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ID: ALA1275305

Journal: Eur J Med Chem

Title: Synthesis and in vitro study of pseudo-peptide thioureas containing α-aminophosphonate moiety as potential antitumor agents.

Authors: Liu JZ, Song BA, Fan HT, Bhadury PS, Wan WT, Yang S, Xu W, Wu J, Jin LH, Wei X, Hu DY, Zeng S.

Abstract: 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, (1)H NMR, (13)C 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.

CiteXplore: 20817326

DOI: 10.1016/j.ejmech.2010.08.021