Synthesis and in Vitro Antileukemic Activity of Some New 1,3-(Oxytetraethylenoxy)cyclotriphosphazene Derivatives

Abstract

A new series of 1,3-(oxytetraethylenoxy)cyclotriphosphazene derivatives bearing 2-chloroethylamine or salicylaldehyde (2-hydroxybenzaldehyde) or its Schiff base (after condensation with 2-chloroethylamine) units and having also 2-naphthyl or anthraquinone groups as cosubstituents has been synthesized. The in vitro cytotoxic activity of these compounds against a panel of four cancer cell lines has been studied. Most of the compounds exhibited antiproliferative activity in the range of the international criterion for synthetic agents (4 microg/mL) against the MOLT4, L 1210, HL-60, and P388 cell lines chosen for testing.

Syntheses, spectral characterization, thermal properties and DNA cleavage studies of a series of Co(II), Ni(II) and Cu(II) polypyridine complexes with some new schiff-bases derived from 2-chloroethylamine

“…These bands were absent in all the complexes, indicating deprotonation on coordination of the Schiff base ligands to metal ion. In addition, the bands at 1346-1350 cm -1 attributed to the phenolic C-O stretching vibrations of the free ligands were blue-shifted to 1341-1431 cm -1 upon complexation suggesting the involvement of the phenolic oxygen atom in the coordination [18][19][20]. The imine (C=N) functional group of the free ligands was observed as strong bands between 1670-1643 cm -1…”

“…The mode of coordination of the Schiff base ligands was further supported by the appearance of two new weak bands in the lower frequency region at 570-520 cm -1 and 478-416 cm -1 . These bands were assigned to the M-N and M-O stretching vibrations, respectively [19,16].…”

Poly‐ and Cyclophosphazenes as Drug Carriers for Anticancer Therapy

“…Furthermore, since (Labarre et al, 1979) discovered the antitumor activity of hexaziridinylcyclotriphosphazene, intensive studies have continued to show improved antitumor activity with reduced toxicity. For example (Siwy et al, 2006(Siwy et al, , 2007 demonstrated recently that water solubility and cytotoxicity could both be improved with reduced toxicity by replacing the aziridinyl groups partially with a crown ether and 2-naphthol or an anthraquinone derivative. However, there are not many studies on anticancer drugs conjugated to cyclotriphosphazenes other than amphiphilic cyclotriphosphazenes, which are dealt with next.…”

Évaluation de la toxicité aiguë de la 2-hydroxy-méthyl-1 (N-phtaloyltryptophyl) aziridine chez le rat Wistar

“…Ainsi certaines recherches ont montré que les aziridines sont immunostimulantes ; c'est le cas par exemple de BM 12 531 ou Azimexon [2-cyanaziridinyl-2-carbamoyl-aziridinyl-1-propane], qui provoque une augmentation spontanée de la concentration des lymphocytes T chez les patients cancéreux et module le système immunitaire chez les animaux [8,9]. D'autres chercheurs ont montré que les aziridines peuvent être aussi des molécules immunodépressives induisant une réduction de la prolifération cellulaire et un déficit immunitaire comme le ciamexon, dérivé de 2-cyan-aziridine, ou le 1,3-(oxytetraethylenoxy)-cyclotriphosphazene [10,11]. Vu l'importance des propriétés biologiques des aziridines, de nouvelles voies de synthèse, simples et efficaces, sont de plus en plus recherchées.…”