bluuebunny/crossref_metadata_2025_split huggingface dataset:
ChemInform Abstract: Regioselective Synthesis of Trichloromethyl‐Substituted Salicylates and Cyclohexenones by One‐Pot Cyclizations of 1,3‐Bis(trimethylsilyloxy)buta‐1,3‐dienes.
Authors: Langer Peter , et al. et al. 
Published: February 2014

AbstractThe reaction of butadienes (II) and (IV) with buten‐2‐one (I) affords trichloromethyl‐substituted salicylates (III) or corresponding cyclohexenones (VIII) depending on the type of Lewis acid employed.
ChemInform Abstract: Magnetically Separable CuFe2O4 Nanoparticles Catalyzed Ligand‐Free C—S Coupling in Water: Access to (E)‐ and (Z)‐Styrenyl‐, Heteroaryl and Sterically Hindered Aryl Sulfides.
Authors: Kundu Debasish , Chatterjee Tanmay , Ranu Brindaban C. 
Published: February 2014

AbstractThe reaction shows high functional group tolerance and is applied to a wide range aromatic and heteroaromatic substituents in bromides or iodides and thiols.
ChemInform Abstract: PhI(OAc)2/KI Mediated 1,2‐Acetoxysulfenylation of Alkenes: Facile Synthesis of β‐Acetoxysulfides.
Authors: Muangkaew Charoensak , Katrun Praewpan , Kanchanarugee Patcharaphon , Pohmakotr Manat , Reutrakul Vichai , Soorukram Darunee , Jaipetch Thaworn , Kuhakarn Chutima 
Published: February 2014

AbstractKI promoted oxidative addition of (diacetoxyiodo)benzene and diaryldisulfides allows a facile synthesis of 1,2‐acetoxysulfides from alkenes.
ChemInform Abstract: Nickel(II) Chloride Hexahydrate Catalyzed Reaction of Aromatic Aldehydes with 2‐Mercaptoethanol: Formation of Supramolecular Helical Assemblage of the Product.
Authors: Laskar Rajibul A. , Begum Naznin A. , Mir Mohammad Hedayetullah , Rohman Md. Rumum , Khan Abu T. 
Published: February 2014

AbstractThe title reaction produces unexpected dithioacetals (III) as major products along with minor amounts of the expected 1,3‐oxathiolanes.
ChemInform Abstract: Copper‐Catalyzed Direct Oxysulfonylation of Alkenes with Dioxygen and Sulfonylhydrazides Leading to β‐Ketosulfones.
Authors: Wei Wei , Liu Chunli , Yang Daoshan , Wen Jiangwei , You Jinmao , Suo Yourui , Wang Hua 
Published: February 2014

AbstractA novel copper‐catalyzed direct oxysulfonylation of alkenes (I) and (IV) with dioxygen and sulfonylhydrazides (II) to furnish β‐ketosulfones (III) and (V), resp., is reported.
ChemInform Abstract: Modulation of Multifunctional N,O,P Ligands for Enantioselective Copper‐Catalyzed Conjugate Addition of Diethylzinc and Trapping of the Zinc Enolate.
Authors: Ye Fei , Zheng Zhan‐Jiang , Deng Wen‐Hui , Zheng Long‐Sheng , Deng Yuan , Xia Chun‐Gu , Xu Li‐Wen 
Published: February 2014

AbstractThe novel catalyst is effective in the asymmetric conjugate addition reaction of Et2Zn to enones and tandem silylation and acylation of enantioenriched zinc enolates.
ChemInform Abstract: Rhodium‐Catalyzed Dynamic Kinetic Asymmetric Transformations of Racemic Allenes by the [3 + 2] Annulation of Aryl Ketimines.
Authors: Tran Duc N. , Cramer Nicolai 
Published: February 2014

AbstractThe title reaction proceeds in a high regio‐, enantio‐, and diastereoselective manner for the allene incorporation.
ChemInform Abstract: Synthesis of Arylated Anthraquinones by Site‐Selective Suzuki—Miyaura Reactions of the Bis(triflates) of 1,3‐Di(hydroxy)anthraquinones.
Authors: Akrawi Omer A. , Khan Afsar , Patonay Tamas , Villinger Alexander , Langer Peter 
Published: February 2014

