Design, synthesis and biological activities of novel 3,6-diamide xanthones
10.16438/j.0513-4870.2017-0056
- VernacularTitle:3，6-二酰氨基吨酮衍生物的设计、合成及生物活性研究
- Author:
Zi-qian LI
1
;
Teng-lei FENG
1
;
Ting-ting CAO
1
;
Long ZHAO
1
;
Zeng-hui ZHOU
1
;
Rui SHEN
1
;
Zheng-yue MA
1
Author Information
1. Key Laboratory of Drug Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding 071002, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
xanthone;
G-quadruplex DNA;
molecular docking;
fluorescence spectroscopy;
cytotoxicity
- From:
Acta Pharmaceutica Sinica
2017;52(7):1133-1139
- CountryChina
- Language:Chinese
-
Abstract:
A series of novel xanthones with terminal amine substituents at xanthone's C3 and C6 positions were designed and synthesized as potential ligands for telomeric G-quadruplex DNA. All the compounds in this series were bound to telomeric G-quadruplex in a "thread intercalation" manner that illustrated both in molecular docking and spectrometric studies. Among them, 10c and 10d showed better binding abilities and specific affinity toward G-quadruplex DNA HTG21 over ctDNA in the fluorescence assay. The antiproliferative activities of four screened compounds were examined in three cancer cells by MTT in vitro, and their inhibitory effects were observed at low micromolar ranges. In addition, the PCR stop assay demonstrated that 10c and 10d effectively inhibited the amplification ability of telomerase.
