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RESEARCH PRODUCT
Synthesis and Cytotoxicity of 1,4-Dihydropyridines and an Unexpected 1,3-Oxazin-6-one
Louis P. SandjoThomas EfferthVictor KueteVictor KueteFrederic NanaGilbert Kirschsubject
0301 basic medicine010405 organic chemistryStereochemistryChemistryOrganic ChemistrySubstituentDihydropyridineDHPSNuclear magnetic resonance spectroscopy01 natural sciencesBiochemistryCatalysis0104 chemical sciencesInorganic ChemistryNormal cell03 medical and health scienceschemistry.chemical_compound030104 developmental biologyDrug DiscoveryIc50 valuesmedicinePhysical and Theoretical ChemistryCancer cell linesCytotoxicitymedicine.drugdescription
Eight heterocycles have been prepared in a one-pot reaction manner based on the Hantzsch dihydropyridine synthesis. The synthesis afforded seven dihydropyridines (DHP) and one unexpected 1,3-oxazin-6-one. Their structures were confirmed based on NMR spectroscopy and mass spectrometry. The obtained products have been evaluated for their cytotoxicity against eight cancer cell lines and one normal cell line. Two halogenated DHPs (7 and 8) displayed cytotoxicity toward all the nine tested cancer cell lines with IC50 values from 4.10 to 58.90 μm, while others showed selective activities. DHPs (7 and 8) bearing a Me group at C(2) and C(6) as well as a halogenated substituent at C(4′) were more antiproliferative than the others.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2016-04-01 | Helvetica Chimica Acta |