bluuebunny/crossref_metadata_2025_split huggingface dataset:
Phenotypic variability in bioprocessing conditions can be tracked on the basis of on‐line flow cytometry and fits to a scaling law
Authors: Baert Jonathan , Kinet Romain , Brognaux Alison , Delepierre Anissa , Telek Samuel , Sørensen Søren J. , Riber Leise , Fickers Patrick , Delvigne Frank 
Published: July 2015

AbstractNoise in gene and protein expression is a major cause for bioprocess deviation. However, this phenomenon has been only scarcely considered in real bioprocessing conditions. In this work, a scaling‐law derived from genome‐scale studies based on GFP reporter systems has been calibrated to an on‐line flow cytometry device, allowing thus to get an insight at the level of promoter activity and associated noise during a whole microbial culture carried out in bioreactor. We show that most of the GFP reporter systems investigated and thus corresponding genes could be included inside the area covered by the scaling‐law. The experimental results suggest that this scaling‐law could be used to predict the dynamics of promoter activity, as well as the associated noise, in bioprocessing conditions. The knowledge acquired throughout this work could be used for the design of more robust expression systems.
Spectrophotometric Determination of Affinities of α‐Factors for Their G Protein‐Coupled Receptors in Saccharomyces cerevisiae
Authors: Ahn Hee Jun , Kim Hyung Jin , Jin Dong Hoon , Hong Nam Joo 
Published: July 2015

A new and relatively simple spectrophotometric technique has been developed for the accurate determination of α‐factor pheromone affinities for Ste2p whole cell receptor in yeast a‐cells. We designed and tested nine detector peptides containing mono‐ (ε412 = 14 500) or tri‐cysteine residues (ε412 = 43 660). The free unbound detector was detected using Ellman's reagent at 412 nm. Saturation binding studies using Saccharomyces cerevisiae Y 7925 (
MATa
) at a concentration of 2.5 × 1011 cells/mL with the highest affinity detector 1, [Orn6]α‐factor‐[Cys]3, resulted in a dissociation constant (
K
D
) of 1.67 × 10−7 and total binding sites per cell (B
cell = 29 500 sites/cell) comparable with those obtained using radiolabeled binding assays. Competitive binding assay using five nonchromogenic α‐factor analogs allowed for the determination of each
K
D
value. [Orn6,d‐Ala9]α‐factor showed the highest receptor affinity (
K
D
= 1.03 × 10−7 M), which was threefold higher than that of native α‐factor. This assay provides rapid and convenient results for determining the relative affinities of nonchromogenic α‐factors and eliminates the need for radioactive waste disposal.
An efficient in vitro and in vivo HPLC method for hydnocarpin in nanomicelles formulation
Authors: Feng Yingshu , Sun Congyong , Omari‐Siaw Emmanuel , Zhu Yuan , Tong Shanshan , Wan Jinyi , Yu Jiangnan , Xu Ximing 
Published: July 2015

AbstractFor quantitative and other related bioactive studies of hydnocarpin, there is a need to establish an efficient, specific and sensitive analytical method (in vitro and in vivo). In this paper, an efficient HPLC method has been established and validated to analyze hydnocarpin in a nanomicelle formulation for the first time. Various chromatographic conditions for in vitro and in vivo determinations were investigated, with the application examined by pharmacokinetics and tissue distribution studies. The analysis was carried out using an HPLC system with a Waters symmetry C18 column (4.6 × 150 mm, 5 µm) at 25°C with a detecting wavelength of 342 nm. Eluting at a rate of 1.0 mL/min, a 65% methanol and 35% acetic acid solution (0.1%) served as the mobile phase for the in vitro determinations while a 62% methanol and 38% acetic acid solution (0.1%) was used for in vivo analysis with isoliquiritigenin as internal standard. The established in vitro linearity range for hydnocarpin was 0.2–20 µg/mL (R2 = 0.9996), with the biological (in vivo) samples following the same trend. The accuracy of the method was >99% (in vitro) and 92.4–105.3% (in vivo). Also, the precision met the acceptance criterion. These results indicate that the established method exhibited high specificity, accuracy, linearity and precision. Additionally, this efficient HPLC method was applied to pharmacokinetics and tissue distribution studies. Copyright © 2015 John Wiley & Sons, Ltd.
Essential Oils and Chemical Diversity of Southeast European Populations of Salvia officinalis L.
Authors: Cvetkovikj Ivana , Stefkov Gjoshe , Karapandzova Marija , Kulevanova Svetlana , Satović Zlatko 
Published: July 2015

