| Literature DB >> 29501940 |
Devi Amujuri1, Bandi Siva1, B Poornima1, Katukuri Sirisha2, A V S Sarma2, V Lakshma Nayak3, Ashok K Tiwari3, U Purushotham4, K Suresh Babu5.
Abstract
A new series of Schizandrin (1) derivatives were synthesized utilizing the C-9 position of the Schizandrin core and evaluated for their cytotoxic activities against HeLa (cervical cancer), A549 (lung cancer), MCF-7 (breast cancer) and DU-145 (prostate cancer) cell lines. Among the synthesized series, 4e, 4f, 4g and 5 showed potent activities against tested cell lines. More significantly, compound 5 exhibited most potent cytotoxic activity against DU-145 with an IC50 value of 1.38 μM which is comparable to the standard agent, doxorubicin. Further, flow cytometry analysis indicated that 5 arrested cells in G2/M phase and consequently leading to apoptosis. Molecular docking analysis showed that 5 occupied the colchicine binding pocket of tubulin. Overall, the present study demonstrates that 5, as a mitotic-agent.Entities:
Keywords: Cytotoxic activities; Docking; Flow cytometric analysis; Schizandrin; Synthesis
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Year: 2018 PMID： 29501940 DOI： 10.1016/j.ejmech.2018.02.066
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514