韦可心,童洋,胡磊,姜欣怡,肖银银,梁光义,徐必学
WEI Kexin,TONG Yang,HU Lei,JIANG Xinyi,XIAO Yinyin,LIANG Guangyi,XU Bixue

• 1:贵阳中医学院
• 2:贵州医科大学省部共建药用植物功效与利用国家重点实验室
• 3:贵州省中国科学院天然产物化学重点实验室
• 4:遵义医学院

摘要(Abstract)：

目的:探讨L-苯丙氨酸二肽衍生物的合成及其抗肿瘤活性。方法:以L-酪氨酸或L-苯丙氨酸为原料,依次酰化反应、缩合反应、亲核取代及烷基化等反应合成得到苯丙氨酸二肽衍生物,并用噻唑蓝(MTT)法测定其对人前列腺癌细胞(PC3)、人慢性髓原白血病细胞(K562)、人红白细胞白血病细胞(HEL)3类肿瘤细胞株的抗肿瘤活性。结果:共合成了3a~3h共8个未见文献报道的苯丙氨酸二肽衍生物,MTT结果显示,部分衍生物对K562细胞株具有一定抑制作用,衍生物3b,3e,3f对PC3和K562有较好的抑制作用。结论:合成了8个新的苯丙氨酸二肽衍生物,其对K562及PC3肿瘤细胞株具有一定的抑制作用。
Objective: To synthesize L-phenylalanine dipeptide derivatives and study their inhibitory effects on tumor cells. Methods: Starting from L-tyrosine or L-phenylalanine,L-phenylalanine dipeptide derivatives were synthesized via acetylation,condensation,nucleophilic substitution and/or alkylation. The cell proliferation inhibiting activities of the derivatives were evaluated by thiazolyl blue tetrazolium bromide( MTT) method. Results: A total of 8 3 a ~ 3 h phenylalanine dipeptide derivatives were synthesized. Some of the target compounds showed certain inhibitory effect against leukemia cell lines K562 and HEL in vitro. Furthermore,the derivatives 3 b,3 e and 3 f had preferably inhibitory effect on prostate cancer cell line PC3 and K562 cells in vitro. Conclusions: Phenylalanine dipeptide derivatives possess good inhibitory effects on the leukemia and prostate cancer cells and are worth of further research.

关键词(KeyWords)： 苯丙氨酸二肽;衍生物;结构设计;合成;抗肿瘤活性;癌细胞株,人前列腺,白血病
phenylalanine dipeptide;derivatives;structural design;synthesis;anti-tumor activity;cancer cell line;human prostate;leukemia

Abstract:

Keywords:

基金项目(Foundation): 黔人项目资助合同(2014)7号;; 国家自然科学基金资助项目(81360472)

作者(Author): 韦可心,童洋,胡磊,姜欣怡,肖银银,梁光义,徐必学
WEI Kexin,TONG Yang,HU Lei,JIANG Xinyi,XIAO Yinyin,LIANG Guangyi,XU Bixue

DOI: 10.19367/j.cnki.1000-2707.2018.05.008

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