AbstractThe essential oils of 25 populations of Dalmatian sage (Salvia officinalis L.) from nine Balkan countries, including 17 indigenous populations (representing almost the entire native distribution area) and eight non‐indigenous (cultivated or naturalized) populations were analyzed. Their essential‐oil yield ranged from 0.25 to 3.48%. Within the total of 80 detected compounds, ten (β‐pinene, 1,8‐cineole, cis‐thujone, trans‐thujone, camphor, borneol, trans‐caryophyllene, α‐humulene, viridiflorol, and manool) represented 42.60 to 85.70% of the components in the analyzed essential oils. Strong positive correlations were observed between the contents of trans‐caryophyllene and α‐humulene, α‐humulene and viridiflorol, and viridiflorol and manool. Principal component analysis (PCA) on the basis of the contents of the ten main compounds showed that four principal components had an eigenvalue greater than 1 and explained 79.87% of the total variation. Performing cluster analysis (CA), the sage populations could be grouped into four distinct chemotypes (A–D). The essential oils of 14 out of the 25 populations of Dalmatian sage belonged to Chemotype A and were rich in cis‐thujone and camphor, with low contents of trans‐thujone. The correlation between the essential‐oil composition and geographic variables of the indigenous populations was not significant; hence, the similarities in the essential‐oil profile among populations could not be explained by the physical proximity of the populations. Additionally, the southeastern populations tended to have higher EO yields than the northwestern ones.
Expanding the Genetic Code for a Dinitrophenyl Hapten
Authors: Ren Wei , Ji Ao , Wang Michael X. , Ai Hui‐wang 
Published: July 2015

AbstractHaptens, such as dinitrophenyl (DNP) are small molecules that induce strong immune responses when attached to proteins or peptides and, as such, have been exploited for diverse applications. We engineered a Methanosarcina barkeri pyrrolysyl‐tRNA synthetase (mbPylRS) to genetically encode a DNP‐containing unnatural amino acid, N6‐(2‐(2,4‐dinitrophenyl)acetyl)lysine (DnpK). Although this moiety was unstable in Escherichia coli, we found that its stability was enhanced in mammalian HEK 293T cells and was able to induce selective interactions with anti‐DNP antibodies. The capability of genetically introducing DNP into proteins is expected to find broad applications in biosensing, immunology, and therapeutics.
Hydrogenation of Nitrobenzene over a Pd/Al2O3 Catalyst – Mechanism and Effect of the Main Operating Conditions
Authors: Couto Clara Sá , Madeira Luis M. , Nunes Clemente Pedro , Araújo Paulo 
Published: July 2015

AbstractThe catalytic hydrogenation of nitrobenzene (NB) was studied in a three‐phase basket reactor with a commercial Pd/Al2O3 sample as catalyst. The kinetic experiments allowed a better understanding of the mechanism behind the formation of aniline (ANL) and by‐products, a topic not yet well comprehended. The effect of some operating conditions was studied and the existence of more by‐products than mentioned in the literature was stated; specifically, benzene formation was verified. Both the reaction kinetics and selectivity were found to be strongly dependent on the temperature, while the effect of total pressure is not that pronounced. Moreover, the high selectivity of the catalyst used in the present work was proved, and as such the deep hydrogenation of ANL to form by‐products only occurs in considerable extension when the NB concentration in the reaction mixture becomes negligible.
ChemInform Abstract: Crystal Structure of Ba5In4Sb6.
Authors: Pan Ming‐Yan , Xia Sheng‐Qing , Tao Xu‐Tang 
Published: July 2015

