Isothiocyanates are a class of naturally occurring chemopreventive agents known to be effective at triggering apoptosis. In this study, we show that whereas overexpression of the oncoprotein Bcl-2 renders Jurkat T-lymphoma cells resistant to a range of cytotoxic agents, phenethyl isothiocyanate is able to overcome the inhibitory action of Bcl-2 and trigger apoptosis. A 50-fold increase in Bcl-2...

At atmospheric pressure and at 130-160 degrees C, primary aromatic amines (p-XC6H4NH2, X = H, Cl, NO2) are mono-N-alkylated in a single step, with symmetrical and asymmetrical dialkyl carbonates [ROCOOR', R = Me, R' = MeO(CH2)2O(CH2)2; R = R' = Et; R = R' = benzyl; R = R' = allyl; R = Et, R' = MeO(CH2)2O(CH2)2], in the presence of a commercially available NaY faujasite. No solvents are required...

The enantiomerically and diastereomerically pure tricyclic oxazolidine cis-10 was prepared in a five step synthesis starting with 1-bromo-2-iodobenzene. Me3SiCN and allylSiMe3 reacted with cis-10 in the presence of TiCl4 to form the nitrile (3S)-11 and the allyl derivative (3S)-12 with high diastereoselectivity. The hydrogenolytic removal of the chiral auxiliary failed, since the endocyclic ben...

The activating effects of the benzyl and allyl groups on S(N)2 reactivity are well-known. 6-Chloromethyl-6-methylfulvene, also a primary, allylic halide, reacts 30 times faster with KI/acetone than does benzyl chloride at room temperature. The latter result, as well as new experimental observations, suggests that the fulvenyl group is a particularly activating allylic group in S(N)2 reactions. ...

Introduction of carbon side chain at C(3)-position of indole ring was accomplished by using Pd-catalyzed allylation and vinylation. The selective vinylation at C(3)-position of 4-bromoindole was applied to the synthesis of optically active 4-bromotryptophan derivatives, which was used as a starting material for the synthesis of several optically active ergot alkaloids, which were clavicipitic a...

Novel N-amino benzylthiolates were synthesized via multicomponent reaction of malononitrile, isothiocyanates and benzyl halides under conventional and solvent-free conditions. Various electron-donating and -withdrawing substitutes within both isothiocyanates and benzyl halides were used to demonstrate the efficiency of new methodology. A broad spectrum of antibacterial and antifungal activities...

The title di-thio-carbazate ester (I), C18H18N2S2 [systematic name: (E)-4-methyl-benzyl 2-[(E)-3-phenyl-allyl-idene]hydrazinecarbodi-thio-ate, comprises an almost planar central CN2S2 residue [r.m.s. deviation = 0.0131 Å]. The methyl-ene(tolyl-4) group forms a dihedral angle of 72.25 (4)° with the best plane through the remaining non-hydrogen atoms [r.m.s. deviation = 0.0586 Å] so the mol-ecule...

A series of halido bis(silylamido) metalates chromium to cobalt is reported. Reaction [NBu4]Br with linear metal silylamides ML2 (M=Mn?Co, L=?N(SiMe3)2, ?N(Dipp)SiMe3; Dipp=2,6-iPr?C6H3) leads NBu4[M(Br)L2] whereas for either intramolecular deprotonation (L=?N(SiMe3)2) or ligand exchange (L=?N(Dipp)SiMe3) observed. Attempts their reduction KC8 showed in part the formation metal(I) silylamide co...

Overdose of acetaminophen causes severe hepatic necrosis in humans and experimental animals. Studies on its hepatotoxicity remain a very active area since some of current data are still uncertain. In this study, freshly isolated rat hepatocytes were used to determine the effects of garlic extract and its component, allicin on the acetaminophen-induced cell cytotoxicity and to compare with the e...