Anti-tumor and Anti-Leishmanial Evaluations of 1,3,4-Oxadiazine, Pyran Derivatives Derived from Cross-Coupling Reactions of B -Bromo-6 H-1,3,4-Oxadiazine Derivatives
- Citation:
- Mohareb, R. M., and J. Schatz, "Anti-tumor and Anti-Leishmanial Evaluations of 1,3,4-Oxadiazine, Pyran Derivatives Derived from Cross-Coupling Reactions of B -Bromo-6 H-1,3,4-Oxadiazine Derivatives", Bioorganic & Medicinal Chemistry, 2011.
Abstract:
Cyanoacetylhydrazine reacted with thex-bromoacetophenones 2a,b to give hydrazide-hydrazone deriv-atives 3a,b . The latter products were cyclized to the 1,3,4-oxadiazine derivatives 4a,b . Bromination of the latter products gave the 6-bromo-6H -1,3,4-oxadiazine derivatives 5a,b which underwent a series of cross-coupling reactions. The antitumor evaluation of the newly synthesized products against the three cancer cells namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS can-cer (SF-268) showed that some of them have high inhibitory effect towards three cell lines which is higher than the standard. Moreover, the anti-leishmanial activity of the newly synthesized product was tested onLeishmania donovani amastigotes showed that some compounds have high activity.
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