Isatin-β-thiosemicarbazones as potent herpes simplex virus inhibitors

• DOI: 10.1016/j.bmcl.2011.02.037
• Publication Date: 2011-02-16T18:01:40Z
• Authors: Iou-Jiun Kang; Li-Wen Wang; Tsu-An Hsu; Andrew Yueh; Chung-Chi Lee; Yen-Chun Lee; Ching-Yin Lee; Yu-Sheng Chao; Shin-Ru Shih; Jyh-Haur Chern
• Keywords: Isatin; Cell Line, Tumor; Herpesvirus 2, Human; Humans; Herpesvirus 1, Human; Drug Screening Assays, Antitumor; Antiviral Agents; 01 natural sciences; 0104 chemical sciences; 3. Good health

A series of isatin-β-thiosemicarbazones have been designed and evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in a plaque reduction assay. Their cytotoxicity was examined using human rhabdomyosarcoma cells (RD cells). Several derivatives of isatin-β-thiosemicarbazone exhibited significant and selective antiviral activity with low cytotoxicity. It was found that the thiourea group at thiosemicarbazone and the NH functionality at isatin were essential for their antiherpetic activity. The synthesis and structure-activity relationship studies are presented.