2. Academic Validation
  3. Cytotoxicity of synthesized 1,4-naphthoquinone analogues on selected human cancer cell lines

Cytotoxicity of synthesized 1,4-naphthoquinone analogues on selected human cancer cell lines

  • Bioorg Med Chem. 2014 Sep 1;22(17):5013-9. doi: 10.1016/j.bmc.2014.06.013.
Navneet Kishore 1,  Brigitte Binneman 1,  Anita Mahapatra 2,  Maryna van de Venter 3,  Debbie du Plessis-Stoman 3,  Gerhardt Boukes 3,  Peter Houghton 4,  J J Marion Meyer 1,  Namrita Lall 5
Affiliations

Affiliations

  • 1 Department of Plant Science, Plant Sciences Complex, University of Pretoria, Pretoria 0002, South Africa.
  • 2 Department of Plant Science, Plant Sciences Complex, University of Pretoria, Pretoria 0002, South Africa; Department of Natural Products, National Institute of Pharmaceutical Education and Research, Ahmedabad 380054, India.
  • 3 Department of Biochemistry and Microbiology, Nelson Mandela Metropolitan University, Summerstrand Campus, Port Elizabeth 6031, South Africa.
  • 4 Department of Plant Science, Plant Sciences Complex, University of Pretoria, Pretoria 0002, South Africa; Pharmaceutical Sciences Division, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NN, UK.
  • 5 Department of Plant Science, Plant Sciences Complex, University of Pretoria, Pretoria 0002, South Africa. Electronic address: namritaup14@gmail.com.
PMID: 25059501 DOI: 10.1016/j.bmc.2014.06.013
Abstract

In an effort to establish new candidates with enhanced Anticancer activity of 5-hydroxy-7-methyl-1,4-naphthoquinone scaffold (7-methyljuglone) previously isolated from the root extract of Euclea natalensis, a series of 7-methyljuglone derivatives have been synthesized and assessed for cytotoxicity on selected human Cancer lines. These compounds were screened in vitro for Anticancer activity on MCF-7, HeLa, SNO and DU145 human Cancer cell lines by MTT assay. Most of them exhibited significant toxicity on Cancer cell lines with lower IC50 values. The most potent derivative (19) exhibited the toxicity on HeLa and DU145 cell lines with IC50 value of 5.3 and 6.8μM followed by compound (5) with IC50 value of 10.1 and 9.3μM, respectively. Structure-activity relationship reveals that the fluoro substituents at position C-8 while hydroxyl substituents at C-2 and C-5 positions played an important role in toxicity.

Keywords

7-Methyljuglone derivatives; Cell apoptosis; Cell cycle analysis; Cytotoxicity; Euclea natalensis.

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