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cc-by (c) Laura Grau, et al., 2022
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/214708

Resveratrol derivatives: Synthesis and their biological activities

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Resveratrol, a natural compound known especially for its antioxidant properties and protective action, opens the door for both it and its structural derivatives to be considered not only as chemopreventive but also as cancer chemotherapeutic agents. Due to the pharmacokinetic problems of resveratrol that demonstrate its poor bioavailability, the study of new derivatives is of interest. Thus, in this work (E)-stilbenes derived directly from resveratrol and other cyclic analogues containing the benzofuran or indole nucleus have been synthesized. The synthesized compounds have been evaluated for their ability to affect tumor growth in vitro. Compounds 2, 3, 4 and 5 have shown cytotoxicity in human colon cancer (HT-29) and human pancreatic adenocarcinoma cells (MIA PaCa-2) higher than those of (E)-resveratrol. The indolic derivative 13, a cyclic analog of resveratrol, has shown in vitro cytotoxic activity 8 times higher than resveratrol against HT-29 cancer cells. The cyclic derivatives 8, 9 and 12 showed a high inhibition of cell growth in HCT-116 (KRas mutant) at 20 μM, while 13 shows moderate antiangiogenesis activity at 10 μM.

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GRAU, Laura, SOUCEK, Richard and PUJOL DILMÉ, M. Dolors. Resveratrol derivatives: Synthesis and their biological activities. European Journal of Medicinal Chemistry. 2022. Vol. 246, num. 114962. ISSN 0223-5234. [consulted: 8 of June of 2026]. Available at: https://hdl.handle.net/2445/214708

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