The Cytotoxic Activity of Honokiol‐Triazole Derivatives in Ovarian Cancer Cells

• Published in: Bulletin of the Korean Chemical Society Vol. 40; no. 4; pp. 359 - 365
• Main Authors: Preya, Umma Hafsa, Jeon, Cheolmin, Lee, Haneul, Kang, Yujung, Wang, Yi‐Yue, Choi, Jung‐Hye, Park, Jeong Ho
• Format: Journal Article
• Language: English
• Published: Weinheim Wiley‐VCH Verlag GmbH & Co. KGaA 01.04.2019; 대한화학회
• Subjects: Anticancer activity; Apoptosis; Honokiol‐triazole derivatives; Ovarian cancer cells; 화학
• ISSN: 1229-5949; 0253-2964; 1229-5949
• DOI: 10.1002/bkcs.11691

Honokiol‐triazole derivatives (4–17) were synthesized via click reactions between 2‐ or 4′‐propargylated honokiol and azide compounds. Their anticancer activities were evaluated by using two ovarian cancer cells (A2780 and OVCAR3). Among the 14 compounds, compound 5 coupled with 4′‐propargylated honokiol and benzyl azide exhibited relatively potent cytotoxic activity (IC50 = 5.5 ± 0.5 μM for A2780 and IC50 = 3.97 ± 0.6 μM for OVCAR3) but was less toxic to normal cells (IC50 = 18.90 ± 0.9 μM for IOSE80PC). The cytotoxic effect of compound 5 is associated with caspase‐dependent apoptotic cell death via induction of intracellular reactive oxygen species.