Synthesis and in vitro study of pseudo-peptide thioureas containing α-aminophosphonate moiety as potential antitumor agents
Synthesis and in vitro study of pseudo-peptide thioureas containing α-aminophosphonate moiety as potential antitumor agents
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DOI：
10.1016/j.ejmech.2010.08.021
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发表时间：
2010-11-01
影响因子：
6.7
通讯作者：
Zeng, Song
中科院分区：
文献类型：
--
作者：
Liu, Jing-Zi;Song, Bao-An;Zeng, Song
由手性α-氨基甲酰胺衍生物Ia ~ c与O，O '-二烷基异硫氰酸基（苯基）甲基膦酸酯5反应，合成了20个含α-氨基膦酸酯部分的假肽硫脲IIa-1。所合成的化合物通过元素分析、物理和光谱（IR、H-1 NMR、C-13 NMR）数据进行了全面的表征。初步的抗肿瘤活性研究表明，化合物IIa-1对肿瘤细胞PD、Bcap 37和BGC 823均有抑制作用。这些化合物通过MTT测定显示出低至高的活性。其中，L-Ilk、D-IIa和D-IIe被鉴定为有效抑制剂，根据体外测定，IC 50值范围为4.7至11.2 μ M。(C)2010年Elsevier Masson SAS。All rights reserved.
Twenty pseudo-peptide thioureas IIa-1 containing alpha-aminophosphonate moiety were synthesized from the reaction of chiral alpha-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, H-1 NMR, C-13 NMR) data. According to the preliminary studies on antitumor activities, compounds IIa-1 could inhibit tumor cells PD, Bcap37 and BGC823. These compounds displayed low to high activity by MTT assays. Among them, L-Ilk, D-IIa and D-IIe were identified as potent inhibitors, with IC50 values ranging from 4.7 to 11.2 mu M according to in vitro assay. (C) 2010 Elsevier Masson SAS. All rights reserved.