Synthesis of N-(trifluoromethyl-2-pyridinyl)arenesulfonamides as an inhibitor of secretory phospholipase A₂

A series of N-(trifluoromethyl-2-pyridinyl)alkane- and arenesulfonamides 2-5 have been synthesized by the substitution reaction of 2-chloro(trifluoromethyl)pyridines 6 with alkane- and arenesulfonamides 7. Their inhibitory activities against secretory phospholipase A? of porcine pancreas were examined and the analog N-[4,5-bis(trifluoromethyl)-2-pyridinyl]-4-trifluoromethylbenzenesulfonamide 4i was shown to have the highest inhibitory activity, with an IC(50) value of 0.58 mM.     

Synthesis of tanshinone ⅡA analogues and their inhibitory activities against Cdc25 phosphatases

Two series of tanshinone IIA derivatives were synthesized and evaluated for their antitumor activities as Cdc25 phosphatase inhibitors. Most of them demonstrated potent Cdc25 inhibitory activity and powerful cytotoxicity against A549 tumor cell line, producing IC₅₀ values in very low micromolar range. At last, the preliminary SAR was discussed.     

Synthesis,structure, DNA-binding,and cytotoxic activities of N-(5-chloro-2-hydroxyphenyl)-N′-[3-(2-hydroxyethylamino)propyl]oxamide and its dicopper(II) complex

A dissymmetrical N,N′-bis(substituted)oxamide, N-(5-chloro-2-hydroxyphenyl)-N′[3-(2-hydroxyethylamino)propyl]oxamide (H₃oxpep), and its dicopper(II) complex, [Cu₂(oxpep)(phen)]ClO₄ (1) (phen?=?1,10-phenanthroline), were synthesized. The crystal structure of 1 was determined by single-crystal X-ray diffraction. In 1, Cu1 and Cu2 are bridged by cis-oxpep^3? with Cu?···?Cu separation of 5.2007(6)?Å. Cu1 is in a distorted square-pyramidal environment, while Cu2 has a square-planar coordination geometry. The 3-D supramolecular structure of 1 is formed through π–π stackings and hydrogen bonds. The DNA-binding properties and cytotoxic activities of the two compounds were investigated. The results suggest that the two compounds can interact with HS-DNA by intercalation with binding affinities following the order 1?>?H₃oxpep, which is consistent with their anticancer activities.     

Synthesis of 3-Substituted-6-(2,4-Dichlorophenyl)-s-Triazolo[3.4-b]-1,3,4-Oxadiazoles

2,5-DisubstitUted-l,3,4-oxadiazolederivativeshavebeenrePort6dtoshowantidrigal1,antiin-flamrnatoof,andplantgrowthpromoter3activities-3,4-Disubstituted-l,2,4-triazolecompoundsalsopossessantifimgal',andplantgrowthpromote/achvities.Authors6havereportedthat(3-bmpl4-aroyl-l,2,4-triazole-5-yl)[5-(3,4,5-triInethoxylphenyl>l,3,4roxadiazole-2-yl]sulfidesshowedsomeantifungalactivity.lnordertoscreennewcompoundsofpossessingphysiologicalactivity'andstUdythereactionruleofnucleophilicdisplacementwehavedevelo…     

Synthesis and Herbicidal Activity of 2-Benzoyliminopyrimido[3,2-b]-1 2,4-Thiadiazolines

SincethesynthesisandherbicidalactivityofDPX-4l89wasreportedinl98o,awidevarietyofsulfonylureaswithimprovedselectivityand/oreffectivenesshavebeendeveloped'-'.Inacontinuingstudyonthesynthesisandherbicidalactivityofthiophenesulfonylureaandsubstitutedbenzenesulfonylureaderivatives'-',wehavefoundthatsulfonylureaherbicideshaveexcellentherbicidalactivityagainstawiderangeofweeds,butmostofthemwerenotselectivelyactiveherbicides.Inthispaperwedescribethesynthesisandherbicidalactivityofthirteen3-benzoly-l-…     

Synthesis of N-(2-chloroethyl)isatins and their β-ethyleneacetals and β-thiosemicarbazones

The nitrogen atoms of isatin, its 5-bromoderivative, and their -ethyleneacetals are alkylated by 1,2-dichloroethane in K₂CO₃–DMF and LiH(NaH)-DMF.Institute of Biological Protection of Plants and Institute of Chemistry of the Moldovan Academy of Sciences, Kishinev 2058. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 907–909, July, 1999.     

