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Synthesis and in vitro study of pseudo-peptide thioureas containing α-aminophosphonate moiety as potential antitumor agents
Ist Teil von
European journal of medicinal chemistry, 2010-11, Vol.45 (11), p.5108-5112
Ort / Verlag
Kidlington: Elsevier Masson SAS
Erscheinungsjahr
2010
Quelle
MEDLINE
Beschreibungen/Notizen
Twenty pseudo-peptide thioureas
IIa–l containing
α-aminophosphonate moiety were synthesized from the reaction of chiral
α-amino carboxamide derivatives
Ia–c with
O,
O′-dialkylisothiocyanato(phenyl)methylphosphonate
5. The synthesized compounds were completely characterized by elemental analysis, physical and spectral (IR,
1H NMR,
13C NMR) data. According to the preliminary studies on antitumor activities, compounds
IIa–l could inhibit tumor cells PC3, Bcap37 and BGC823. These compounds displayed low to high activity by MTT assays. Among them,
L-
IIk,
D-
IIa and
D-
IIe were identified as potent inhibitors, with IC
50 values ranging from 4.7 to 11.2
μM according to
in vitro assay.
The pseudo-peptide thioureas containing
α-aminophosphonate moiety were synthesized from the reaction of chiral
α-amino carboxamide derivatives with
O,O′-dialkyl isothiocyanato(phenyl)methylphosphonate. The compounds were screened for their antitumor activities.
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