2-hydroxy-methyl-1(N-phtaloyltryptophyl) aziridine stimule la prolifération in vitro des lymphocytes humains et la sécrétion des interleukines

Synthesis of a Novel Class of Phosphonoaziridines as Interesting Antibacterial Agents

“…The same approach was successfully applied to generate aziridines from N-phtaloylamino acids 13. Phenylalanine and tyrosine were chosen as a models, since in our initial work in this field [27], aziridine from the former amino acid showed the best biological profile [28], whereas tyrosine is claimed to behave as a residue of utmost importance in many receptors [41]. Derivatives 13 were prepared according to a modified literature procedure [42] and were recrystallized.…”

“…As compared to our initial work [27], the present study has allowed us develop a second class of aziridines of interesting biological activities, represented by compound 7. The phtaloyl derivatives were active against breast cancer cells [28] whereas phosphonate showed antibacterial activitiy. Work is going on for the diversification of the initial work, especially for the search of targeted cancer chemotherapy, through the synthesis of hybrids.…”

“…The biological activity of aziridines is highly related to the establishment of covalent bond with DNA [26]. In a previous work we reported the synthesis of aziridinyl derivatives [27] that had antitumor activities against breast cancer cells [28]. Such a behaviour was likely due to their capacity to strengthen and modulate the immune system [29].…”