New α,ω-Diamido and α,ω-Diamino Mono- and Bi-Bridged Acridine Dimers
A novel set of dimers derived from 9-amino acridine was prepared and characterized by 1H and 13C NMR.These derivatives are bridged at several different positions of the heterocyclic moieties, by the way of α,ω-diamide or α,ω-diamino side-chains.Additionally the preparation of some bi-bridged compounds was achieved. Keywords. 9-Amino-acridine; Mono-bridged dimers; Bi-bridged dimers;
Moisan, Martine,Galy, Jean-Pierre,Galy, Anne-Marie,Barbe, Jacques
Synthesis and antileishmanial activity of 6-mono-substituted and 3,6-di-substituted acridines obtained by acylation of proflavine
Two new series of diaminoacridinic derivatives obtained from proflavine and N-(6-amino-3-acridinyl)acetamide were synthesised and assessed for their cytotoxic and antileishmanial activities. Two compounds, N-[6-(acetylamino)-3-acridinyl]acetamide and N-[6-(benzoylamino)-3-acridinyl]benzamide demonstrated highly specific antileishmanial properties against the intracellular amastigote form of the parasite. Structure-activity relationships established that the antiproliferative activity against human cells was greatly enhanced by the presence of a benzoylamino group in 6-mono-substituted acridines, while the presence of two acetylamino or benzoylamino groups in 3,6-di-substituted acridines strongly increased the specificity of the molecules for Leishmania parasite, suggesting that symmetric conformations could preferentially interfere with Leishmania metabolism.
Di Giorgio, Carole,Shimi, Kamal,Boyer, Gerard,Delmas, Florence,Galy, Jean-Pierre
Photo-inducible cytotoxic and clastogenic activities of 3,6-di-substituted acridines obtained by acylation of proflavine
The cytotoxicity and photo-enhanced cytotoxicity of a series of 18 3,6-di-substituted acridines were evaluated on both tumour CHO cells and human normal keratinocytes, and compared to their corresponding clastogenicity as assessed by the micronucleus assa
Benchabane, Yohann,Di Giorgio, Carole,Boyer, Gerard,Sabatier, Anne-Sophie,Allegro, Diane,Peyrot, Vincent,De Meo, Michel
experimental part
p. 2459 - 2467
(2009/11/30)
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