Add time:07/29/2019         Source:sciencedirect.com

A series of new 4β-anilino-4′-O-demethyl-4-desoxypodophyllotoxin derivatives were prepared and evaluated for their cytotoxicities against four human cancer cell lines including KB, KB/VCR, A549 and 95D. Most compounds showed better growth-inhibition activities against tested cell lines than that of etoposide (VP-16). Preliminary structure–activity relationships (SARs) were concluded and it indicated that the side chains substituted at 4β position of podophyllotoxin significantly influenced the cytotoxic activity, especially for the drug resistance profile. In vivo studies of compound 26c on highly metastatic human lung cancer xenograft in nude mice showed that it can significantly inhibit tumor growth with administrating by oral route.

► Three classes of 4β-Anilino-4′-O-demethyl-4-desoxypodophyllotoxin derivatives were designed and synthesized with the aim to improve the antiproliferative activity of etoposide as well as the drug-resistance profile. ► Most target compounds were identified as potent antitumor agents and showed improved activities comparing with their parent compound. ► Compound 26c exhibited as a promising agent that can be orally administered, and at 50 mg/kg it significantly inhibited high metastatic human lung cancer growth.

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