Elizabeth Raux, Jeffrey Klenc, Ava Blake, Jarosław Sączewski and Lucjan Strekowski
Article: Conjugate Addition of Nucleophiles to the Vinyl Function of 2-Chloro-4-vinylpyrimidine Derivatives
Molecules 2010, 15(3), 1973-1984; doi:10.3390/molecules15031973 - published online 19 March 2010
Show/Hide AbstractAbstract: Conjugate addition reaction of various nucleophiles across the vinyl group of 2-chloro-4-vinylpyrimidine, 2-chloro-4-(1-phenylvinyl)pyrimidine and 2-chloro-4-vinylquinazoline provides the corresponding 2-chloro-4-(2-substituted ethyl)pyrimidines and 2-chloro-4-(2-substituted ethyl)quinazolines. Treatment of these products, without isolation, with N-methylpiperazine results in nucleophilic displacement of chloride and yields the corresponding 2,4-disubstituted pyrimidines and quinazolines.

Jan Marek, Petr Stodulka, Jiri Cabal, Ondrej Soukup, Miroslav Pohanka, Jan Korabecny, Kamil Musilek and Kamil Kuca
Communication: Preparation of the Pyridinium Salts Differing in the Length of the N-Alkyl Substituent
Molecules 2010, 15(3), 1967-1972; doi:10.3390/molecules15031967 - published online 19 March 2010
Show/Hide AbstractAbstract: Quaternary pyridinium salts with chains ranging from C₈ to C₂₀ belong in the large group of cationic surfactants. In this paper, the preparation of such cationic surface active agents based on the pyridinium moiety and differing in the length of the N-alkyl chain is described. Additionally, HPLC technique was established to distinguish each prepared pyridinium analogue. This study represents universal method for preparation and identification of quaternary pyridinium detergents.

Jin-Jie Li, Xiao-Ya Shang, Ling-Ling Li, Ming-Tao Liu, Jian-Quan Zheng and Zong-Lian Jin
Article: New Cytotoxic Azaphilones from Monascus purpureus-Fermented Rice (Red Yeast Rice)
Molecules 2010, 15(3), 1958-1966; doi:10.3390/molecules15031958 - published online 18 March 2010
Show/Hide AbstractAbstract: Using a cell-based cytotoxicity assay three new cytotoxic azaphilones, including two stereoisomers and designated monapurones A-C (1-3), were isolated from the extract of Monascus purpureus-fermented rice (red yeast rice). Their structures were elucidated by detailed interpretation of spectroscopic and chemical data. The relative configurations were assigned on the basis of analysis of NOE data, and the absolute configurations were determined by direct comparison of their CD spectra with those of known azaphilones and chemical correlations. In the in vitro assays, monapurones A-C (1-3) showed selective cytotoxicity against human cancer cell line A549 with IC₅₀ values of 3.8, 2.8 and 2.4mM respectively, while exhibiting no significant toxicity to normal MRC-5 and WI-38 cells at the same concentration.

Sireesha Chemburu, Kyle Fenton, Gabriel P. Lopez and Reema Zeineldin
Review: Biomimetic Silica Microspheres in Biosensing
Molecules 2010, 15(3), 1932-1957; doi:10.3390/molecules15031932 - published online 17 March 2010
Show/Hide AbstractAbstract: Lipid vesicles spontaneously fuse and assemble into a lipid bilayer on planar or spherical silica surfaces and other substrates. The supported lipid bilayers (SLBs) maintain characteristics of biological membranes, and are thus considered to be biomembrane mimetic systems that are stable because of the underlying substrate. Examples of their shared characteristics with biomembranes include lateral fluidity, barrier formation to ions and molecules, and their ability to incorporate membrane proteins into them. Biomimetic silica microspheres consisting of SLBs on solid or porous silica microspheres have been utilized for different biosensing applications. The advantages of such biomimetic microspheres for biosensing include their increased surface area to volume ratio which improves the detection limits of analytes, and their amenability for miniaturization, multiplexing and high throughput screening. This review presents examples and formats of using such biomimetic solid or porous silica microspheres in biosensing.

Motoki Ito, Chieko Ogawa, Nobutaka Yamaoka, Hiromichi Fujioka, Toshifumi Dohi and Yasuyuki Kita
Article: Enhanced Reactivity of [Hydroxy(tosyloxy)iodo]benzene in Fluoroalcohol Media. Efficient Direct Synthesis of Thienyl(aryl)iodonium Salts
Molecules 2010, 15(3), 1918-1931; doi:10.3390/molecules15031918 - published online 17 March 2010
Show/Hide AbstractAbstract: In this manuscript, we report clear evidence for the generation of aromatic cation radicals produced by using [hydroxy(tosyloxy)iodo]benzene (HTIB) in fluoroalcohol solvents such as 2,2,2-trifluoroethanol (TFE) and 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP). The single-electron-transfer (SET) oxidation ability of HTIB to give cation radicals was first established by ESR and UV measurements. The reaction was broadly applied to various thiophenes, and unique thienyliodonium salts were directly synthesized by this method in excellent yields without the production of any harmful byproducts.

Zi-Guo Jiao, Hong-Qiu He, Cheng-Chu Zeng, Jian-Jun Tan, Li-Ming Hu and Cun-Xin Wang
Article: Design, Synthesis and Anti-HIV Integrase Evaluation of N-(5-Chloro-8-Hydroxy-2-Styrylquinolin-7-yl)Benzenesulfonamide Derivatives
Molecules 2010, 15(3), 1903-1917; doi:10.3390/molecules15031903 - published online 16 March 2010
Show/Hide AbstractAbstract: Styrylquinoline derivatives are demonstrated to be HIV-1 integrase inhibitors. On the basis of our previous CoMFA analysis of a series of styrylquinoline derivatives, N-[(2-substituted-styryl)-5-chloro-8-hydroxyquinolin-7-yl]-benzenesulfonamide derivatives were designed and synthesized,and their possible HIV IN inhibitory activity was evaluated.