Design, synthesis and cytotoxic activities of fluorine-containing 2, 5-diketopiperazine derivatives
10.11665/j.issn.1000-5048.20160405
- VernacularTitle:含氟2,5-二酮哌嗪衍生物的设计、合成及细胞毒活性
- Author:
Yong TANG
1
;
Shengrong LIAO
;
Jinsheng LI
;
Yonghong LIU
Author Information
1. 中国科学院南海海洋研究所；中国科学院大学
- Publication Type:Journal Article
- Keywords:
2,5-diketopiperazine derivative;
fluorine-containing;
synthesis;
cytotoxic activity
- From:
Journal of China Pharmaceutical University
2016;47(4):412-412
- CountryChina
- Language:Chinese
-
Abstract:
Twenty-one novel fluorine-containing 2, 5-diketopiperazine derivatives(2a-2u)were synthesized by using N, N-diacetyl-2, 5-diketopiperazine, allylbromide, 2-fluorobenzaldehyde and other aromatic aldehydes. The structures were characterized by 1H NMR, 13C NMR, and HRMS. The cytotoxicities were evaluated against ten human tumour cell lines(K562, U937, MOLT-4, HL60, HeLa, DU145, MCF-7, A549, SGC-7901, H1975)by using CCK8 assay. Results showed that compounds 2a, 2d, 2e, 2f, 2g, 2h, 2k, and 2t showed significant cytotoxicity against U937(IC50=0. 2 μmol/L), HeLa(IC50=0. 5 μmol/L), and DU145(IC50=0. 7 μmol/L), respectively. Compound 2t could become a lead compound for further development for anticancer agents.