AbstractWhile the reaction of the anthraquinones (I) and (IV) proceeds with very good selectivity, similar reactions of the compound (VIII) are not selective.
ChemInform Abstract: Cascade Cyclizations of Acyclic and Macrocyclic Alkynones: Studies Toward the Synthesis of Phomactin A.
Authors: Ciesielski Jennifer , Gandon Vincent , Frontier Alison J. 
Published: February 2014

AbstractA study of the reactivity and diastereoselectivity of the Lewis acid promoted cascade cyclizations of both acyclic and macrocyclic alkynones is described.
ChemInform Abstract: Fluoroalkanosulfonyl Fluorides‐Mediated Cyclodehydration of β‐Hydroxy Sulfonamides and β‐Hydroxy Thioamides to the Corresponding Aziridines and Thiazolines.
Authors: Yan Zhaohua , Guan Chengbo , Yu Zhangxin , Tian Weisheng 
Published: February 2014

AbstractAn efficient method for the perfluorobutanesulfonyl fluoride‐induced cyclodehydration of β‐hydroxy sulfonamides and β‐hydroxy thioamides to the corresponding aziridines and thiazolines is reported.
ChemInform Abstract: Synthesis of Fused‐β‐Lactams Through Selective Gold‐Catalyzed Oxycyclization of Dioxolane‐Tethered Enynes.
Authors: Alcaide Benito , Almendros Pedro , Martinez del Campo Teresa , Torres M. Rosario 
Published: February 2014

AbstractThe gold‐catalyzed preparation of 2‐azetidinone‐fused oxacycles is accomplished from β‐lactam‐linked enynes through heterocyclization reaction taking advantage of the acetonide pendant group.
ChemInform Abstract: Palladium‐Catalyzed Carbene Migratory Insertion Using Conjugated Ene—Yne—Ketones as Carbene Precursors.
Authors: Wang Jianbo , et al. et al. 
Published: February 2014

AbstractThe reaction is proposed to proceed via oxidative addition, alkyne activation—cyclization, palladium carbene migratory insertion and β—hydride elimination followed by catalyst regeneration.
ChemInform Abstract: Visible Light Photoredox Atom Transfer Ueno—Stork Reaction.
Authors: Gu Xiangyong , Lu Ping , Fan Weigang , Li Pixu , Yao Yingming 
Published: February 2014

AbstractThe light‐promoted Ueno—Stork reaction of propargyl esters (I) yields desired tetrahydrofuran vinyl iodides (II).
ChemInform Abstract: Trifluoromethanesulfonic Acid Catalyzed Synergetic Oxidative/[3 + 2] Cyclization of Quinones with Olefins.
Authors: Meng Lingkui , Zhang Guanghui , Liu Chao , Wu Kun , Lei Aiwen 
Published: February 2014

AbstractA synthesis of tetrahydrobenzodifurans and tetrahydrobenzofurans in a TfOH‐catalyzed direct C‐H functionalization of benzoquinone and naphthoquinone with olefins is presented.
ChemInform Abstract: Phosphazene‐Catalyzed Intramolecular Cyclization of Nitrogen‐Tethered Alkynyl Esters.
Authors: Kondoh Azusa , Ando Kenichi , Terada Masahiro 
Published: February 2014

AbstractThe phosphazene‐catalyzed intramolecular addition of enolates of simple esters to alkynes is reported.
ChemInform Abstract: α‐Vinylation of Amides with Arylacetylenes: Synthesis of Allylamines under Metal‐Free Conditions.
Authors: Sun Manman , Wu Huandong , Bao Weiliang 
Published: February 2014

AbstractA novel method is reported for the preparation of allylamines (III) by a solvent‐free oxidative α‐vinylation of amides (II) with arylacetylenes (I).
ChemInform Abstract: Modular CeCl3·7H2O‐Catalyzed Multi‐Component Synthesis of 1,2,3,4‐Tetrasubstituted Pyrroles under Microwave Irradiation and Their Further Trichloroisocyanuric Acid‐Mediated Conversion into 5‐Sulfenylpyrrole Derivatives.
Authors: Silveira Claudio C. , Mendes Samuel R. , Martins Guilherme M. , Schloesser Sheila C. , Kaufman Teodoro S. 
Published: February 2014

