P(2) region of compounds of 2-cyanopyrrolidine class was explored to develop novel DPP-IV inhibitors. The synthesis, structure-activity relationship, and selectivity against related proteases are delineated. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sattigeri JA,Andappan MM,Kishore K,Thangathirupathy S,Sundaram S,Singh S,Sharma S,Davis JA,Chugh A,Bansal VS

更新日期：2008-07-15 00:00:00

abstract：:The seminal human dopamine D3 receptor (hD3R) ligand BP 897 has shown interesting properties during clinical trials. However, its lack of selectivity towards human adrenergic receptor impedes further development. Two approaches were followed to increase hD3R selectivity. The lead optimisation succeeded, we disclose he...

journal_title：Bioorganic & medicinal chemistry letters

authors： Capet M,Calmels T,Levoin N,Danvy D,Berrebi-Bertrand I,Stark H,Schwartz JC,Lecomte JM

更新日期：2016-02-01 00:00:00

abstract：:A new method for the synthesis of 2'-O-methyl-2-thiouridine (s2Um) found in thermophilic bacterial tRNA was developed. Structural properties of s2Um and s2Um(p)U were studied by using 1H NMR spectroscopy. A modified nonaribonucleotide (RNA*: 5'-CGUUs2UmUUGC-3') was synthesized to study the base-recognition ability of ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Shohda K,Okamoto I,Wada T,Seio K,Sekine M

更新日期：2000-08-21 00:00:00

abstract：:Installation of a C2-aminopropyl side chain to the 2,4-diaryl-2,5-dihydropyrrole series of kinesin spindle protein (KSP) inhibitors results in potent, water soluble compounds, but the aminopropyl group induces susceptibility to cellular efflux by P-glycoprotein (Pgp). We show that by carefully modulating the basicity ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Cox CD,Breslin MJ,Whitman DB,Coleman PJ,Garbaccio RM,Fraley ME,Zrada MM,Buser CA,Walsh ES,Hamilton K,Lobell RB,Tao W,Abrams MT,South VJ,Huber HE,Kohl NE,Hartman GD

更新日期：2007-05-15 00:00:00

abstract：:Clausenamide, isolated from aqueous extract of dry leaves of Clausena lansium, a Chinese folk medicine, was found to have potent activity in enhancing LTP and show nootropic activity in animal tests. In order to discovery more potent stereoisomers and to analyze the relationship of structure-activity, the synthesis of...

journal_title：Bioorganic & medicinal chemistry letters

authors： Feng Z,Li X,Zheng G,Huang L

更新日期：2009-04-15 00:00:00

abstract：:2'-O-[N-(4-Aminobutylcarbamoyl)]uridine (U(abcm)) was synthesized and incorporated into oligonucleotides. The oligonucleotides incorporating U(abcm) formed more stable duplexes with their complementary and mismatched RNAs than those containing 2'-O-carbamoyluridine (U(cm)). The stability of duplex with a U(abcm)-rG ba...

journal_title：Bioorganic & medicinal chemistry letters

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

更新日期：2012-04-01 00:00:00

abstract：:A novel series of potent DGAT-1 inhibitors was developed originating from the lactam-based clinical candidate PF-04620110. Incorporation of a dioxino[2,3-d]pyrimidine-based core afforded good alignment of pharmacophore features and resulted in improved passive permeability. Development of an efficient, homochiral synt...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dow RL,Andrews M,Aspnes GE,Balan G,Michael Gibbs E,Guzman-Perez A,Karki K,Laperle JL,Li JC,Litchfield J,Munchhof MJ,Perreault C,Patel L

更新日期：2011-10-15 00:00:00

abstract：:This work describes a set of discovery research studies of an influenza cap-dependent endonuclease (CEN) inhibitor with a carbamoyl pyridone bicycle (CAB) scaffold. Using influenza CEN inhibitory activity, antiviral activity and pharmacokinetic (PK) parameters as indices, structure activity relationships (SAR) studies...

journal_title：Bioorganic & medicinal chemistry letters

authors： Taoda Y,Miyagawa M,Akiyama T,Tomita K,Hasegawa Y,Yoshida R,Noshi T,Shishido T,Kawai M

更新日期：2020-11-15 00:00:00

abstract：:A series of thieno[3,2-b]quinoline derivatives designed based on A-278637 scaffold, were synthesized efficiently via one-pot three-component reaction under solvent-free and catalyst-free conditions. This work provides a new compound library with potential biological activity for biomedical screening. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li T,Feng X,Yao C,Yu C,Jiang B,Tu S

更新日期：2011-01-01 00:00:00

abstract：:Acetyl CoA carboxylase (ACC) catalyzes the carboxylation of acetyl CoA to form malonyl CoA. In skeletal muscle and heart, malonyl CoA functions to regulate lipid oxidation by inhibition of carnitine palmitoyltransferase-1, an enzyme which controls the entry of long chain fatty acids into mitochondria. We have found th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Seng TW,Skillman TR,Yang N,Hammond C

