所选二酮哌嗪的合成及抗癌活性
The synthesis and anticancer activity of selected diketopiperazines.
作者信息
van der Merwe E, Huang D, Peterson D, Kilian G, Milne P J, Van de Venter M, Frost C
机构信息
Department of Pharmacy, Nelson Mandela Metropolitan University, Port Elizabeth 6031, South Africa.
出版信息
Peptides. 2008 Aug;29(8):1305-11. doi: 10.1016/j.peptides.2008.03.010. Epub 2008 Mar 18.
Six selected diketopiperazines, cyclo(Gly-Val), cyclo(Gly-D-Val), cyclo(Gly-Leu), cyclo(Gly-Ile), cyclo(Phe-Cys) and cyclo(Tyr-Cys), were synthesized via various synthetic routes. Their potential to inhibit cancer cell growth in HT-29, HeLa and MCF-7 cells was determined. Cyclo(Tyr-Cys) caused the greatest inhibition in cervical carcinoma cells with near equivalent activity against HT-29 and MCF-7 cells. The other cyclic dipeptides tested were effective in the inhibition of colon, cervical and breast carcinoma cells, respectively, but the percentage inhibition was lower than for cyclo(Tyr-Cys).
通过各种合成路线合成了六种选定的二酮哌嗪，即环（甘氨酸-缬氨酸）、环（甘氨酸-D-缬氨酸）、环（甘氨酸-亮氨酸）、环（甘氨酸-异亮氨酸）、环（苯丙氨酸-半胱氨酸）和环（酪氨酸-半胱氨酸）。测定了它们在HT-29、HeLa和MCF-7细胞中抑制癌细胞生长的潜力。环（酪氨酸-半胱氨酸）对子宫颈癌细胞的抑制作用最大，对HT-29和MCF-7细胞的活性几乎相当。测试的其他环二肽分别对结肠癌细胞、子宫颈癌细胞和乳腺癌细胞有抑制作用，但抑制百分比低于环（酪氨酸-半胱氨酸）。
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