AbstractA multicomponent synthesis of 1,2,3,4‐tetrasubstituted pyrroles promoted by cerous chloride is carried out under microwave irradiation.
ChemInform Abstract: Synthesis of Highly Functionalized Dihydrobenzofurans and Indolines by Palladium‐Catalyzed Mizoroki—Heck—Heteroannulation Cascade Reactions of Alkoxy‐1,3‐dienes.
Authors: Toppino Antonio , Arru Paolo , Bianco Niccolo , Prandi Cristina , Venturello Paolo , Deagostino Annamaria 
Published: February 2014

AbstractThe products can be further transformed into ketones, e.g. benzofuran (IV), in quantitative yields.
ChemInform Abstract: Regioselective Synthesis of Elusive 4,9‐Dihydro‐1H‐carbazoles by Gold‐Catalyzed Cycloisomerization of 3‐Allenylmethylindoles.
Authors: Alvarez Estela , Garcia‐Garcia Patricia , Fernandez‐Rodriguez Manuel A. , Sanz Roberto 
Published: February 2014

AbstractA general and efficient synthesis of carbazoles from 3‐allenylmethylindoles is reported.
ChemInform Abstract: A Short Synthesis of Polyhydroxylated Pyrrolizidines via Sequential 1,3‐Dipolar Cycloaddition and Reductive Amination.
Authors: Gkizis Petros , Argyropoulos Nikolaos G. , Coutouli‐Argyropoulou Evdoxia 
Published: February 2014

AbstractA series of pyrrolizidines bearing a methyl group at C‐5 are synthesized by 1,3‐dipolar cycloaddition of five‐membered cyclic nitrones with methyl vinyl ketone.
ChemInform Abstract: Regioselective Synthesis of 1,3,4,5‐Tetrasubstituted Pyrazoles from α‐Alkenyl‐α,β‐enones Derived from Morita—Baylis—Hillman Adducts.
Authors: Kim Sung Hwan , Lim Jin Woo , Yu Jin , Kim Jae Nyoung 
Published: February 2014

AbstractThe reaction of α‐alkenyl‐α,β‐enones with hydrazine derivatives in o‐dichlorobenzene under nitrogen atmosphere yields 4‐arylethylpyrazoles (III) whilst similar reaction in EtOH under O2 atmosphere gives selectively 4‐styrylpyrazoles [cf.
ChemInform Abstract: Improved Preparation of 1,3‐Bis(2,6‐di‐iso‐propylphenyl)imidazolium Tetrafluoroborate.
Authors: Briggs Andrew J. 
Published: February 2014

AbstractTitle compound (V) is prepared in a multi‐hundred‐gram scale with an overall yield of 61% from commercially available aniline (I).
ChemInform Abstract: Practical Oxazole Synthesis Mediated by Iodine from α‐Bromoketones and Benzylamine Derivatives.
Authors: Gao Wen‐Chao , Wang Ruo‐Lin , Zhang Chi 
Published: February 2014

AbstractA variety of oxazole derivatives including alkaloid halfordinol (VIII) is readily prepared by a oxidative cyclization of bromoketones with amines.
ChemInform Abstract: Synthesis and Binding Affinity of New 1,4‐Disubstituted Triazoles as Potential Dopamine D3 Receptor Ligands.
Authors: Insua Ignacio , Alvarado Mario , Masaguer Christian F. , Iglesias Alba , Brea Jose , Loza Maria I. , Carro Laura 
Published: February 2014

AbstractA series of new 1,4‐disubstituted triazoles (V) are synthesized using click chemistry methodology and evaluated as potential ligands on several subtypes of dopamine receptors.
ChemInform Abstract: Halonium‐Initiated Double Oxa‐Cyclization Cascade as a Synthetic Strategy for Halogenated Furo[3,2‐c]pyran‐4‐ones.
Authors: Wei Enxiang , Liu Bing , Lin Shaoxia , Zhao Baozhong , Liang Fushun 
Published: February 2014

