Microwave Assisted Synthesis of Novel Six-Membered 4-C, 4-O and 4-S Lactams Derivatives: Characterization and in vitro Biological Evaluation of Cytotoxicity and Anticoagulant Activity
AUTOR(ES)
Núñez-Navarro, Nicolás E., Segovia, Gerardine F., Burgos, Renato A., Lagos, Carlos F., Fuentes-Ibacache, Nataly, Faúndez, Mario A., Zacconi, Flavia C.
FONTE
J. Braz. Chem. Soc.
DATA DE PUBLICAÇÃO
2017-02
RESUMO
A series of six-membered lactam derivatives containing C, O and S atoms in position 4 were synthesized using microwave methodology through coupling reactions. The novel compounds were synthesized following two step reaction to yield fifteen derivatives. The final derivative N-(4-(3-oxotiomorpholin)phenyl) hexanamide was selectively toxic to the HCT-116 cell line over the HeLa cancerous and HEK-293 human non-malignant control cells with low inhibition Factor Xa (FXa) activity. The new products were characterized by spectral data including 1H and 13C nuclear magnetic resonance (NMR), infrared (IR) and high-resolution mass spectrometry (HRMS). Cytotoxicity of products on HCT-116, HeLa, HEK-293 cell lines and FXa activity assays are also reported.
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