Synthesis and antitumor activity of novel podophyllotoxin derivatives against multidrug-resistant cancer cells

• Published in: Journal of asian natural products research Vol. 13; no. 5; pp. 417 - 424
• Main Authors: Guo, Yong-En, Chen, Hong, Zuo, Song, Liu, Dai-Lin, Lu, Yan-Ling, Lv, Jing-Jing, Wen, Shao-Peng, Zhang, Tong-Cun
• Format: Journal Article
• Language: English
• Published: ABINGDON Taylor & Francis Group 01.05.2011; Taylor & Francis; Taylor & Francis Ltd
• Subjects: Antineoplastic agents; Antineoplastic Agents, Phytogenic - chemical synthesis; Antineoplastic Agents, Phytogenic - chemistry; Antineoplastic Agents, Phytogenic - pharmacology; antitumor; Antitumor activity; Biological and medical sciences; Cancer; Chemistry; Chemistry, Applied; Chemistry, Medicinal; Cytotoxicity; Derivatives; Drug resistance; Drug Resistance, Multiple - drug effects; Drug Screening Assays, Antitumor; General aspects; HeLa Cells; Humans; Indole; K562 Cells; KB Cells; Life Sciences & Biomedicine; Medical sciences; Molecular Structure; Multidrug resistance; multiple drug resistance; Natural products; neoplasm cells; Nutrition; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Physical Sciences; Plant Sciences; Podophyllotoxin; Podophyllotoxin - analogs & derivatives; Podophyllotoxin - chemical synthesis; Podophyllotoxin - chemistry; Podophyllotoxin - pharmacology; prepare; Science & Technology; Structure-Activity Relationship; Tumor cell lines; podophyllotoxin; prepare; ETOPOSIDE; indole; antitumor; ACIDS; AGENTS; POTENT INHIBITORS; 4'-O-DEMETHYLEPIPODOPHYLLOTOXIN; cytotoxicity; Antineoplastic agent; Human; Podophyllotoxin; Leukemia; Cytotoxicity; Podophyllotoxin derivatives; Epidermis; Uterine cervix; In vitro; Hela cell line; Biological activity; Cell line; KB cell line; Multiple resistance; Lignan; Indole derivatives; Chemical synthesis; Tumor cell
• ISSN: 1477-2213; 1028-6020; 1477-2213
• DOI: 10.1080/10286020.2011.568941

Seven novel 4β-N-substituted podophyllotoxin derivatives with indole rings were prepared and evaluated for cytotoxicity against human cancer cell lines HeLa, KB, KBV, K562, and K562/AO2. Most of them demonstrated improved antitumor activity and weak multidrug resistance compared to the drugs currently available.