Over the past decade, a variety of benzothiazole derivatives have been reported with promising anticancer activity. Benzothiazole and its analogues are capable of acting on a number of molecular targets and thus exerting their anticancer activity. To further develop benzothiazole derivatives as anticancer agents, we attempted to design and synthesize a library of benzothiazole-triazole derivatives. The synthesized hybrid compounds have been selected by National Cancer Institute, USA for the in vitro activity evaluation against 60 human cancer cell lines in a one dose screening panel. Most of the synthesized compounds showed 60-80% growth rate against renal cancer cell line UO-31