| Literature DB >> 21737288 |
Ahmed Kamal1, Paidakula Suresh, M Janaki Ramaiah, Adla Mallareddy, Banala Ashwini Kumar, Paidakula Raju, J Vinay Gopal, S N C V L Pushpavalli, A Lavanya, Pranjal Sarma, Manika Pal-Bhadra.
Abstract
A series of new 4β-acrylamidopodophyllotoxin derivatives (13a-o) were synthesized by coupling of substituted acrylic acids (10a-l and 11m-o) to the 4β-aminopodophyllotoxin. The synthesized derivatives 13a-o were evaluated for their cytotoxicity against five human cancer cell lines (breast, oral, colon, lung and ovarian). These podophyllotoxin conjugates have shown promising activity with GI₅₀ values ranging from <0.1 to 0.29 μM. Some of the compounds 13j, 13k and 13l that showed significant antiproliferative activity were also evaluated for related cytotoxic effects in MCF-7 cells, and compared to etoposide. These compounds (13j, 13k and 13l) showed G2/M cell cycle arrest and the apoptotic event was found to be due to both the single-strand DNA breaks as observed by comet assay as well as double-strand breaks as observed by the large accumulation of gamma H2AX foci.Entities:
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Year: 2011 PMID： 21737288 DOI： 10.1016/j.bmc.2011.06.017
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641