期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 30, 期 2, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.126816
关键词
Indoles; Synthesis; Tubulin polymerization; Antiproliferative activity
资金
- Natural Science Foundation of Guangdong Province, China [2018B030311067]
- National Natural Science Foundation of China [21372113]
- Science and Technology Program of Guangzhou City, China [201707010198]
A series of novel indole-based oxalamide and aminoacetamide derivatives were designed, synthesized, and evaluated for antiproliferative activities. Preliminary results revealed that compound 8g exhibited significant antiproliferative effect against PC-3, HeLa and HCT-116 cell lines. Flow cytometric analysis of the cell cycle demonstrated the compound 8g induced the cell cycle arrest at G2/M phase in HeLa cell lines. Immunocytochemistry revealed loss of intact microtubule structure in cells treated with 8g and inhibition of tubulin polymerization. Additionally, molecular docking analysis suggested that 8g formed stable interactions in the colchicine-binding site of tubulin. These preliminary results demonstrated that a new class of novel indole-based oxalamide and aminoacetamide derivatives described in the investigation could be developed as potential scaffolds to new anticancer agents.
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