ArticleEuropean journal of medicinal chemistry2014
Toward synthesis of third-generation spin-labeled podophyllotoxin derivatives using isocyanide multicomponent reactions.
Article in European journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Chemistry and Biological Activities of Naturally Occurring and Structurally Modified Podophyllotoxins.Molecules (Basel, Switzerland) · 2022Review
- Expanding the Chemical Space of Drug-like Passerini Compounds: Can α-Acyloxy Carboxamides Be Considered Hard Drugs?ACS medicinal chemistry letters · 2022Article
- Design, Semisynthesis, and Estrogenic Activity of Lignan Derivatives from Natural Dibenzylbutyrolactones.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Synthesis of Biologically Active Molecules through Multicomponent Reactions.Molecules (Basel, Switzerland) · 2020Review
- Article
- Nitroxides as Antioxidants and Anticancer Drugs.International journal of molecular sciences · 2017Review
- Design and synthesis of novel spin-labeled camptothecin derivatives as potent cytotoxic agents.Bioorganic & medicinal chemistry · 2014Article
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Authors and funding
9 authors.
Funding
Abstract
Spin-labeled podophyllotoxins have elicited widespread interest due to their far superior antitumor activity compared to podophyllotoxin. To extend our prior studies in this research area, we synthesized a new generation of spin-labeled podophyllotoxin analogs via isocyanide multicomponent reactions and evaluated their cytotoxicity against four human cancer cell lines (A-549, DU-145, KB and KBvin). Most of the compounds exhibited potent cytotoxic activity against all four cell lines, notably against the drug resistant KBvin cancer cell line. Among the new analogs, compounds 12e (IC50: 0.60-0.75 μM) and 12h (IC50: 1.12-2.03 μM) showed superior potency to etoposide (IC50: 2.03 to >20 μM), a clinically available anticancer drug. With a concise efficient synthesis and potent cytotoxic profiles, compounds 12e and 12h merit further development as a new generation of epipodophyllotoxin-derived antitumor clinical trial candidates.
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