更新日期：2003-10-06 00:00:00

abstract：:A series of artemisinin derived esters 7a-j, incorporating pharmacologically privileged substructure, such as biphenyl, adamantane and fluorene, have been prepared and evaluated for antimalarial activity against multidrug-resistant (MDR) Plasmodium yoelii nigeriensis by oral route. Several of these compounds were foun...

journal_title：Bioorganic & medicinal chemistry letters

authors： Singh C,Chaudhary S,Puri SK

更新日期：2008-02-15 00:00:00

abstract：:A series of 4-substituted (benzo[b]thiophene-2-carbonyl)guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardioprotective efficacy both in vitro and in vivo. Several analogs exhibited a strong inhibition on NHE-1, and which was generally well correlated with their cardioprotective efficac...

journal_title：Bioorganic & medicinal chemistry letters

authors： Lee S,Lee H,Yi KY,Lee BH,Yoo SE,Lee K,Cho NS

更新日期：2005-06-15 00:00:00

abstract：:A series of 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones were designed and synthesized as a novel class of inhibitors of NAD(+)-dependent DNA ligase that possess potency against Gram-positive bacteria. ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Wang T,Duncan L,Gu W,O'Dowd H,Wei Y,Perola E,Parsons J,Gross CH,Moody CS,Arends SJ,Charifson PS

更新日期：2012-06-01 00:00:00

abstract：:Currently, there is an ongoing interest in the synthesis of nucleoside diphosphate analogs as important regulators in catabolism/anabolism, and their potential applications as mechanistic probes and chemical tools for bioassays. However, the pyrophosphate bond formation step remains as the bottleneck. In this Digest, ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Xu Z

更新日期：2015-09-15 00:00:00

abstract：:The general strategy and rationale underlying the design of COPD therapeutics that possess protease inhibitory activity and are also capable of releasing a species that attenuates inflammation by inhibiting caspase-1, are described. The synthesis and in vitro biochemical evaluation of a dual function molecule that seq...

journal_title：Bioorganic & medicinal chemistry letters

authors： Dou D,He G,Alliston KR,Groutas WC

更新日期：2011-05-15 00:00:00

abstract：:Cyclophilins (Cyps) are ubiquitous proteins that effect the cis-trans isomerization of Pro amide bonds, and are thus crucial to protein folding. CypA is the most prevalent of the ~19 human Cyps, and plays a crucial role in viral infectivity, most notably for HIV-1 and HCV. Cyclophilins have been shown to play key role...

journal_title：Bioorganic & medicinal chemistry letters

authors： Peel M,Scribner A

更新日期：2013-08-15 00:00:00

abstract：:The synthesis of novel C6-aryl substituted derivatives of 3-(dimethylamino)chroman is described. The novel derivatives display 5-HT(7) receptor affinities that varies from nM to muM, indicating that this small set of derivatives constitute a novel and interesting starting point for further structure-serotonin 5-HT(7) ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Holmberg P,Tedenborg L,Rosqvist S,Johansson AM

更新日期：2005-02-01 00:00:00

abstract：:The synthesis of [1-[(5-hydroxy-4-(phenylmethyl)-3-oxazolidinyl)carbonyl]-2-ethylpropy lcarbamic acid phenylmethyl ester (2; MDL 104,903), a potent inhibitor of calpain, is described. Synthesis of related compounds, which offer insights into the mechanism of action for 2, are also described, as is an O-acetyl prodrug ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Peet NP,Kim HO,Marquart AL,Angelastro MR,Nieduzak TR,White JN,Friedrich D,Flynn GA,Webster ME,Vaz RJ,Linnik MD,Koehl JR,Mehdi S,Bey P,Emary B,Hwang KK

更新日期：1999-08-16 00:00:00

abstract：:Derivatives of phaeosphaeride A (PPA) were synthesised and characterised; then anti-cancer studies were carried out on the A549 cancer cell line. It was found that the acetyl derivative (compound 3) displayed comparable in vitro cytotoxicity to that of PPA (EC50=49±7 μM and EC50=46±5 μM, respectively), while chloroace...

journal_title：Bioorganic & medicinal chemistry letters

authors： Abzianidze VV,Prokofieva DS,Chisty LA,Bolshakova KP,Berestetskiy AO,Panikorovskii TL,Bogachenkov AS,Holder AA

更新日期：2015-12-01 00:00:00

abstract：:A new series of 5-(1-aryl-3-methyl-1H-pyrazol-4-yl)-1H-tetrazole derivatives (4a-m) and their precursor 1-aryl-3-methyl-1H-pyrazole-4-carbonitriles (3a-m) were synthesized and evaluated as antileishmanials against Leishmania braziliensis and Leishmania amazonensis promastigotes in vitro. In parallel, the cytotoxicity ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Faria JV,dos Santos MS,Bernardino AM,Becker KM,Machado GM,Rodrigues RF,Canto-Cavalheiro MM,Leon LL

更新日期：2013-12-01 00:00:00

abstract：:In silico modelling was used to guide the positioning of the fluorescent dye NBD-F on the cannabinoid CB2 receptor agonist JWH-015. While the ultimate fluorescent conjugate lost extensive binding affinity to the cannabinoid CB2 receptor, affinity and efficacy studies on the naphthoyl 3-position modified precursor mole...