AbstractSingle crystals of Ba5In4Sb6 are grown from a reactive indium flux using a molar mixture of Ba:In:Sb of 3:30:5 (alumina crucible, 1173 K, 20 h; cooling to 773 K at a rate of 2 k/h).
ChemInform Abstract: Preparation of p‐Type AgCrO2 Nanocrystals Through Low‐Temperature Hydrothermal Method and the Potential Application in p‐Type Dye‐Sensitized Solar Cell.
Authors: Xiong Dehua , Wang Huan , Zhang Wenjun , Zeng Xianwei , Chang Haimei , Zhao Xiujian , Chen Wei , Cheng Yi‐Bing 
Published: July 2015

AbstractPhase‐pure AgCrO2 nanocrystals 10‐20 nm in size are hydrothermally grown from aqueous solutions of AgNO3, Cr(NO3)3, and NaOH as mineralizer (autoclave, 190‐230 °C, 60 h).
ChemInform Abstract: Honeycomb‐Like Macro‐Germanium as High‐Capacity Anodes for Lithium‐Ion Batteries with Good Cycling and Rate Performance.
Authors: Liang Jianwen , Li Xiaona , Hou Zhiguo , Zhang Tianwen , Zhu Yongchun , Yan Xuedong , Qian Yitai 
Published: July 2015

AbstractMacroporous Ge powder is prepared by reduction of commercial GeO2 with Mg under hydrothermal conditions (autoclave, 200 °C, 5 h).
ChemInform Abstract: Synthesis, Crystal, and Electronic Structure of Ba3Sb2Q7 (Q: S, Se).
Authors: Wang Jian , Lee Kathleen , Kovnir Kirill 
Published: July 2015

AbstractThe new title compounds are synthesized by solid state reactions of stoichiometric mixtures of the elements (773 K for 24 h, 1173 K for 168 h, and 923 K for 96 h) and characterized by single crystal XRD, UV/VIS diffuse reflectance spectroscopy, and quantum chemical TB‐LMTO‐ASA computations.
ChemInform Abstract: Ruthenium‐Catalyzed Synthesis of 2,3‐Cyclo[3]dendralenes and Complex Polycycles from Propargyl Alcohols.
Authors: Thies Nora , Haak Edgar 
Published: July 2015

AbstractMulticomponent cascade transformations of unsaturated alcohols, catalyzed by cyclopentadienone ruthenium complexes, yield complex polycyclic products with up to nine stereogenic centers.
ChemInform Abstract: Conformationally Constrained Penta(hetero)cyclic Molecular Architectures by Photoassisted Diversity‐Oriented Synthesis.
Authors: Umstead Weston J. , Mukhina Olga A. , Kutateladze Andrei G. 
Published: July 2015

AbstractFused hydantoins [(V) and (VI)], oxazolidinones [(X), (XIV), and (XV)], and imidazolines [(XIX) and (XX)] are synthesized through photoinduced intramolecular cycloadditions of appropriate precursors containing acylurea (IV), urethane [(IX) or (XIII), resp.], or urea (XVIII) linkers, respectively.
ChemInform Abstract: Catalytic Aerobic Oxidation of Alcohols Using Recoverable IAPNO α‐Hydrogen Nitroxyl Radicals.
Authors: Bar Sukanta , Kumar Jayprakash N. , Amar Michal , Toledo Hila , Batrice Rami J. , Szpilman Alex M. 
Published: July 2015

