New Antiamebic Acridines

Abstract

A series of novel 9-acridanones and 9-iminoacridines has been prepared and investigated by a number of spectroscopic techniques in order to determine the nature and extent of the binding of these compounds to DNA. Results are discussed with reference to antiamebic activity in vitro.

SYNTHESIS, INTERCALATION INTO DNA AND ANTICANCER ACTIVITY OF SOME 4,6- DIALKOXY-10-METHYL-PYRIDO [3,2-g] QUINOLINES

“…Biological data are given in Table 2. As previously noted in the acridine series [4,5], intercalation occurs only when simultaneously exist a ring system as planar as possible and a protonatable nitrogen. However, there are no correlations between DNA affinity the cytotoxic potency.…”

“…Spectrophotometric measurements were carried out in 0.018 mol/1 NaCl -0.03 mol/1 Tris CI Buffer (pH = 7.0), using a Pye-Unicam SP 8000 spectrophotometer fitted with a Pye-Unicam SP 876 series 2 temperature programme controller. Conditions were those previously described [4]. Binding constants were calculated using "Enzfitter", a non linear regression analysis programme from Elsevier Biosoft.…”

Preparation of some new N-substituted 9,10-dihydroacridine derivatives

“…of Galy et al (9). In the latter, which was successfully used in similar cases (10)(11)(12), toluene is used as solvent instead of butanone and the mixture is refluxed 5 days instead of about 2 h. On the other hand, alkylation of the 9,10-dihydroacridine (4) by phase-transfer catalysis never succeeded, whatever the previously quoted methods used were.…”