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Updated: Jun 16, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design and synthesis of C-ring lactone- and lactam-based podophyllotoxin analogues as anticancer agents
Pragya Singh1, Uzma Faridi, Suchita Srivastava
1Central Institute of Medicinal and Aromatic Plants (CIMAP-CSIR), P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow-226 015, India.
Abstract:
A series of novel podophyllotoxin (PDT) analogues was synthesized in which the lactone moiety was shifted to C ring. Some of the derivatives were also synthesized with modified A ring. Analogues 23 and 25 exhibited potent in vitro cytotoxicity against colon cancer (CaCO(2)) cell line. p-Demethylated E-ring analogues exhibited better potency than the corresponding methylated analogues. These analogues showed toxicity comparable to PDT against human erythrocytes albeit at much higher concentrations (100 microg/ml) than their cytotoxicity values.
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