AbstractConditions for the oxidation of primary aliphatic, benzylic, allylic, and propargylic alcohols and secondary benzylic alcohols including benzoin in the presence of newly developed stable α‐hydrogen nitroxyl radicals as the catalyst are elaborated.
ChemInform Abstract: Temperature‐Controlled Bidirectional Enantioselectivity in a Dynamic Catalyst for Asymmetric Hydrogenation.
Authors: Storch Golo , Trapp Oliver 
Published: July 2015

AbstractA stereochemically flexible diastereomeric catalyst (I) is prepared and used in the asymmetric hydrogenation of aminocarboxylic acids (II)/(IV) and diester (VI).
ChemInform Abstract: Efficient Asymmetric Transfer Hydrogenation of Ketones in Ethanol with Chiral Iridium Complexes of spiroPAP Ligands as Catalysts.
Authors: Liu Wei‐Peng , Yuan Ming‐Lei , Yang Xiao‐Hui , Li Ke , Xie Jian‐Hua , Zhou Qi‐Lin 
Published: July 2015

AbstractChiral alcohols [(II) and (IV)] are simply and efficiently synthesized with up to 98% e.e.
ChemInform Abstract: Visible‐Light‐Induced Chemoselective Reductive Decarboxylative Alkynylation under Biomolecule‐Compatible Conditions.
Authors: Yang Jie , Zhang Jing , Qi Li , Hu Chenchen , Chen Yiyun 
Published: July 2015

AbstractVarious aryl‐, alkyl‐, and silyl‐substituted alkynes are chemoselectively obtained with excellent functional group compatibility.
ChemInform Abstract: De novo Synthesis of Functionalized 1,3‐Enynes and Extended Conjugated Molecular Systems.
Authors: Rao Maddali L. N. , Dasgupta Priyabrata , Murty Venneti N. 
Published: July 2015

AbstractA new palladium catalyzed reaction of 1,3‐dienyldibromides with triarylbismuths to give a wide range of 1,3‐enynes is demonstrated.
ChemInform Abstract: Copper‐Catalyzed Asymmetric Allylation of Chiral N‐tert‐Butanesulfinyl Imines: Dual Stereocontrol with Nearly Perfect Diastereoselectivity.
Authors: Zhao Yi‐Shuang , Liu Qiang , Tian Ping , Tao Jing‐Chao , Lin Guo‐Qiang 
Published: July 2015

AbstractA BINOL‐derived phosphoramidite ligand is successfully applied in the copper‐catalyzed asymmetric allylation of chiral N‐tert‐butanesulfinyl aldimines (I) and ketimines (IV) leading to homoallylic amines with high diastereoselectivity.
ChemInform Abstract: Condensed‐Phase, Halogen‐Bonded CF3I and C2F5I Adducts for Perfluoroalkylation Reactions.
Authors: Sladojevich Filippo , McNeill Eric , Boergel Jonas , Zheng Shao‐Liang , Ritter Tobias 
Published: July 2015

AbstractTetramethylguanidine and DMSO can be used to prepare the required adducts of type (I), (IX), and (XIV).
ChemInform Abstract: Enantioselective Redox‐Neutral Rh‐Catalyzed Coupling of Terminal Alkynes with Carboxylic Acids Toward Branched Allylic Esters.
Authors: Koschker Philipp , Kaehny Matthias , Breit Bernhard 
Published: July 2015

AbstractThe scalable, highly enantioselective reaction procedure delivers allylic esters with high regioselectivity in favor of the branched vs.
ChemInform Abstract: A Novel Rhodium‐Catalyzed Domino‐Hydroformylation‐Reaction for the Synthesis of Sulphonamides.
Authors: Dong Kaiwu , Fang Xianjie , Jackstell Ralf , Beller Matthias 
Published: July 2015

AbstractAn efficient and highly selective method for the synthesis of sulfonamides by a new domino hydroformylation‐reductive sulfonamidation reaction is presented.
ChemInform Abstract: Microwave‐Assisted Oxidation of Indan‐1‐ones into Ninhydrins.
Authors: Marminon Christelle , Nacereddine Abdelhamid , Bouaziz Zouhair , Nebois Pascal , Jose Joachim , Le Borgne Marc 
Published: July 2015