Synthesis and Crystal Structure of Bis[2-[2-(diethylamino)ethyliminomethyl]-4-nitrophenolato]dimethanolcobalt(II) Dinitrate

1 INTRODUCTION The significance of cobalt coordination com- pounds in biological systems is recognized[1～3]. In many instances the cobalt coordination compounds of Schiff bases have been suggested as models to describe energy transfer in naturally occurring systems. In such cases the coordination sphere about the metal ion is believed to play an important role in determining the nature of the model system[4, 5]. In order to investigate the structures of such complexes, we report herein t…     

Synthesis and cyclization of N-(2-hydroxyphenyl)-and N-(2-benzyloxyphenyl)-Β-alanines

N-Substituted -alanines have been synthesized by treating o-aminophenol or o-benzyloxyaniline with acrylic, methacrylic, or crotonic acids. Their cyclization to 2-benzoxazolinones and dihydro-2,4(1H,3H)-pyrimidinediones has been studied.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 527–531, April, 1991.     

Use of solvent isotope effect to identify an intermediate carbanion in the β-elimination reactions from N-[2-(4-pyridyl)ethyl]quinuclidinium and N-[2-(2-pyridyl)ethyl]quinuclidinium induced by acetohydroxamate/acetohydroxamic acid buffers

Solvent isotope effect is a useful technique for identifing and characterizing an intermediate carbanion in the base-induced -elimination reaction from N-[2-(4-pyridyl)ethyl]quinuclidinium, 1, and N-[2-(2-pyridyl)ethyl]quinuclidinium, 2. While at high [buffer]k _obs(D₂O) > k _obs(H₂O) due to the presence of a primary kinetic solvent isotope effect on the reprotonation of the intermediate carbanion by BD, at low [buffer] no solvent isotope effect is observed, and k _obs(D₂O) k _obs(H₂O). The data are in agreement with a reversible E1cb mechanism in which carbon deprotonation occurs from NH⁺, the substrate protonated at the nitrogen atom of the pyridine ring. In the absence of solvent isotope effect at low [buffer], and with the similarity of the results obtained with the two isomers, 1 and 2, the significance of an intramolecular proton transfer in the intermediate carbanion can be excluded in these processes.     

Synthesis and chemistry of tris(2-pyridyl)phosphine and bis(2-pyridyl)phenylphosphine complexes of mercury(II) X (X = Br,Cl) and X-ray crystal structural determination of [HgBr2(PPh(2-py)2)2]

Mercury(II) halide complexes [HgX₂(P(2-py)₃)₂] (X?=?Br (1), Cl (2)) and [HgX₂(PPh(2-py)₂)₂] (X?=?Br (3), Cl (4)) containing P(2-py)₃ and PPh(2-py)₂ ligands (P(2-py)₃ is tris(2-pyridyl)phosphine and PPh(2-py)₂ is bis(2-pyridyl)phenylphosphine) were synthesized in nearly quantitative yield by reaction of corresponding mercury(II) halide and appropriate ligands. The synthesized complexes are fully characterized by elemental analysis, melting point determination, IR, ¹H, and ³¹P-NMR spectroscopies. Furthermore, the crystal structure of [HgBr₂(PPh(2-py)₂)₂] determined by X-ray diffraction is also reported.     

