This study evaluated if the density of sigma sites was modulated following stimulation of mitosis and progression through the cell cycle. The sigma ligand N-[1′(2-piperidinyl)ethyl)-4-[I-125]-iodobenzamide (I-125-PAB) was a binding probe on the mammary tumor cell lines T47D and MCF-7, and the p...

A new route allowing the one-step synthesis of (2-heteroarylphenyl)tetrazole and fluorinated biphenyltetrazole derivatives is disclosed. By using 2 mol% of an air-stable diphosphine-palladium catalyst [PdCl(C3H5)(dppb)], potassium pivalate as base and dimethylacetamide as solvent, a wide range o...

The carbon acids activated by two thiobenzyl groups have been synthesized and the products of the proton transfer reaction between 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) and studied compounds in solution were defined by electrospray ionization mass spectrometry method. The ionization of carbo...

The reaction of N-unsubstituted imines of 2-hydroxyacetophenones with trichloro(trifluoro)ethylidene nitromethanes in the presence of DABCO proceeds via tandem oxa-Michael/aza-Henry additions (in dichloromethane) or aza-Michael addition (in benzene) to give 4-methyl-3-nitro-2-trichloro(trifluoro...

The base-mediated reaction of enantiomerically pure α-sulfinylketimine (+)-1 with (E)-methyl cinnamate afforded (+)-5a in a one-pot procedure with complete diastereoselectivity. A sole diastereomer of the eight possible ones was isolated which revealed the stereocontrol of the chiral sulfinyl g...

The optimized molecular structure, vibrational frequencies, corresponding vibrational assignments of the title compound have been investigated experimentally and theoretically. The HOMO and LUMO analysis is used to determine the charge transfer within the molecule. The stability of the molecule ...

A series of novel 2-[(arylimino)alkyl]pyridine derivatives, containing electron-withdrawing groups (F, Cl, Br, CF3, NO2, CN) in the aryl rings, have been synthesized and characterized by 1H, 13C and 19F NMR spectroscopy. The corresponding nickel(II) complexes (24 complexes) have been prepared in...

To obtain potent liver X receptor (LXR) agonists, a structure–activity relationship study was performed on a series of tert-butyl benzoate analogs. As the crystal structure analysis suggested applicable interactions between the LXR ligand-binding domain and the ligands, two key functional group...

In this paper we report the synthesis of novel S-alkenyl derivatives of 5-(trifluoromethyl)-4H-1,2,4-triazole-3-thiol via alkenation reaction with different alkenyl halides. Reaction between the resulting S-alkenation products and iodine proceeds regiospecifically to give new fused fluorine- and...

1,1,1-Trifluoro-4-methoxy-4-aryl-but-3-en-2-ones react with 2-pyridylcarboxamidrazone to produce the corresponding 1,1,1-trifluoro-4-aryl-4-(N1-pyridine-2-carboxamidrazone)-3-buten-2-ones. The butenones react with copper(II) chloride to give 1:1 adducts, in which the donor molecules were shown t...

The synthesis of a series of 5-phenyl substituted 1-methyl-2-pyridones (I) and 4′-substituted biphenyl-4-carboxylic acids (II) as novel A–C ring steroidomimetic inhibitors of 5α-reductase (5αR) is described. Compounds 1–4 (I) were synthesized by palladium catalyzed cross coupling (Ishikura)...

An assay for 3-oxoacyl-coenzyme A (3-oxoacyl-CoA) thiolases is described. The reaction utilizes acetyldithio-CoA as the nucleophile and variable chain length saturated acyl-CoA's as the electrophiles. The properties of the 3-oxoacyl-CoA dithioester product, notably a pKa of 6.6 ± 0.1 and a...

Characterization of the sites recognized by antibody on the V3 loop of the envelope glycoprotein gp120 of HIV-1 was done by competition ELISAs on a series of four mouse mAbs, a human mAb and a human Fab. The solid-phase antigen consisted of biotin-YNKRKRIHIGPGRAFYTTKN, a sequence from the center...

Identifying the earliest neutralizing antibody specificities that are elicited following infection or vaccination by HIV-1 is an important objective of current HIV/AIDS vaccine research. We have shown previously that transplantation of HIV-1 V3 epitopes into an HIV-2 envelope (Env) scaffold prov...

The development of a safe, effective and globally affordable HIV vaccine offers the best hope for the future control of the HIV-1 pandemic. Since 1987, scores of candidate HIV-1 vaccines have been developed which elicited varying degrees of protective responses in nonhuman primate models, includ...

The synthesis of novel building blocks corresponding to the Tn [α-D-GalNAc-(1 → O)-Thr] an sialyl Tn [α-D-Neu5Ac-(2→6)-α-D-GalNAc-(1→O)-Thr] epitopes is descibed. The Tn building block was prepared from 4-methylphenyl 2-azido-2-deoxy-1-thio-β-D-galactopyranoside in four steps (42% yield) ...

This review is a Part II of the series aiming to provide comprehensive overview of currently used antiviral drugs and to show modern approaches to their analysis. While in the Part I antivirals against herpes viruses and antivirals against respiratory viruses were addressed, this part concerns a...

A concise total synthesis of the complex indole alkaloid (±)-actinophyllic acid was accomplished by a sequence of reactions requiring only 10 steps from readily-available, known starting materials. The approach featured a Lewis acid-catalyzed cascade of reactions involving stabilized carbocatio...

Based on the encouraging results found for 3,5-dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f][1,2,3,5]tetrazepin-4-(3H)-one 7 previously tested by us, as well as the consideration that heterocycle fused tetrazepinones bearing the 2-chloroethyl substituent show a better cytotoxi...

Regioisomeric analogues of gramine, 5-(dialkylaminomethyl)indole-2-carboxylates were prepared by the Fischer indolization of 4-(dialkylaminomethyl)phenylhydrazones easily obtained from diazotized 4-(dialkylaminomethyl)anilines by the Japp–Klingemann reaction. These formal Mannich bases are valu...