AbstractA simple method is reported for the preparation of 7‐halogenated furo[3,2‐c]pyran‐4‐ones (II) and (III) by a double oxa‐cyclization of cyclopropanecarboxylic acids (I).
ChemInform Abstract: Synthesis of Chromeno[2,3‐b]indole Derivatives.
Authors: Graczol‐Foerdoes Eszter , Novak Tibor , Blasko Gabor , Fejes Imre , Perron‐Sierra Francoise , Nyerges Miklos 
Published: February 2014

AbstractSeveral new polysubstituted chromeno[2,3‐b]indole derivatives of type (VI) and (VIII) are prepared.
ChemInform Abstract: 4,6‐Diacetylresorcinol in Heterocyclic Synthesis. Part 1. Synthesis and Biological Evaluation of Some New Linearly and Angularly Substituted Pyrano[3,2‐g]chromenes via Vilsmeier—Haack Formylation of 4,6‐Diacetylresorcinol, Its Schiff Bases, and Hydrazones.
Authors: Ali Tarik E. , Ibrahim Magdy A. , El‐Gendy Zeinab M. , El‐Amin Eman M. 
Published: February 2014

AbstractMost products are shown to have weak antimicrobial activities, and dicarboxaldehydes [(III) and (V)] exhibit moderate antibacterial activity against Gram‐positive bacteria, yeast, and fungus.
ChemInform Abstract: An Efficient Synthesis of Poly‐Substituted Phenols and Pyridines from Morita—Baylis—Hillman Acetates and Diethyl Oxalacetate.
Authors: Yu Jin , Kim Ko Hoon , Lee Hyun Ju , Kim Jae Nyoung 
Published: February 2014

AbstractVarious phenol derivatives (III) synthesized by a one‐pot reaction of Morita—Baylis—Hillman acetates and sodium diethyl oxalacetate via a [4 + 2]‐cyclization.
ChemInform Abstract: Microwave‐Assisted One‐Pot Synthesis of Bioactive Ugi‐4CR Using Fluorite as Benign and Heterogeneous Catalyst.
Authors: Mohanram Ipsita , Meshram Jyotsna , Shaikh Ambareen , Kandpal Bhavna 
Published: February 2014

AbstractUgi derivatives (V) are synthesized and screened for their potential antibacterial activities.
ChemInform Abstract: Catalytic Synthesis of Polyhydroquinolines by Lithium Perchlorate in Polyethylene Glycol.
Authors: Wu Chunlei , Shen Runpu , Tao Feifei , Gao Xiaozhong , Deng Liping , Zhou Yubo 
Published: February 2014

AbstractAn effective synthesis of polyhydroquinoline derivatives via a four‐component one‐pot reaction of aromatic aldehydes, dimedone, ethyl acetoacetate, and ammonium acetate is presented.
ChemInform Abstract: A Facile Eco‐Friendly One‐Pot Five‐Component Synthesis of Novel 1,2,3‐Triazole‐Linked Pentasubstituted 1,4‐Dihydropyridines and Their Biological and Photophysical Studies.
Authors: Singh Harjinder , Sindhu Jayant , Khurana Jitender M. , Sharma Chetan , Aneja Kamal R. 
Published: February 2014

AbstractNew dihydropyridines (VII) (16 examples) are readily prepared by a multicomponent synthesis under ultrasonic or microwave irradiation in PEG‐400.
ChemInform Abstract: Intramolecular Diels—Alder Furan‐Mediated Synthesis of 8‐Aryl‐3,4‐dihydroisoquinolin‐1(2H)‐ones, Convenient Precursors of Indenol[1,2,3‐ij]isoquinolines.
Authors: Treus Monica , Harwood Laurence M. , Estevez Juan C. , Salas Cristian , Drew Michael G. B. , Estevez Ramon J. 
Published: February 2014

