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Paper | Regular issue | Vol 104, No. 6, 2022, pp.1085-1097
Published online, 22nd April, 2022
DOI: 10.3987/COM-22-14652
Synthesis and Antitumor Activity of Novel Linear Tricyclic Compounds Derived from Purine

Hongmei Guo, Lifei Nie, Khurshed Bozorov, Haji Akber Aisa,* and Jiangyu Zhao*

*State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, 40-1 South Beijing Road Urumqi, Xinjiang 830011, China


Synthesis and antitumor activity of two series of novel linear tricyclic purine derivatives were reported. The structures of new compounds were characterized by 1H NMR, 13C NMR, HRMS (ESI). The inhibitory activities of the synthesized compounds were evaluated by conventional MTT assay against HT-29 human colorectal adenocarcinoma cell line, MCF-7 breast cancer cell line, and HeLa human cervical cancer cell. The compounds 5n~5q with long-chain alkane revealed the better inhibitory effect against all three kinds of cancer cells, while the compounds 4a~4l and 5a~5l with different substituted phenyl seemed to be more beneficial for the HeLa cell. Meanwhile, the toxicity of compounds 5m~5q against L-02 normal human liver cell was tested. The compound 5q showed promising antitumor activity in vitro against HT-29 (IC50 = 3.28 ± 0.57 μM), MCF-7 (IC50 = 7.13 ± 0.27 μM), and HeLa (IC50 = 14.24 ± 0.41 μM) cell lines and relatively low toxicity against L-02 (IC50 >100 μM) cell. The results suggested that compound 5q could serve as the promising antitumor lead compound for further research.