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Synthesis of novel α-aminophosphonates under microwave irradiation, biological evaluation as antiproliferative agents and apoptosis inducers

Journal Article · · Medicinal Chemistry Research (Print)
 [1];  [2]; ;  [1];  [3];
  1. Universidad Autónoma de Nuevo León, Facultad de Ciencias Químicas, Laboratorio de Química Industrial y Laboratorio de Ingeniería Genética y Genómica Av. Universidad s/n, Cd. Universitaria (Mexico)
  2. University of Alberta, Faculty of Pharmacy and Pharmaceutical Sciences (Canada)
  3. Universidad Autónoma de Nuevo León, Facultad de Medicina (Mexico)
The synthesis of two series of α-aminophosphonates was achieved by Microwave Irradiation (MW), using the one-pot Kabachnik–Fields reaction. Based on a green chemistry approach, the reactions were carried out using ethanol as the only solvent and without any catalyst, and short reaction times (20–40 min), in variable yields. Both series were tested to determine their cell proliferation inhibition activity in MDA-MB-231, MCF-7 and MCF-10A cell lines. Ethyl 4-(((diphenoxyphosphoryl)(4-(diphenylamino)phenyl)methyl)amino) benzoate 4e and diphenyl (((4-(((S)-2-hydroxy-1-phenylethyl)carbamoyl)phenyl)amino)(4-hydroxyphenyl)methyl)phosphonate 6b, showed cell proliferation inhibition activity only in the cancer cell line MCF-7 and no effect on the normal cell line MFC-10A, both compounds caused cell death by inducing apoptosis.
OSTI ID:
22936159
Journal Information:
Medicinal Chemistry Research (Print), Journal Name: Medicinal Chemistry Research (Print) Journal Issue: 11 Vol. 28; ISSN 1054-2523
Country of Publication:
United States
Language:
English

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