Synthesis and antiproliferative activity of some novel derivatives of diospyrin, a plant-derived naphthoquinonoid.
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.
Das Sarma
Madhushree
M
Department of Pharmaceutical Technology, Jadavpur University, Calcutta 700 032, India.
Ghosh
Rina
R
Patra
Amarendra
A
Hazra
Banasri
B
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects*; D029788:Diospyros / Q000737:chemistry; D004195:Disease Models, Animal; D006801:Humans; D020128:Inhibitory Concentration 50; D007963:Leukocytes, Mononuclear / Q000187:drug effects; D051379:Mice; D009285:Naphthoquinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D024301:Plant Bark / Q000737:chemistry; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D009285:Naphthoquinones; C043546:diospyrin