2. Academic Validation
  3. Design and synthesis of β-carboline linked aryl sulfonyl piperazine derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability

Design and synthesis of β-carboline linked aryl sulfonyl piperazine derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability

  • Bioorg Chem. 2020 Aug;101:103983. doi: 10.1016/j.bioorg.2020.103983.
Kesari Lakshmi Manasa 1,  Sowjanya Thatikonda 2,  Dilep Kumar Sigalapalli 1,  Arpita Sagar 3,  Gaddam Kiranmai 4,  Arunasree M Kalle 3,  Mallika Alvala 5,  Chandraiah Godugu 2,  Narayana Nagesh 6,  Bathini Nagendra Babu 7
Affiliations

Affiliations

  • 1 Department of Fluoro-Agrochemicals, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India; Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
  • 2 Department of Regulatory Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
  • 3 Department of Animal Biology, School of Life Sciences, University of Hyderabad, Hyderabad 500 046, India.
  • 4 CSIR-Centre for Cellular and Molecular Biology, Hyderabad 500 007, India.
  • 5 Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
  • 6 CSIR-Centre for Cellular and Molecular Biology, Hyderabad 500 007, India. Electronic address: nagesh@ccmb.res.in.
  • 7 Department of Fluoro-Agrochemicals, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India. Electronic address: bathini@iict.res.in.
PMID: 32683136 DOI: 10.1016/j.bioorg.2020.103983
Abstract

A series of new β-carboline linked aryl sulfonyl piperazine congeners have been synthesized by coupling various β-carboline acids with substituted aryl sulfonyl piperazines. Evaluation of their Anticancer activity against a panel of human Cancer cell lines such as colon (HT-29), breast (MDA-MB-231), bone osteosarcoma (MG-63), brain (U87 MG), prostate (PC- 3) and normal monkey kidney (Vero) cell line has been done. Among the series, compound 8ec and 8ed has shown most potent cytotoxicity with an IC50 values of 2.80 ± 0.10 µM and 0.59 ± 0.28 µM respectively against MG-63 cell line and also potent on other cell lines tested. Compounds 8ec and 8ed was found to inhibit Topo II that is confirmed by specific Topo II inhibition assay. DNA binding studies, cell cycle analysis, Annexin V study indicate that these compounds has potential Anticancer activity. Molecular docking studies for compound 8ec and 8ed are incorporated to understand the nature of interaction with Topoisomerase IIα and dsDNA.

Keywords

Aryl sulfonyl piperazine; Cytotoxicity and Molecular docking; DNA binding studies; Topoisomerase II inhibition; β-carboline.

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