Bicyclic molecule

About: Bicyclic molecule is a research topic. Over the lifetime, 29587 publications have been published within this topic receiving 451252 citations. The topic is also known as: bicyclic molecule.

Further insight into magnetostructural correlations in binuclear copper(II) species related to methemocyanin: x-ray crystal structure of 1,2-.mu.-nitrito complex

Abstract: Determination de la structure de [Cu 2 (L-Et)(NO 2 )] [ClO 4 ] avec HL-Et=N,N,N'N'-tetrakis-([ethyl-1 benzimidazolyl]-2) hydroxy-2 diamino-1,3 propane

Recent Developments in Enantioselective Metal‐Catalyzed Domino Reactions

Abstract: This review updates the major progress in the field of enantioselective one-, two-, and multi-component domino reactions promoted by chiral metal catalysts, covering the literature since the beginning of 2012. It illustrates how enantioselective metal-catalyzed processes have emerged as outstanding tools for the development of a wide variety of fascinating one-pot asymmetric domino reactions, allowing complex and diverse structures to be easily generated from simple materials in a single step. During the last 4 years, a myriad of already existing as well as completely novel and powerful asymmetric domino processes have been developed on the basis of asymmetric metal catalysis, taking economical advantages, such as avoiding costly protecting groups and time-consuming purification procedures after each step. Abbreviations: acac: acetylacetonate; Ad: 1-adamantyl; Ar: aryl; BArF: tetrakis[3,5-bis(trifluoromethyl)phenyl]borate; BBN: 9-borabicyclo[3.3.1]nonane; BINAP: 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl; BINAP(O): 2-diphenylphosphino-2′-diphenylphosphinyl-1,1′-binaphthalene; BINOL: 1,1′-bi-2-naphthol; BIPHEP: 2,2′-bis(diphenylphosphino)-1,1′-biphenyl; Bipy: bipyridine; Bn: benzyl; Boc: tert-butoxycarbonyl; bod: bicyclo[2.2.2]octane-2,5-diene; Box: bisoxazoline; bpe: 1,2-bis(2-pyridyl)ethane; Bs: p-bromobenzenesulfonyl (brosyl); Bz: benzoyl; Cat: catalyst; Cbz: benzyloxycarbonyl; CMOF: chiral mixed metal-organic framework; cod: cyclooctadiene; coe: cyclooctene; Cp: cyclopentadienyl; CPME: cyclopentyl methyl ether; Cy: cyclohexyl; DABCO: 1,4-diazabicyclo[2.2.2]octane; dba: (E,E)-dibenzylideneacetone; DBDMH: 1,3-dibromo-5,5-dimethylhydantoin; DCE: dichloroethane; de: diastereomeric excess; Dec: decyl; DET: diethyl tartrate; DIPEA: diisopropylethylamine; DME: 1,2-dimethoxyethane; DMF: N,N-dimethylformamide; DTBM: di-tert-butylmethoxy; ee: enantiomeric excess; EWG: electron-withdrawing group; Fesulphos: 1-phosphino-2-sulfenylferrocene; Hept: heptyl; Hex: hexyl; HFIPA: hexafluoroisopropyl alcohol; HMPA: hexamethylphosphoramide; JohnPhos: (2-biphenyl)di-tert-butylphosphine; Josiphos: 1-[2-(diphenylphosphino)ferrocenyl]ethyldicyclohexylphosphine ethanol adduct; L: ligand; Mandyphos: 1,1′-bis[(dimethylamino)benzyl]-2,2′-bis(diphenylphosphino)ferrocene; Me-DuPhos: 1,2-bis(2,5-dimethylphospholano)benzene; MOM: methoxymethyl; Ms: mesyl; MS: molecular sieves; MTBE: methyl tert-butyl ether; Naph: naphthyl; NBS: N-bromosuccinimide; Ns: nosyl (4-nitrobenzenesulfonyl); Oct: octyl; Pent: pentyl; Phos: phosphinyl; Phox: phosphinooxazoline; Pin: pinacolato; PG: protecting group; Phth: phthalimido; Piv: pivaloyl; PMB: p-methoxybenzyl; PMP: 1,2,2,6,6-pentamethylpiperidine; PTAD: 4-phenyl-1,2,4-triazoline-3,5-dione; Py: pyridyl; Pybox: 2,6-bis(2-oxazolyl)pyridine; QUINOX: (quinolin-2-yl)-oxazoline; rs: regioselectivity ratio; r.t.: room temperature; SDS: sodium dodecyl sulfate; Segphos: 5,5′-bis(diphenylphosphino)-4,4′-bi-1,3-benzodioxole; SES: β-trimethylsilylethanesulfonyl; Taniaphos: [2-diphenylphosphinoferrocenyl](N,N-dimethylamino)(2-diphenylphosphinophenyl)methane; TBS: tert-butyldimethylsilyl; TEA: trimethylamine; Tf: trifluoromethanesulfonyl; TFA: trifluoroacetic acid; THF: tetrahydrofuran; TIPS: triisopropylsilyl; TMG: 1,1,3,3-tetramethylguanidine; TMS: trimethylsilyl; Tol: tolyl; Ts: 4-toluenesulfonyl (tosyl); VANOL: 3,3′-diphenyl-2,2′-bi-1-naphthol; Walphos: 1-{2-[2′-(diphenylphosphino)phenyl]ferrocenyl}ethyldi[3,5-bis(trifluoromethyl)phenyl]phosphine; Xyl: 3,5-dimethylphenyl.

Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 3. Structure-activity relationships of fused rings at the 7,8-positions.

Abstract: As a continuation of our efforts to discover and develop the apoptosis-inducing 4-aryl-4H-chromenes as novel anticancer agents, we explored the SAR of fused rings at the 7,8-positions. It was found that a five-member aromatic ring, such as pyrrolo with nitrogen at either the 7- or 9-position, is preferred. A six-member aromatic ring, such as benzo or pyrido, also led to potent compounds. The SAR of the 4-aryl group was found to be similar for chromenes with a fused ring at the 7,8-positions. These compounds were found to inhibit tubulin polymerization, indicating that cyclization of the 7,8-positions into a ring does not change the mechanism of action. Compound 2h was identified to be a highly potent apoptosis inducer with an EC 50 of 5 nM and a highly potent inhibitor of cell proliferation with a GI 50 of 8 nM in T47D cells.

Discovery of Novel, Potent, and Selective Small-Molecule CCR5 Antagonists as Anti-HIV-1 Agents: Synthesis and Biological Evaluation of Anilide Derivatives with a Quaternary Ammonium Moiety

Abstract: The search for new small-molecule CCR5 antagonists by high-throughput screening (HTS) of the Takeda chemical library using [125I]RANTES and CHO/CCR5 cells led to the discovery of lead compounds (A, B) with a quaternary ammonium or phosphonium moiety, which were synthesized to investigate new MCP-1 receptor antagonists. A series of novel anilide derivatives 1 with a quaternary ammonium moiety were designed, synthesized, and tested for their CCR5 antagonistic activity. Through the optimization of lead compounds, we have found N,N-dimethyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl]carbonyl]amino]benzyl]tetrahydro-2H-pyran-4-aminium chloride (1r, TAK-779) as a highly potent and selective nonpeptide CCR5 antagonist with a IC50 value of 1.4 nM in the binding assay. Compound 1r also inhibited the replication of macrophage (M)-tropic HIV-1 (Ba-L strain) in both MAGI-CCR5 cells and PBMCs with EC50 values of 1.2 and 3.7 nM, respectively. The synthesis and structure−activity relationships of 1r...

Substituted alpha-l-bicyclic nucleosides

Abstract: The present disclosure describes substituted α-L-bicyclic nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, substituted α-L-bicyclic nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.