The Reaction of Cyanoacetylhydrazine with Chloroacetone: Synthesis of 1,2,4-Triazine, 1,3,4-Oxadiazine and Their Fused Derivatives with Antitumor Activities

The reaction of cyanoacetylhydrazine with chloroacetone gave the N-(1-chloropropan-2-ylidene)-2-cyanoacetohy- drazide. This compound reacted with either hydrazine hydrate or phenylhydrazine to give the corresponding 1,2,4-tri- azine derivatives. On the other hand, its reaction with either benzenediazonium chloride or benzaldehyde gave in each case the 1,3,4-oxadiazine derivatives. Moreover, the reaction of the cyanoacetylhydrazine with 2-boromocyclohexa- none gave the corresponding hydrazine-hydrozon derivative. The antitumor evaluation of the newly synthesized prod- ucts against three cancer cell lines, namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) was recorded. Some of the tested compounds showed activities which was higher than the reference doxorubicin.

The Reaction of Cyanoacetylhdrazine with Furan-2-Aldehyde: Novel Synthesis of Thiophene, Azole, Azine and Coumarin Derivatives and Their Antitumor Evaluation

The reaction of cyanoacetylhydrazine 1 with furan-2-aldehyde 2 gives the hydrazide-hydrazone derivative 3. The latter compound undergoes a series of heterocyclization reactions to give new heterocyclic compounds. The antitumor evaluation of the newly synthesized products against three cancer cell lines, namely breast adenocarcinoma (MCF-7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) were recorded. Some of the synthesized compounds show high inhibitory effects.