Synthesis and antitumor evaluation of novel sulfonylcycloureas derived from nitrogen mustard.

A new series of sulfonylcycloureas derivatives have been synthesized and evaluated in vitro for their antitumor activity against four cancer cell lines (A431, Jurkat, U266, and K562). These compounds were prepared by the condensation of several sulfonamides (2a-m) with ethyl bis(2-chloroethyl)carbamate (1a). The relative cytotoxicity of these new derivatives in comparison to chlorambucil is reported.

Effect of novel phosphoramidate on growth and respiratory metabolism of Paramecium aurelia.

The continuous increase in the number of new chemicals as well as the discharges of solid and liquid wastes triggered the need for simple and inexpensive bioassays for routine testing. In recent years, there has been increasing development of methods (particularly rapid tests) for testing environmental samples. This paper describes the quick toxic evaluation of a novel synthetic compound: Phosphoramidate derivative B at different concentrations (2, 4 and 8 µM) for 72 h on Paramecium aurelia. We showed that B concentrations affect the growth of Paramecium in concentration- dependent manner; also it decreases the growth rate and increases response percentage in concentration- dependent manner. The value of LC50 obtained for these protozoa was estimated at 4.9693 µM after 24 hours of exposure. The respiratory metabolism of protozoan is perturbed at three concentrations, noting that the oxygen consumption was significantly increased at high concentrations after 18 hours of exposure. The results indicate that the Paramecium toxicity assay could be used as a complementary system to rapidly elucidate the cytotoxic potential of insecticides. The major advantages associated with these tests are: inexpensive, simple, rapid and seem to be attractive alternatives to conventional bioassays.