journal_title：Bioorganic & medicinal chemistry letters

authors： Yates AS,Doughty SW,Kendall DA,Kellam B

更新日期：2005-08-15 00:00:00

abstract：:Based on the X-ray crystallography of our lead compound 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-cyanopyrazin-2-yl)urea in the checkpoint kinase 1 (Chk1) enzyme, we modified R4, and to a lesser extent, R2, and R5 of the phenyl ring, and made a variety of N-aryl-N'-pyrazinylurea Chk1 inhibitors. Enzymatic activity less th...

journal_title：Bioorganic & medicinal chemistry letters

authors： Li G,Hasvold LA,Tao ZF,Wang GT,Gwaltney SL 2nd,Patel J,Kovar P,Credo RB,Chen Z,Zhang H,Park C,Sham HL,Sowin T,Rosenberg SH,Lin NH

更新日期：2006-04-15 00:00:00

abstract：:The protein tyrosine kinases (PTKs) are essential enzymes in cellular signaling processes that regulate cell growth, differentiation, migration and metabolism. Their inhibition was recently shown to constitute a new modality for treating cancers. Two clinically used PTK inhibitors (PTKIs), imatinib (Glivec/Gleevec) an...

journal_title：Bioorganic & medicinal chemistry letters

authors： Parkkila S,Innocenti A,Kallio H,Hilvo M,Scozzafava A,Supuran CT

更新日期：2009-08-01 00:00:00

abstract：:In the search of new antihyperglycemic agents and following rational approach of drug designing here new 2-hydrazolyl-4-thiazolidinone-5-carboxylic acids (4a-g) with pyrazolyl pharmacophore have been synthesized via thia Michael addition reaction of 1-((3-(4-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)thios...

journal_title：Bioorganic & medicinal chemistry letters

authors： Bhosle MR,Mali JR,Pal S,Srivastava AK,Mane RA

更新日期：2014-06-15 00:00:00

abstract：:Oxygen dependent degradation of hypoxia-inducible factor (HIF)-1α is triggered with hydroxylation by proline hydroxylase domain 2 (PHD2) under normoxic conditions. Some of previously developed PHD2 inhibitors show a considerable potency against factor inhibiting HIF (FIH), the HIF asparagine hydroxylase. For specific ...

journal_title：Bioorganic & medicinal chemistry letters

authors： Kwon HS,Choi YK,Kim JW,Park YK,Yang EG,Ahn DR

更新日期：2011-07-15 00:00:00

abstract：:Modification of the major insecticide fipronil (1) by replacing three pyrazole substituents (hydrogen for both cyano and amino and trifluoromethyldiazirinyl for trifluoromethylsulfinyl) gives a candidate photoaffinity probe (3) of high potency (IC(50) 2-28 nM) in blocking the chloride channel of Drosophila and human b...

journal_title：Bioorganic & medicinal chemistry letters

authors： Sirisoma NS,Ratra GS,Tomizawa M,Casida JE

更新日期：2001-11-19 00:00:00

abstract：:A series of 6-alkoxyisoindolin-1-ones with a magic shotgun pharmacological profile are presented as potential antipsychotics. The in vitro pharmacological profile includes D(2) partial agonism (30-55%), 5-HT(1A) partial agonism (60-90%), and 5-HT(2A) antagonism. Selected compounds in this series displayed good in vivo...

journal_title：Bioorganic & medicinal chemistry letters

authors： Favor DA,Powers JJ,White AD,Fitzgerald LW,Groppi V,Serpa KA

更新日期：2010-10-01 00:00:00

abstract：:2-Propargylthiobenzimidazole 1, 4-bromomethyl coumarins/1-aza-coumarins 2/3 and sodium azide have been reacted in one pot under Click chemistry conditions to give exclusively 1,4-disubstituted triazoles 5a-n. Anti-tubercular assays against M. tuberculosis (H37Rv) coupled with in silico molecular docking studies indica...

journal_title：Bioorganic & medicinal chemistry letters

authors： Anand A,Kulkarni MV,Joshi SD,Dixit SR

更新日期：2016-10-01 00:00:00

abstract：:Current therapy for blood vessel thrombosis has the risk of leading to gastrointestinal bleeding and thrombocytopenia. We previously reported that a new derivative of diosgenin, compound 5, had significant anti-inflammatory activity superior to that of aspirin, prolonged bleeding time, and inhibited platelet aggregati...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zheng H,Wei Z,Xin G,Ji C,Wen L,Xia Q,Niu H,Huang W

更新日期：2016-07-15 00:00:00

abstract：:A new 'naked-eye' quinoline-based 'reactive' ratiometric fluorescent probe was prepared. The reactive stoichiometry of the probe with Hg²⁺ ion was 2:1. The probe exhibited high selectivity towards Hg²⁺ ion to other metal ions with a 410-fold increase in absorbance intensity ratio (A₄₀₂/A₃₄₀) in aqueous solution over a...

journal_title：Bioorganic & medicinal chemistry letters

authors： Zhang Y,Yan Y,Chen S,Gao Z,Xu H

更新日期：2014-12-01 00:00:00