Design and synthesis of 4β-Acetamidobenzofuranone-podophyllotoxin hybrids and their anti-cancer evaluation

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2153-2156. doi: 10.1016/j.bmcl.2019.06.060.

Suresh Paidakula ¹, Srinivas Nerella ², Ravinder Vadde ², Ahmed Kamal ³, Shravankumar Kankala ⁴

Affiliations

1 Department of Chemistry, Kakatiya University, Warangal 506009, India; Centre for Semio Chemicals, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad 500007, India. Electronic address: sureshpaidakula@gmail.com.
2 Department of Chemistry, Kakatiya University, Warangal 506009, India.
3 Centre for Semio Chemicals, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad 500007, India; School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi 110062, India.
4 Department of Chemistry, Kakatiya University, Warangal 506009, India. Electronic address: shravankankala@yahoo.com.

PMID: 31281022 DOI: 10.1016/j.bmcl.2019.06.060

Abstract

A new series of amide derivatives of 4β-Acetamidobenzofuranone-podophyllotoxin hybrids (14a-g) were synthesized and their chemical structures were confirmed by ¹H, ¹³C NMR and mass spectral data. Further, all the synthesized Acetamidobenzofuranone-podophyllotoxin hybrids were evaluated for in vitro cytotoxic activity against a panel of four human Cancer cell lines i.e., human breast (MCF-7, MDA MB-231), lung (A549), and prostrate (DU-145). Among benzofuranone-podophyllotoxin hybrid compounds, 14b and 14e were exhibited more potent activity than standard drug and 14c and 14f were showed Anticancer activity equivalent to etoposide.

Keywords

Acetamidobenzofuranone; Anti-cancer activity; Benzofuranone-podophyllotoxin hybrids; Etoposide; Teniposide.

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