title: Anti-tumor and anti-leishmanial evaluations of 1,3,4-oxadiazine, pyran derivatives derived from cross-coupling reactions of β-bromo-6H-1,3,4-oxadiazine derivatives.
abstract: Cyanoacetylhydrazine reacted with the ω-bromoacetophenones 2a,b to give hydrazide-hydrazone derivatives 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 cancer (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 on Leishmania donovani amastigotes showed that some compounds have high activity.
authors: Faculty of Pharmacy, Organic Chemistry Department, October University for Modern Science and Arts University, October City, Egypt. raafat_mohareb@yahoo.com
authors: Rafat M
authors: RM
authors: Mohareb
authors: Jürgen
authors: J
authors: Schatz
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D003500:Cyclization; D004354:Drug Screening Assays, Antitumor; D054879:Halogenation; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D006835:Hydrazones / Q000737:chemistry; D007891:Leishmania / Q000187:drug effects*; D021261:Parasitic Sensitivity Tests; D011714:Pyrans
chemical_list: D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds; D006835:Hydrazones; D011714:Pyrans