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Synthesis and biological evaluation of benzimidazole fused ellipticine derivatives as anticancer agents

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Abstract

A series of ten novel benzimidazole fused ellipticine derivatives have been synthesized and these compounds were evaluated for their antiproliferative activity against four human cancer cell lines (Zr-75-1, MCF-7, HeLa, and A-549). It is observed that all the synthesized compounds showed significant antiproliferative activity with GI50 values ranging from <0.1 to 34.6 μM, while the positive control, etoposide demonstrated the GI50 in the range of 0.2–3.08 μM, respectively. Some of the compounds were distinctly more potent than etoposide, with GI50 concentrations in the submicromolar level on certain cell lines.

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Acknowledgments

N. Bramhananda Reddy thankful to department of Chemistry, Sri Krishnadevaraya University, Anantapur for providing research facilities; Reddymasu Sreenivasulu thankful to Acharya Nagarjuna University, Nagarjuna Nagar for providing HPLC data to test the purity of compounds before doing the cancer activity studies and Dr. Palle Sadanandam thankful to Department of Science & Technology, India for financial assistance in the form of Young Scientist major research project F. No. SB/FT/CS-141/2013.

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Correspondence to Reddymasu Sreenivasulu.

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Bramhananda Reddy, N., Burra, V.R., Ravindranath, L.K. et al. Synthesis and biological evaluation of benzimidazole fused ellipticine derivatives as anticancer agents. Monatsh Chem 147, 599–604 (2016). https://doi.org/10.1007/s00706-016-1684-z

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  • DOI: https://doi.org/10.1007/s00706-016-1684-z

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