Synthesis of somatostatin analogues containing C-terminal adamantane and their antiproliferative properties.
Synthesis of somatostatin analogues containing C-terminal adamantane and their antiproliferative properties.
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DOI：
10.1021/jm701599w
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发表时间：
2008-08
影响因子：
7.3
通讯作者：
A. Miyazaki;Y. Tsuda;S. Fukushima;T. Yokoi;T. Vántus;Gyöngyi Bökönyi;E. Szabó;A. Horváth;G. Ké
中科院分区：
文献类型：
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作者：
A. Miyazaki;Y. Tsuda;S. Fukushima;T. Yokoi;T. Vántus;Gyöngyi Bökönyi;E. Szabó;A. Horváth;G. Ké
根据生长抑素类似物TT-232(1)的结构，我们合成了小的线性肽衍生物，并评估了它们的抗肿瘤和凋亡活性。其中，Boc-Tyr-D-Trp-1-adamantylamide(5)在SW480和A431细胞系中具有最有效的细胞抗增殖活性，FACS分析表明A431细胞系中subG1部分的DNA片段明显增加。
On the basis of the structure of somatostatin analogue TT-232 (1), which exhibited a highly potent antitumor activity, we synthesized small linear peptide derivatives and evaluated their antitumor and apoptotic activity. Of them, Boc-Tyr-D-Trp-1-adamantylamide (5) had the most potent cell antiproliferative activity in SW480 and A431 cell lines, which was supported in A431 cell lines by FACS analysis that demonstrated a major increase in DNA fragmentation in the subG1 fraction.