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Synthesis and SOD activity of manganese complexes of substituted pyridino pentaaza macrocycles that contain axial auxiliary

New manganese(II) complexes of substituted pyridino pentaaza macrocyclic ligands were prepared. The amino-, carboxy-, or other functional groups were placed in the vicinity of the axial position of the metal complex. Their SOD-like activity was determined by cytochrome c assay and compared with one another. The activities of pyridine analogs (12a-b and 13) and m-substituted analogs (12c and 12j) were similar and significantly better than that of the standard compound M-40403. The most potent compound was an o-aminobenzoyl derivative 12i, while the o-carboxybenzoyl analog 12d was the lowest active compound.

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Chiral Catalysts,
Chiral catalysts – SlideShare

 

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Reaction of alkynyl alkoxy metal carbene complexes with 1,2-diamines

Reaction of alkynyl alkoxy carbenes 1 with 1,2-primary and secondary diamines is discussed. The descriptions of mono and biscarbene amino complexes and the effect of the reaction conditions, esteric and electronic factors on the product distribution are also discussed. Changes in the reaction conditions were found to effect greatly the resulting products.

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Chiral Catalysts,
Chiral catalysts – SlideShare

 

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Synthesis and evaluation of series of diazine-bridged dinuclear platinum(II) complexes through in vitro toxicity and molecular modeling: Correlation between structure and activity of pt(II) complexes

Polynuclear Pt(II) complexes are a novel class of promising anticancer agents with potential clinical significance. A series of pyrazine (pz) bridged dinuclear Pt(II) complexes with general formulas {[Pt(L)Cl]2(mu-pz)}2+ (L, ethylenediamine, en; (¡À)-1,2-propylenediamine, 1,2-pn; isobutylenediamine, ibn; trans-(¡À)-1,2-diaminocyclohexane, dach; 1,3-propylenediamine, 1,3-pd; 2,2-dimethyl-1,3-propylenediamine, 2,2-diMe-1,3-pd) and one pyridazine (pydz) bridged {[Pt(en)Cl]2(mu-pydz)}2+ complex were prepared. The anticancer potential of these complexes were determined through in vitro cytotoxicity assay in human fibroblasts (MRC5) and two carcinoma cell lines (A375 and HCT116), interaction with double stranded DNA through in vitro assay, and molecular docking study. All complexes inhibited cell proliferation with inhibitory concentrations in the 0.5-120 muM range. While {[Pt(1,3-pd)Cl]2(mu-pz)}2+ showed improved activity and {[Pt(en)Cl]2(mu-pydz)}2+ showed comparable activity to that of clinically relevant cisplatin, {[Pt(en)Cl]2(mu-pydz)}2+ was less toxic in an assay with zebrafish (Danio rerio) embryos, causing no adverse developmental effects. The in vitro cytotoxicity of all diazine-bridged dinuclear Pt(II) complexes is discussed in correlation to their structural characteristics.

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Chiral Catalysts,
Chiral catalysts – SlideShare

 

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The role of chelating diamine ligands in the Goldberg reaction: A kinetic study on the copper-catalyzed amidation of aryl iodides

The mechanistic details of the Cu-catalyzed amidation of aryl iodides are presented. The kinetic data suggest that the diamine ligand prevents multiple ligation of the amide. The formation of an amidocuprate species external to the catalytic cycle helped to rationalize the dependence on diamine concentration and the inverse dependence on amide concentration at low diamine concentrations. The intermediacy of a Cu(I) amidate was established through both its chemical and kinetic competency. Copyright

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Chiral Catalysts,
Chiral catalysts – SlideShare

 

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Synthesis and structure elucidation of pyrimidobenzimidazoles and fused derivatives II [1]. Dodecahydrobenzimidazo-[2,1-b]quinazolines and decahydrobenzimidazo-[2,1-b]benzo[h]quinazolines [2]

The cyclization reactions of trans-3a-hexahydro-2-benzimidazolamine with 2-alkylidene-and 2-benzylidenecyclohexanones and alpha-tetralones, respectively, yield mixtures of two isomeric condensates each. Thorough high resolution NMR analyses (1H and 13C NMR, HH-COSY, gs-HSQC, gs-HMBC, 1D TOCSY, and 1D NOE difference spectra) revealed that the corresponding isomers are in all cases linearly fused diastereomeric 12alpha-and 12beta-substituted trans-6aalpha-dodecahydrobenzimidazo[2,1-b]quinazolines and 7alpha-substituted trans-8abeta-and trans-8aalpha-decahydrobenzimidazo[2,1-b]benzo[h]quinazolines, respectively. The formation of corresponding angularly fused regioisomers was not observed so far. The stereochemistry and the tautomerism of some bases and their hydrochlorides as well as the regiospecific course of the cyclization reactions are discussed. Biological tests showed that the novel compounds don’t exert remarkable antibacterial and antimycotic effects.