AbstractA sequential intramolecular high pressure Diels—Alder reaction of furans (I) and subsequent acid‐mediated ring opening of the resulting oxabicycle gives dihydroisoquinolinones (III) in good yields.
ChemInform Abstract: The Organocatalytic Enantioselective [3 + 2] Cycloaddition Reaction of α,β‐Unsaturated Aldehydes with Azomethine Ylides Applied to the Asymmetric Synthesis of Densely Substituted Pyrroloisoquinolines.
Authors: Iza Ainara , Ugarriza Iratxe , Uria Uxue , Reyes Efraim , Carrillo Luisa , Vicario Jose L. 
Published: February 2014

AbstractThe synthesis of densely functionalized pyrroloisoquinolines (VIII) is reported, representing the core structure of various alkaloids.
ChemInform Abstract: A Microwave Assisted Synthesis of Highly Substituted 7‐Methyl‐5H‐thiazolo[3,2‐a]pyrimidine‐6‐carboxylate Derivatives via One‐Pot Reaction of Aminothiazole, Aldehyde and Ethyl Acetoacetate.
Authors: Zhao Bing , Jiang Li‐Li , Liu Zhuo , Deng Qi‐Gang , Wang Li‐Yan , Song Bo , Gao Yan 
Published: February 2014

AbstractOptimum reactions are examined for the three‐component one‐pot synthesis of 12 title compounds (IV) under microwave irradiation.
ChemInform Abstract: Practical and Economical Approach to Synthesize Sitagliptin.
Authors: Lin Kuaile , Cai Zhengyan , Zhou Weicheng 
Published: February 2014

AbstractThe dipeptidyl peptidase 4 (DPP‐4) inhibitor sitagliptin phosphate monohydrate (V) is synthesized starting from compound (I) in an overall yield of 42% in four steps using the stereoselective reduction of compound (III) as the key step without the use of expensive and toxic catalysts or ligands.
ChemInform Abstract: A Donor—Acceptor Cyclopropene as a Dipole Source for a Silver(I) Catalyzed Asymmetric Catalytic [3 + 3]‐Cycloaddition with Nitrones.
Authors: Xu Xinfang , Zavalij Peter J. , Doyle Michael P. 
Published: February 2014

AbstractAg(I)‐catalyzed asymmetric formal [3 + 3]‐cycloaddition of nitrones (III) to the donor‐acceptor substituted cyclopropene (II) affords 3,6‐dihydro‐1,2‐oxazine derivatives (IV) (19 examples) in high yields with exceptional stereocontrol.
ChemInform Abstract: Synthesis of Azepine Derivatives by Silver‐Catalyzed [5 + 2] Cycloaddition of γ‐Amino Ketones with Alkynes.
Authors: Zhou Ming‐Bo , Song Ren‐Jie , Wang Cheng‐Yong , Li Jin‐Heng 
Published: February 2014

AbstractA novel method for the synthesis of 2,3‐dihydro‐1H‐azepines is established using a silver‐catalyzed [5 + 2] cycloaddition of γ‐aminoketones with terminal alkynes.
ChemInform Abstract: A Simple and One‐Pot Synthesis of 2,3,4,5‐Tetrasubstituted 4,5‐Dihydro‐3H‐1,4‐benzodiazepines.
Authors: Wang Ying , Chen Min , Ding Ming‐Wu 
Published: February 2014

AbstractTitle compounds (V) and (VII) are synthesized in a facile one‐pot procedure by a new sequential Ugi 4CC/Staudinger/aza‐Wittig reaction.
ChemInform Abstract: Syntheses of 1,5‐Benzothiazepines. Part 40. Syntheses and Antimicrobial Studies of 10‐Substituted‐6a,7‐dihydro‐6‐(4‐methoxyphenyl/phenyl)‐7‐ (3‐nitrophenyl)‐6H‐[1]benzopyrano[3,4‐c][1,5]benzothiazepines.
Authors: Pant Seema , Dharamveer Dharamveer , Saxena Deepika 
Published: February 2014