Synthesis of 3-[tris(ψ-trifluoropropyl)sily]propyldimethylsilane

Monofunctional silane containing a tris(ψ-trifluoropropyl) fragment was synthesized in high yield by a series of successive reactions including the Grignard reaction, hydrosilylation, and reduction. Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 4, pp. 808–809, April, 1999.     

Synthesis of stereospecifically labeled carbohydrates: Preparation of (3S)− and (3R)-[3-2H1]ascarylose

The general problem of the synthesis of 3,6-dideoxy sugars containing stereospecifically labeled hydrogen isotope at C-3 is addressed for the specific case of ascarylose (3,6-dideoxy-L-arabino-hexose).     

Synthesis and spectroscopic characterization of new heteroleptic ruthenium(II) complexes incorporating 2-(2′-pyridyl)quinoxaline and 4-carboxy-2-(2′-pyridyl)quinoline

Starting from cis-[Ru(dcbpyH₂)₂Cl₂] (1), two new heteroleptic ruthenium(II) complexes, [Ru(dcbpyH₂)₂(L¹)](NO₃)₂ (L^1?=?2-(2′-pyridyl)quinoxaline (2), and [Ru(dcbpyH₂)₂(L²)](NO₃)₂ (L^2?=?4-carboxy-2-(2′-pyridyl)quinoline (4); dcbpyH_2?=?2,2′-bipyridine-4,4′-dicarboxylic acid), were synthesized and spectroscopically characterized. During the preparation of 2 and 4, the homoleptic [Ru(dcbpyH₂)₃]Cl₂ complex (3) was isolated as a side product. Characterization includes IR and Raman spectroscopy, UV-Vis, multinuclear NMR spectroscopy, elemental, and ESI-mass spectrometric analyses.     

Synthesis and Chiroptical Properties of Poly[N-(4-N′-(α-Methylbenzyl)-Aminocarbonylphenyl)-Mamaleimide]

Abstract

Radical homopolymerization of N-[4-N′-(α-methylbenzyl)-aminocarbonylphenyl]maleimide ((S)-MBCP) was carried out at 50 and 70°C for 24 h to give optically active polymers ([α]²⁵ _D = 159.8 to 163.4°). Radical copolymerizations of (S)-MBCP (M₁) were performed with styrene (ST, M₂, methyl methacrylate (MMA, M²) in THF at 50°C. The monomer reactivity ratios (r ₁, r ₂) and the Alfrey-Price Q, e values were determined as follows: r ₁ = 0.32, r ₂= 0.14, Q ₁ = 1.74, e ₁ = 0.96 in the (S)-MBCP-ST system; r ₁ = 0.54, r ₂ = 0.93, Q ₁ = 1.11, e ₁ = 1.23 in the (S)-MBCP-MMA system. Chiroptical properties of the polymers and the copolymers were also investigated, and asymmetric induction into the copolymer main chain is discussed.     

Synthesis and Crystal Structure of (E)-[1-Ferrocenyl-2-(4-Chlorophenyl) ethylene]

1INTRoDUCTIoNCurrently,thereisaconsiderableinterestintheinvestigationoforganicandorganometallicmaterialsshowinglargenonlinearopticalresponse.Theirpotentialusehasbeenresearchedindeviceapplicationswhicharerelatedtothetelecommuni-cations,opticalcomputingandopticalinformationprocessing"2i.Onamicroscopiclevel,oneofthemajorphysicalparameterstodecidethenonlinearopticalpropertiesofmaterialsisthemolecularhyperpolarizability,avaluedeterminedbyelectronicandgeometricstructureofmolecule.Thetitlecompoun…     

Synthesis and Crystal Structure of [Pd(NH_3)_4]Cl_2·2[Pd(NH_3)_3Cl]Cl

PreparahonofsomecomplexcomPOundsof[Pd(NH3)41X2tw,tvhereX=Cl-,Br,I-,X2=Co,:-,RdChl'-,etc.,wasdescribedasearlyl942l'].SynthesisandcryStalstIUCtUreOfthesaltSt'ithamons,Cr2o7",Cro.:',MoO"',andC,o'=',ttcrestillreportedmorcrecenh/'-'j.IPd(NH)4lX2,tvhereX=Cl',BrandNOz,isanotherkindofamndnepalladiumcomplexcompounds.IntheSyStemofIPd(NH).1"-Cl'-H2o,diamlltinedichloridepalladium(II)wasObtalnedbythereachonOfIPd(NH)4lHcomplexionwtthanutebydrogenchloride,andtetrachloridepalladiumaDbythe…     

