2. Academic Validation
  3. Synthesis and antiproliferative activity of some novel derivatives of diospyrin, a plant-derived naphthoquinonoid

Synthesis and antiproliferative activity of some novel derivatives of diospyrin, a plant-derived naphthoquinonoid

  • Bioorg Med Chem. 2007 Jun 1;15(11):3672-7. doi: 10.1016/j.bmc.2007.03.050.
Madhushree Das Sarma 1,  Rina Ghosh,  Amarendra Patra,  Banasri Hazra
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Technology, Jadavpur University, Calcutta 700 032, India.
PMID: 17400463 DOI: 10.1016/j.bmc.2007.03.050
Abstract

Derivatisation of diospyrin, a bisnaphthoquinonoid isolated from Diospyros montana Roxb., led to the modification of its inhibitory activity, in vitro, towards a murine tumour model, Ehrlich ascites carcinoma (EAC), and two human Cancer cell lines, viz., malignant skin melanoma (A375) and epidermoid laryngeal carcinoma (Hep2). Among the novel derivatives, an epoxide exhibited the maximum antiproliferative activity (IC(50) values in the range of 0.03-0.21 microM) and a comparatively lower toxicity (IC(50) approximately 98 microM) in normal human peripheral blood mononuclear cells (PBMC). This compound might provide a novel 'lead' for the development of clinically effective antiproliferative agents against Cancer.

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