AbstractThe convenient oxidation using SeO2 as the oxidant tolerates a wide variety of substituents on the aromatic ring.
ChemInform Abstract: Synthesis of Functionalized γ‐Lactone via Sakurai exo‐Cyclization/Rearrangement of 3,3‐Bis(silyl) Enol Ester with a Tethered Acetal.
Authors: Yin Zhiping , Liu Zengjin , Huang Zhenggang , Chu Yang , Chu Zhiwen , Hu Jia , Gao Lu , Song Zhenlei 
Published: July 2015

AbstractAn efficient synthesis of functionalized γ‐lactones is developed.
ChemInform Abstract: Copper‐Mediated Tandem Reaction of β‐Ketoesters/Ketones with Tertiary Amines for the Synthesis of 2,3‐Dihydrofurans.
Authors: Guo Shengmei , Lu Lin , Gong Jiuhan , Zhu Zheng , Xu Feng , Wei Zhenhong , Cai Hu 
Published: July 2015

AbstractA series of β‐keto esters and β‐diketones is examined giving the desired products in moderate to excellent yields.
ChemInform Abstract: Formal anti‐Carbopalladation Reactions of Non‐Activated Alkynes: Requirements, Mechanistic Insights, and Applications.
Authors: Pawliczek Martin , Schneider Tobias F. , Maass Christian , Stalke Dietmar , Werz Daniel B. 
Published: July 2015

AbstractAlkyne systems are designed which are able to undergo a distinct, formal anti‐carbopalladation.
ChemInform Abstract: Broensted Acid‐Catalyzed Enantioselective Synthesis of Isatin‐ Derived N,S‐Acetals.
Authors: Beceno Christian , Chauhan Pankaj , Rembiak Andreas , Wang Ai , Enders Dieter 
Published: July 2015

AbstractThe isatin‐derived N,S‐acetals are synthesized in high yields and high enantioselectivities from nucleophilic addition of thiols to isatin‐derived ketimines using BINOL‐derived phosphoric acid as catalyst.
ChemInform Abstract: Chiral Phosphoric Acid Catalyzed Enantioselective Decarboxylative Alkylation of β‐Keto Acids with 3‐Hydroxy‐3‐indolyloxindoles.
Authors: Tang Xiao‐Dong , Li Shen , Guo Ran , Nie Jing , Ma Jun‐An 
Published: July 2015

AbstractThe method tolerates a variety of aryl, hetaryl, and alkyl β‐keto acids and furnishes the desired 3‐functionalized 3‐indolyloxindoles with an all‐quaternary stereocenter in high yields and enantioselectivities.
ChemInform Abstract: Access to Polysubstituted Indoles or Benzothiophenes via Palladium‐Catalyzed Cross‐Coupling of Furfural Tosylhydrazones with 2‐Iodoanilines or 2‐Iodothiophenols.
Authors: Yin Biaolin , Zhang Xiaoyu , Zhang Xiaoting , Peng Hui , Zhou Wen , Liu Bo , Jiang Huanfeng 
Published: July 2015

AbstractPolysubstituted indoles [(III), (VI), and (IX)] or benzothiophenes (XI) are efficiently synthesized by cross‐coupling of readily available furfural tosylhydrazones [(II), (V), or (VIII), resp.] with 2‐iodoanilines or 2‐iodothiophenol, respectively.
ChemInform Abstract: Asymmetric Dearomatization of Indoles Through a Michael/Friedel—Crafts‐Type Cascade to Construct Polycyclic Spiroindolines.
Authors: Zhao Xiaohu , Liu Xiaohua , Mei Hongjiang , Guo Jing , Lin Lili , Feng Xiaoming 
Published: July 2015