Synthesis and characterisation of [tris(1,3-dithiole-2-thione-4,5-dithiolato)-stannate]2−, [Q]2[Sn(dmit)3], [tris(1,3-dithiole-2-one-4,5-dithiolato)stannate]2−, [Q]2[Sn(dmio)3] and [tris(1,3-dithiole-2-thione-4,5-selenolato)stannate]2−, [Q]2[Sn(dsit)3], complexes: Analysis of the structural variations of the [Sn(dmit)3]2− and [Sn(dmio)3]2− dianions

[Tris(1,3-dithiole-2-thione-4,5-dithiolato)stannate]²⁻, [Q]₂[Sn(C₃S₅)₃], [tris(1,3-dithiole-2-one-4,5-dithiolato)stannate]²⁻, [Q]₂[Sn(C₃S₄O)₃], and [tris(1,3-dithiole-2-thione-4,5-diselenolato)stannate]²⁻ [Q]₂[Sn(C₃S₃Se₂)₃], complexes, have been synthesised and characterised. Crystal structure determinations of [Q]₂[Sn(C₃S₅)₃] (Q=1,4-dimethylpyridinium, monoclinic and orthorhombic forms; NMe₄, NEt₄, and PPh₄) and [NEt₄]₂[Sn(C₃S₄O)₃] revealed variations in the overall dianion structures. The geometry about tin in each case is essentially octahedral with the chelate bite angles in the range 80.7(5)–87.45(4)°: the range of Sn–S distances is 2.5207(18)–2.571(17) Å. A statistical analysis, carried out on the crystal structure data for the six complexes, indicated that the most critical factors in controlling the overall shape of the dianion were the distances of the Sn atom from the dithiolate ligand planes [Sn–OOP]. Interanionic S⋯S interactions, within the sum of the van der Waals’ radii for two S atoms, are affected by the size of the cation, Q; the secondary connectivity is 3-dimensional for the smallest cations, Q=1,4-dimethylpyridinium and NMe₄, in chains for the somewhat larger cation, NEt₄ and is absent for the still larger, PPh₄ cation.     

Crystal Structure and Antitumor Activity of Tri[2- [N-(4''''-methyl-benzylsulfonyl)amino]ethyl]-amine

1 INTRODUCTION The supramolecular architectures of tripodal ligands with special cavities have attracted much attention of chemists and biochemists because of their interesting structures and possible properties such as ion and molecular recognition, selective inclusion and important biological function[1～5]. However, their potential applications in supra- molecular and biological chemistry for constructing various complexes have not been clearly realized until recent years. Few crystal…     

Synthesis and structure of oxacalix[2]arene[2]triazines of an expanded π-electron-deficient cavity and their interactions with anions

Novel macrocyclic anion receptors based on the principle of anion-π interactions were reported. By means of both post-macrocyclization modification protocol and the stepwise fragment coupling approach, functionalized oxacalix[2]arene[2]triazines bearing two other electron-deficient (hetero)aromatic rings on the lower rim were efficiently synthesized. The resulting oxacalix[2]arene[2]triazine macrocyclesadopt 1,3-alternate conformation, yielding therefore an expanded electron-deficient cavity or space consisting of two triazine rings and two appending aromatic rings. Spectroscopic titration study showed the selective interaction of the pentafluorophenyl-substituted oxacalix[2]arene[2]triazine with azide and fluoride in solution with the binding constants (K(1:1)) ranging from 1.33 × 10(3) to 3.52 × 10(3) M(-1).