Design, synthesis, and biological antitumor evaluation of tetrahydroisoquinoline derivatives.

Bioorg Med Chem Lett

State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China. Electronic address:

Published: September 2024

Cancer, as a public health issue, is the leading cause of death worldwide. Tetrahydroisoquinoline derivatives have effective biological activities and can be used as potential therapeutic agents for antitumor drugs. In this work, we designed and synthesized a series of novel tetrahydroisoquinoline compounds and evaluated their antitumor activity in vitro on several representative human cancer cell lines. The results showed that the vast majority of compounds showed good inhibitory activities against the cancer cell lines of HCT116, MDA-MB-231, HepG2, and A375.

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http://dx.doi.org/10.1016/j.bmcl.2024.129824DOI Listing

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Article Synopsis
  • The study focused on synthesizing new compounds, specifically 5,6,7,8-tetrahydroisoquinolines and 6,7,8,9-tetrahydrothieno[2,3-c]isoquinolines, and confirmed their structures using various spectroscopic techniques.
  • Anticancer activities of these new compounds were tested against eight tumor cell lines, revealing that compound 3 was most effective against the HEPG2 cell line and compound 9c against the HCT116 cell line.
  • Further analysis showed that compound 3 induced significant apoptosis and cell cycle arrest in HEPG2 cells, while molecular docking studies indicated that compounds 3
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