Novel antitumor artemisinin derivatives targeting G1 phase of the cell cycle

• Published in: Bioorganic & medicinal chemistry letters Vol. 11; no. 1; pp. 5 - 8
• Main Authors: Li, Ying, Shan, Feng, Wu, Jin-Ming, Wu, Guang-Shao, Ding, Jian, Xiao, Dong, Yang, Wei-Yi, Atassi, Ghanem, Léonce, Stéphane, Caignard, Daniel-Henri, Renard, Pierre
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 08.01.2001; Elsevier
• Subjects: Animals; Antineoplastic agents; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Apoptosis - drug effects; Artemisinins; Biological and medical sciences; Cell Division - drug effects; G1 Phase - drug effects; General aspects; Humans; Inhibitory Concentration 50; Medical sciences; Mice; Models, Molecular; Molecular Structure; Pharmacology. Drug treatments; Sesquiterpenes - chemical synthesis; Sesquiterpenes - chemistry; Sesquiterpenes - pharmacology; Sesquiterpenes - toxicity; Tumor Cells, Cultured; Antineoplastic agent; Endoperoxide; Human; Terpenoid; Nitrile; Lung; P388-Leukemia; Cytotoxicity; In vitro; Biological activity; Peracetal; G1 Phase; Cell line; Cell death; Sesquiterpenes; Cell cycle; Benzenic compound; Chemical synthesis; Apoptosis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(00)00578-3

Modification of artemisinin structure led us to the discovery of a novel class of antitumor compounds. These artemisinin derivatives containing cyano and aryl groups showed potent antiproliferative effect in vitro against P388 and A549 cells. This activity was reflected in P388 murine leukemia by an accumulation of cells in G1 phase, and induction of apoptosis.