AbstractA variety of new benzopyranobenzothiazepines (III) (12 examples) are synthesized and evaluated for their antimicrobial activities.
ChemInform Abstract: Lancolides [A (Ia), B (IIa), C (Ib), D (IIb)], Antiplatelet Aggregation Nortriterpenoids with Tricyclo[6.3.0.02,11]undecane‐Bridged System from Schisandra lancifolia.
Authors: Shi Yi‐Ming , Wang Xin‐Bo , Li Xiao‐Nian , Luo Xiao , Shen Zi‐Ying , Wang Yi‐Ping , Xiao Wei‐Lie , Sun Han‐Dong 
Published: February 2014

AbstractLancolides A (Ia) and D (IIb) show specific antiplatelet aggregation induced by platelet‐activating factor (PAF).
ChemInform Abstract: Trading N and O: Asymmetric Syntheses of β‐Hydroxy‐α‐amino Acids via α‐Hydroxy‐β‐amino Esters.
Authors: Davies Stephen G. , Fletcher Ai M. , Frost Aileen B. , Lee James A. , Roberts Paul M. , Thomson James E. 
Published: February 2014

AbstractThe conversion of readily synthesized α‐hydroxy‐β‐amino acid derivatives to N‐protected aziridines (VII) is developed and their utilization in the synthesis of β‐hydroxy‐α‐amino acids is demonstrated.
ChemInform Abstract: Bioactive Oleanane‐Type Saponins from the Rhizomes of Anemone taipaiensis.
Authors: Wang Xiao‐Yang , Gao Hui , Zhang Wei , Li Yuan , Cheng Guang , Sun Xiao‐Li , Tang Hai‐Feng 
Published: February 2014

AbstractFive new oleanane‐type triterpenoid saponins (structure example (I)), together with seven known saponins are isolated.
ChemInform Abstract: Alkaloids from Melodinus suaveolens.
Authors: Zhang Ting‐Ting , Liu Zhi‐Wen , Wang Wen‐Jing , Tong Yong‐Bin , Xu Fang‐Fang , Yuan Jing‐Quan , Liu Bo , Zhang Xiao‐Qi , Ye Wen‐Cai 
Published: February 2014

Abstract2 New quinoline alkaloids (I) and (II) are isolated from the twigs and leaves of Melodinus suaveolens along with 6 known alkaloids.
ChemInform Abstract: Heteroanellated and 7‐Deoxygenated Goniofufurone Mimics with Antitumor Activity: Design, Synthesis and Preliminary SAR Studies.
Authors: Popsavin Velimir , Francuz Jovana , Zelenovic Bojana Sreco , Benedekovic Goran , Popsavin Mirjana , Kojic Vesna , Bogdanovic Gordana 
Published: February 2014

AbstractNew compounds (II) and (III) show diverse growth inhibitory effects against selected tumor cell lines, but are devoid of any significant toxicity towards the normal foetal lung fibroblasts.
ChemInform Abstract: Insight into Dihalogenation of E‐Ring of Podophyllotoxins, and Their Acyloxylation Derivatives at the C4 Position as Insecticidal Agents.
Authors: Che Zhiping , Yu Xiang , Fan Lingling , Xu Hui 
Published: February 2014

AbstractAn unexpected sequential E‐ring double halogenation of podophyllotoxin analogues is reported.
ChemInform Abstract: Synthetic Developments in Functionalized Pyrano[2,3‐c]pyrazles. A Review
Authors: Myrboh Bekington , Mecadon Hormi , Rohman Md. Rumum , Rajbangshi Mantu , Kharkongor Icydora , Laloo Badaker M. , Kharbangar Iadeishisha , Kshiar Baskhemlang 
Published: February 2014

AbstractReview: 97 refs.
ChemInform Abstract: Benzenoid Polycyclic Hydrocarbons with an Open—Shell Biradical Ground State
Authors: Sun Zhe , Zeng Zebing , Wu Jishan 
Published: February 2014

AbstractReview: recent progress, from both theoretical and experimental perspectives, on four types of benzenoid polycyclic hydrocarbons with an open‐shell biradical ground state: 1) acenes, 2) periacenes and anthenes, 3) zethrenes, and 4) extended p‐quinodimethane derivatives; 63 refs.
ChemInform Abstract: Utilization of Alkoxysilyl Groups for the Creation of Structurally Controlled Siloxane‐Based Nanomaterials
Authors: Kuroda Kazuyuki , Shimojima Atsushi , Kawahara Kazufumi , Wakabayashi Ryutaro , Tamura Yasuhiro , Asakura Yusuke , Kitahara Masaki 
Published: February 2014

