An improved synthesis of multifunctionalized pyrrolo[2,3,4-kl]acridine derivatives with different substituted patterns using silica sulfuric acid (SSA) as a heterogeneous catalyst under microwave irradiation conditions was developed. The reaction could be conducted by using readily available and inexpensive substrates within short periods of 12-15 min. under microwave irradiation. Compared with...

Simple alkylating derivatives of polycyclic aromatic hydrocarbons have been found to be much more carcinogenic in the Strain A mouse than are the parent hydrocarbons. It has also been shown that the carcinogenicity of these halomethyl hydrocarbons is not a function of the first-order solvolysis rate. The acridine antitumor agent and mutagen ICR 170, 2-methoxy-6-chloro-9-[3-(ethyl-2-chloroethyl)...

Carcinogenic bromomethyl- and chloromethylanthracenes and benz(a)anthracenes were found to react rapidly in vitro with DNA under physiological conditions and to varying degrees with nucleotides and nucleosides. The compounds were assayed for production of lung adenomas in strain A mice and relative carcinogenic potencies were compared with in vitro alkylation and with in vitro solvolysis rates....

Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease associated with aggregation of TAR DNA-binding protein-43 (TDP-43) in neuronal cells and manifests as motor neuron dysfunction &muscle atrophy. The carboxyl-terminal prion-like domain of TDP-43 can aggregate in vitro into toxic β-sheet rich amyloid-like structures. So far, treatment options for ALS are very limited and Ril...

Methods for the synthesis of N1, N8-bis(9-acridinyl)-N4-(4-hydroxybenzyl)spermidine and N1, N7-(hydroxybenzyl)-bis-(3-aminopropyl)amine were investigated. Thus monocyanoethylation of 4-methoxybenzylamine followed by treatment with 4chlorobutyronitrile gave the dinitrile N-(2-cyanoethyl)-N-(3-cyanopropyl)-4-methoxybenzylamine. Subsequent in situ reduction with lithium aluminium hydride gave the ...

Toxic effects of many persistent organic pollutants (e.g., polychlorinated biphenyls or polychlorinated dibenzo-p-dioxins and furans) are mediated via the aryl hydrocarbon receptor (AhR). Although polycyclic aromatic hydrocarbons (PAHs) and their derivatives also activate AhR, their toxic effects remain to be fully elucidated. In the present study, we used the in vitro H4IIE-luc transactivation...