AbstractAsymmetric dearomatization of indoles is achieved by a cascade reaction between isocyanoethylindole and alkylidene malonates catalyzed by a chiral N,N‐dioxide/Mg catalyst.
ChemInform Abstract: Synthesis of Pyrazoles from 1,3‐Diols via Hydrogen Transfer Catalysis.
Authors: Schmitt Daniel C. , Taylor Alexandria P. , Flick Andrew C. , Kyne Robert E. Jr. 
Published: July 2015

AbstractStarting from 2‐alkyl or 2‐aryl substituted 1,3‐diols and alkyl or aryl hydrazines a scalable protocol for the preparation of otherwise hardly accessible 4‐substituted pyrazoles is elaborated.
ChemInform Abstract: Catalytic Cyclization Reactions of Huisgen Zwitterion with α‐Ketoesters by in situ Chemoselective Phosphine Oxide Reduction.
Authors: Fourmy Kevin , Voituriez Arnaud 
Published: July 2015

AbstractThe first examples of catalytic cyclization reactions of the Huisgen zwitterion with α‐ketoesters are described.
ChemInform Abstract: Radical‐Based Route to 2‐(Trifluoromethyl)‐1,3,4‐oxadiazoles and Trifluoromethyl‐Substituted Polycyclic 1,2,4‐Triazoles and Dihydrofurans.
Authors: Qin Ling , Zard Samir Z. 
Published: July 2015

AbstractVarious trifluoromethyl‐substituted structures can be obtained by exploitation of the 2‐(trifluoromethyl)‐1,3,4‐oxadiazolyl‐5‐methyl radical.
ChemInform Abstract: Oxidative Povarov Reaction via sp3 C—H Oxidation of N‐Benzylanilines Induced by Catalytic Radical Cation Salt: Synthesis of 2,4‐Diarylquinoline Derivatives.
Authors: Liu Jing , Liu Fang , Zhu Yingzu , Ma Xingge , Jia Xiaodong 
Published: July 2015

AbstractThe reaction tolerates differently substituted N‐benzylic aniline derivatives and styrene derivatives, but is not applicable to α‐methylstyrene.
ChemInform Abstract: Base‐Promoted Cross‐Dehydrogenative Coupling of Quinoline N‐Oxides with 1,3‐Azoles.
Authors: Chen Xiaopei , Cui Xiuling , Yang Fangfang , Wu Yangjie 
Published: July 2015

AbstractA simple protocol for the preparation of biheteroaryls is developed based on the coupling of substituted quinoline N‐oxides and 1,3‐benzoxazoles.
ChemInform Abstract: Novel One‐Pot Synthesis of 3,4‐Dihydropyrimidin‐2(1H)‐ones and 3,4,7,8‐ Tetrahydroquinazoline‐2,5‐diones Using Pyridinium p‐Toluenesulfonate as Catalyst.
Authors: Khodja Imene Amine , Boulcina Raouf , Debache Abdelmadjid 
Published: July 2015

AbstractSimple and efficient procedure for the synthesis of the title heterocycles (IV) and (VI), resp., using multicomponent reactions are described.
ChemInform Abstract: Direct Introduction of a Naphthalene‐1,8‐diamino Boryl [B(dan)] Group by a Pd‐Catalyzed Selective Boryl Transfer Reaction.
Authors: Xu Liang , Li Pengfei 
Published: July 2015

AbstractThe non‐symmetrical diboron compound, B(pin)—B(dan) (I), is employed as borylating reagent in the Pd‐catalyzed Miyaura‐type reaction.
ChemInform Abstract: Transition‐Metal‐Free Direct anti‐Carboboration of Alkynes with Boronic Acids to Produce Alkenylheteroarenes.
Authors: Roscales Silvia , Csaky Aurelio G. 
Published: July 2015

AbstractA new protocol for the intermolecular direct anti‐carboboration by using tartaric acid as promoter and boronic acids as reactants is presented.
ChemInform Abstract: Borylstannylation of Alkynes with Inverse Regioselectivity: Copper‐Catalyzed Three‐Component Coupling Using a Masked Diboron.
Authors: Yoshida H. , Takemoto Y. , Takaki K. 
Published: July 2015