AbstractReview: 73 refs.
Design, Synthesis and Biological Evaluation of 4‐Amino‐N‐(4‐aminophenyl)benzamide Analogues of Quinoline‐Based SGI‐1027 as Inhibitors of DNA Methylation
Authors: Rilova Elodie , Erdmann Alexandre , Gros Christina , Masson Véronique , Aussagues Yannick , Poughon‐Cassabois Valérie , Rajavelu Arumugam , Jeltsch Albert , Menon Yoann , Novosad Natacha , Gregoire Jean‐Marc , Vispé Stéphane , Schambel Philippe , Ausseil Fréderic , Sautel François , Arimondo Paola B. , Cantagrel Frédéric 
Published: February 2014

AbstractQuinoline derivative SGI‐1027 (N‐(4‐(2‐amino‐6‐methylpyrimidin‐4‐ylamino)phenyl)‐4‐(quinolin‐4‐ylamino)benzamide) was first described in 2009 as a potent inhibitor of DNA methyltransferase (DNMT) 1, 3A and 3B. Based on molecular modeling studies, performed using the crystal structure of Haemophilus haemolyticus cytosine‐5 DNA methyltransferase (MHhaI C5 DNMT), which suggested that the quinoline and the aminopyridimine moieties of SGI‐1027 are important for interaction with the substrates and protein, we designed and synthesized 25 derivatives. Among them, four compounds—namely the derivatives 12, 16, 31 and 32—exhibited activities comparable to that of the parent compound. Further evaluation revealed that these compounds were more potent against human DNMT3A than against human DNMT1 and induced the re‐expression of a reporter gene, controlled by a methylated cytomegalovirus (CMV) promoter, in leukemia KG‐1 cells. These compounds possessed cytotoxicity against leukemia KG‐1 cells in the micromolar range, comparable with the cytotoxicity of the reference compound, SGI‐1027. Structure–activity relationships were elucidated from the results. First, the presence of a methylene or carbonyl group to conjugate the quinoline moiety decreased the activity. Second, the size and nature of the aromatic or heterocycle subsitutents effects inhibition activity: tricyclic moieties, such as acridine, were found to decrease activity, while bicyclic substituents, such as quinoline, were well tolerated. The best combination was found to be a bicyclic substituent on one side of the compound, and a one‐ring moiety on the other side. Finally, the orientation of the central amide bond was found to have little effect on the biological activity. This study provides new insights in to the structure–activity relationships of SGI‐1027 and its derivative.
Near‐Field Hyperspectral Optical Imaging
Authors: Bouillard Jean‐Sebastien G. , Dickson Wayne , Wurtz Gregory A. , Zayats Anatoly V. 
Published: February 2014

AbstractThis Minireview presents an overview of near‐field hyperspectral imaging and discusses its applications. Based on a fibre‐tip probe, the hyperspectral near‐field optical microscope allows the simultaneous acquisition of near‐field images over a broad spectral range (400 to 1000 nm), enabling the recovery of local spectroscopic information, which is essential for understanding the resonant interaction of light with nanostructured objects because the far‐field and near‐field spectral responses can differ significantly, as is the case for plasmonic nanostructures. The optical information is collected through local interactions with the evanescent fields at the surface of the sample; therefore, the approach provides spectroscopic information with nanoscale spatial resolution. Several applications of spectroscopic near‐field microscopy are described for the visualisation of plasmonic modes in metallic nanostructures and near‐field fluorescence spectroscopy.
Optical Imaging of Liquid Crystals at the Nanoscale
Authors: Rosenblatt Charles 
Published: February 2014

AbstractThe instrumentation associated with near‐field scanning optical microscopy (NSOM) can be exploited to provide three‐dimensional structure and dynamic information about liquid crystals at scales not possible with diffraction‐limited tools. This Minireview focuses on our use of NSOM techniques to probe spatial variations of the nematic director and the nematic orientational order parameter on length scales as small as a few nanometers.