European Journal of Medicinal Chemistry p. 5108 - 5112 (2010)
Update date:2022-08-05
Topics:
Liu, Jing-Zi
Song, Bao-An
Fan, Hui-Tao
Bhadury, Pinaki S.
Wan, Wen-Ting
Yang, Song
Xu, Weiming
Wu, Jian
Jin, Lin-Hong
Wei, Xue
Hu, De-Yu
Zeng, Song
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 IC50 values ranging from 4.7 to 11.2 μM according to in vitro assay.
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