Synthesis and Biological Evaluation of Some Novel Substituted Pyrrolizines and Pyrimidopyrrolizines as Chemotherapeutic Agents

A novel series of 3-ethyl ester substituted pyrrolizines (4, 5, 8-11, 14a,b, 15-19c), 3-oxadiazinyl substituted pyrolizines (21-23b, 25-27b), 3-carboxilic acid substituted pyrrolizine (7) and pyrimidopyrrolizines (6, 12, 14a,b, 24a,b, 28a,b) were synthesized. Their chemical structures were confirmed by spectral and elemental analysis. Ten compounds of these new derivatives showed activity against MCF7 cancer cell line with IC₅₀ value less than 60 μM. Moreover, compound ethyl 2-{[aminomethylene]amino}-1-cyano -6,7-dihydro-5H-pyrrolizine-3-carboxylate (11) that was prepared by facile chemical reaction of the ethyl ester start 3 with formamide, showed activity on candida albicans equipotent with that of clotrimazole.

Author(s): Samir M El-Moghazy, Mona M Hanna, Awatef El-Said Farag, Amany Belal

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