The biological half-lives and decay rate constants under the conditions of a human brain tumor clonogenic cell assay were determined for six clinically used anticancer agents. The agents studied were: 1,3-bis(2-chloroethyl)-1-nitrosourea; 3-(2-chloroethyl-3-nitrosoureido-2-deoxy-D-glucopyranose; cis-diaminedichloroplatinum(II); 2,5-diaziridinyl-3,6-bis-(carboethoxyamino)-1,4-benzoquinone; 4-dem...

Simian virus 40 small-t antigen allows the growth of CV-1 cells in concentrations of theophylline that normally prevent cell cycling. This effect is completely overcome by two ionophores that uncouple mitochondria and by the anti-mitochondrial drug methylglyoxal bis-(guanylhydrazone).

A bis-imine (prepared via a new FeCl₃-based method) in combination with CoCl₂ facilitated lipase-mediated acetylation of the (R)-isomer of a racemic benzylic secondary alcohol with 91% ee(s). The methodology was used for the preparation of the known drug rivastigmine.

Unsymmetrical dispiro- and spirotetraoxanes have been designed and synthesized via acid-catalyzed cyclocondensation of bis(hydroperoxides) with ketones. Incorporation of water-soluble and polar functionalities, via reductive amination and amide bond formation, produces several analogues with low nanomolar in vitro antimalarial activity. Several analogues display an unprecedented level of oral a...

Investigators report the identification of novel mutant-specific inhibition of EGF receptor (EGFR) T790M by bis-indole-based inhibitors of protein kinase C using a small-molecule cancer cell line-based screening platform. This study shows the power of high-throughput drug screening in cancer cell lines and provides new lead scaffolds for optimization against resistant EGFR mutants in lung cancer.

4,5-Bis(aminomethyl)acridine, useful as an immunosuppressant, was prepared in 31% overall yield by the reaction of acridine with N-(hydroxymethyl)phthalimide and subsequent decomposition with excess 6 N HCl. The drug was found to produce a suppression of the humoral antibody response comparable to several known immunosuppressive agents.

Examples of a combined approach using in vivo as well as in vitro methods for the assessment of prenatal toxicity are presented. The topics discussed include the analysis of the possible embryotoxic potential of valproic acid (VPA), female sex hormones, bis(tri-n-butyltin) oxide (TBTO), and acyclovir and the problem of supplementing in vitro systems with drug-metabolizing activity.

The synthesis of some 9,10-disubstituted anthracene derivatives are described. 9,10-Bis(2-bromoethyl) anthracene 4,9,10-Bis (2-cyanoethyl) anthracene 5 and 9,10-Bis (4-hydroxybutyl) anthracene 11 are synthesized for the first time.

BACKGROUND Impulsivity plays a prominent role in numerous psychopathological states and poses an important clinical dilemma. However, different aspects of impulsivity are related to mood disorders, addictions, personality disorders, eating disorders, the relationship between anxiety and impulsivity is controversial and not well explored. The impact of anxiety on cognitive functioning is less ex...