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Chiral Catalysts,
Chiral catalysts – SlideShare

 

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A convenient synthesis of (Z)-3-(alpha-Cyano-alpha-alkoxy-carbonylmethylene)- 2-piperazinones and their derivatives

(Z)-3-(alpha-Cyano-alpha-alkoxycarbonylmethylene)-2-piperazinone derivatives (3) and trans-(Z)-3-(alpha-cyano-alpha-alkoxycarbonylmethylene)octahydro-2(1H)- quinoxalinone derivatives (5) possessing various alkoxycarbonyl groups are prepared directly from the reaction of dialkyl (E)-2,3-dicyanobutenedioates (1) with ethylenediamine (2) and with trans-1,2-diaminocyclohexane (4), respectively. Furthermore, cis-1,2-diaminocycloheptane (6) and meso-2,3- diaminobutane (8) were reacted with the diethyl ester 1b to give cis-(Z)-3- (alpha-cyano-alpha-ethoxycarbonylmethylene)decahydro-2H-cycloheptapyrazin-2-one (7) and cis-(Z)-3-(alpha-cyano-alpha-ethoxycarbonylmethylene)-5,6-dimethyl-2- piperazinone (9), respectively. The structural studies of 3, 5, 7, and 9 were carried out by NMR experiments in some details.

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Chiral Catalysts,
Chiral catalysts – SlideShare

 

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 1436-59-5, Name is cis-Cyclohexane-1,2-diamine, molecular formula is C6H14N2. In a Article£¬once mentioned of 1436-59-5, Recommanded Product: cis-Cyclohexane-1,2-diamine

Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors

A novel series of CHK1 inhibitors based on thienopyridine template has been designed and synthesized. These inhibitors maintain critical hydrogen bonding with the hinge and conserved water in the ATP binding site. Several compounds show single digit nanomolar CHK1 activities. Compound 70 shows excellent enzymatic activity of 1 nM.

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Chiral Catalysts,
Chiral catalysts – SlideShare

 

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Consistent supramolecular assembly arising from a mixture of components-self-sorting and solid solutions of chiral oxygenated trianglimines

The [3 + 3] cyclocondensation of either oxygen or methoxy group-containing terephthalaldehydes with optically pure vicinal diamines provides triangular macrocycles, whose constitution and symmetry depend on the structure of the aldehyde substrate. Formation of hexa-oxygenated trianglimine is highly stereoselective: that is, the use of racemic diamine yields a racemic mixture of homochiral triangular macrocycles, each having the same absolute configuration at all stereogenic centers. However, no self-sorting is observed when a mixture of non-, mono- and di-oxygenated dialdehydes is subjected to the cyclocondensation reaction with the optically pure diamine. In crystals, the variously oxygenated trianglimines consistently assemble into chiral columnar aggregates and form two- or three-component solid solutions. Some of these assemblies exhibit intracolumnar and/or intercolumnar inclusion properties. While the tris-oxygenated trianglimine crystallizes as a solid solution of molecular isomers, a mixture of uniformly chiral macrocycles that are built of variously oxygenated aldehyde sub-units provides a ternary solid solution deprived of any solvent molecules. For racemic trianglimine, formation of supramolecular columnar assemblies is accomplished by enantioselective self-recognition.

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Chiral Catalysts,
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Synthesis of monoacylated derivatives of 1,2- cyclohexanediamine. Evaluation of their catalytic activity in the preparation of Wieland-Miescher ketone

Ureas, carbamoyl derivatives, amides, and sulfonamides can be easily prepared from the strained (R,R)-cylohexanediamine urea (1) in high yield, leaving a free amino group that shows good catalytic activity in intramolecular aldol condensations. The preparation of Wieland-Miescher ketone has been studied with these catalysts.

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Chiral Catalysts,
Chiral catalysts – SlideShare

 

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An efficient and convenient protocol for the synthesis of quinoxalines and dihydropyrazines via cyclization-oxidation processes using HClO4¡¤SiO2 as a heterogeneous recyclable catalyst

A convenient and straightforward method has been developed for the synthesis of quinoxalines and dihydropyrazines (DHPs) using alpha-bromo ketones and 1,2-diamines in the presence of silica supported perchloric acid (HClO4¡¤SiO2) at room temperature. The quinoxalines and DHPs were presumably formed via cyclization-oxidation. The catalyst works under heterogeneous conditions and can be recycled.

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Chiral Catalysts,
Chiral catalysts – SlideShare