AbstractThe three‐component borylstannylation reaction of terminal alkynes proceeds with inverse regioselectivity in the presence of a copper catalyst using a masked diboron compound giving diverse cis‐boryl(stannyl)alkenes.
ChemInform Abstract: Nine New Diterpenes from the Leaves of Plantation‐Grown Cunninghamia lanceolata.
Authors: Zhao Shuangshuang , Ling Junhong , Li Zhanlin , Wang Silong , Hu Jiangchun , Wang Nan 
Published: July 2015

Abstract9 New diterpenes are isolated from the leaves of plantation‐grown Cunninghamia lanceolata along with 12 known compounds.
ChemInform Abstract: Synthesis of D‐ and L‐Phenylalanine Derivatives by Phenylalanine Ammonia Lyases: A Multienzymatic Cascade Process.
Authors: Parmeggiani Fabio , Lovelock Sarah L. , Weise Nicholas J. , Ahmed Syed T. , Turner Nicholas J. 
Published: July 2015

AbstractStarting from inexpensive cinnamic acids, a novel chemoenzymatic cascade one‐pot approach to D‐phenylalanine derivatives is developed.
ChemInform Abstract: Oximoaspergillimide, a Fungal Derivative from a Marine Isolate of Aspergillus sp.
Authors: Cardoso‐Martinez Faviola , de la Rosa Jose M. , Diaz‐Marrero Ana R. , Darias Jose , D'Croz Luis , Cerella Claudia , Diederich Marc , Cueto Mercedes 
Published: July 2015

Abstractisolation and structure elucidation of oximoaspergillimide (I)
ChemInform Abstract: Pd—Imidate Complexes as Recyclable Catalysts for the Synthesis of C5‐Alkenylated Pyrimidine Nucleosides via Heck Cross‐Coupling Reaction.
Authors: Ardhapure Ajaykumar V. , Sanghvi Yogesh S. , Kapdi Anant R. , Garcia Joaquin , Sanchez Gregorio , Lozano Pedro , Serrano J. Luis 
Published: July 2015

AbstractThe new approach is used for the highly efficient scale‐up synthesis of the HSV‐1 inhibitor Brivudine (BVDU) (IV).
ChemInform Abstract: Layer‐by‐Layer Assembly for Graphene‐Based Multilayer Nanocomposites: Synthesis and Applications
Authors: Lee Taemin , Min Sa Hoon , Gu Minsu , Jung Yun Kyung , Lee Wonoh , Lee Jea Uk , Seong Dong Gi , Kim Byeong‐Su 
Published: July 2015

AbstractReview: 101 refs.
Dipeptidyl Enoates As Potent Rhodesain Inhibitors That Display a Dual Mode of Action
Authors: Royo Santiago , Rodríguez Santiago , Schirmeister Tanja , Kesselring Jochen , Kaiser Marcel , González Florenci V. 
Published: July 2015

AbstractDipeptidyl enoates were prepared through a high‐yielding two‐step synthetic route. They have a dipeptidic structure with a 4‐oxoenoate moiety as a warhead with multiple reactive sites. Dipeptidyl enoates were screened against rhodesain and human cathepsins B and L, and were found to be potent and selective inhibitors of rhodesain. Among them (S,E)‐ethyl 5‐((S)‐2‐{[(benzyloxy)carbonyl]amino}‐3‐phenylpropanamido)‐7‐methyl‐4‐oxooct‐2‐enoate (6) was the most potent, with an IC50 value of 16.4 nM and kinact/Ki=1.6×106 M−1 s−1 against rhodesain. These dipeptidyl enoates display a reversible mode of inhibition at very low concentrations and an irreversible mode at higher concentrations. Inhibition kinetics data, supported by docking studies, suggest a dual mode of action via attack of cysteine thiolate at two reactive positions.