Antiproliferative Activity of Natural Taiwaniaquinoids and Related Compounds

• Published in: Journal of natural products (Washington, D.C.) Vol. 80; no. 2; pp. 308 - 318
• Main Authors: Guardia, Juan J, Tapia, Rubén, Mahdjour, Soumicha, Rodriguez-Serrano, Fernando, Mut-Salud, Nuria, Chahboun, Rachid, Alvarez-Manzaneda, Enrique
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society and American Society of Pharmacognosy 24.02.2017; Amer Chemical Soc
• Subjects: Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Cell Proliferation - drug effects; Chemistry, Medicinal; Drug Screening Assays, Antitumor; Female; Humans; Life Sciences & Biomedicine; MCF-7 Cells; Molecular Structure; Pharmacology & Pharmacy; Plant Sciences; Science & Technology; Stereoisomerism; Taiwan; Terpenes - chemistry; Terpenes - pharmacology; DITERPENES; (+/-)-DICHROANAL-B; PRODUCTS; BARK; EFFICIENT ROUTE; SYNTHETIC BIOLOGY; ANTITUMOR; DERIVATIVES; (+/-)-TAIWANIAQUINOL-B; SKELETON
• ISSN: 0163-3864; 1520-6025
• DOI: 10.1021/acs.jnatprod.6b00700

The in vitro antiproliferative activities of some taiwaniaquinoids and related compounds with functionalized A, B, or C rings against human breast (MCF-7), colon (T-84), and lung (A-549) tumor cell lines were assayed. The most potent compounds, 16, 27, and 36, were more effective than the naturally occurring taiwaniaquinones A (4) and F (5) in all three cell lines. The structure–activity relationship study of these new taiwaniaquinoids highlighted the correlation between the bromo substituent and the antiproliferative activity, especially in MCF-7 cells. These findings indicate that some of the taiwaniaquinoids might be useful as cytostatic agents against breast, colon, and lung cancer cell lines.