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This review chronicles the exploration of the curcumin in terms of development of analogues for the anticancer activity over the last century. Curcumin is a natural phytochemical obtained from dried root and rhizome of Turmeric (Curcuma Longa). It has been shown to interfere with multiple cell signaling pathways, including apoptosis (activation of caspases and downregulation of antiapoptotic gene products), proliferation (HER-2, EGFR, and AP-1), angiogenesis (VEGF), and inflammation (NF-kappaB, TNF, IL-6, IL-1, COX-2, and 5-LOX). In the last decade it has been much explored and various synthetic analogues have been prepared and evaluated for various pharmacological activities. Most of the analogues have shown very good anticancer activity in various models and various cell lines. However, some analogues have also shown antioxidant, anti-HIV, antimutagenic, antiangiogenic, antimalarial, antitubercular, antiandrogenic, COX inhibitory activities. Few analogues have shown very potent results and may be considered as clinical candidates for the development of future anticancer agent. This review contains 728 curcumin analogues and covers the literature from 1815 to mid 2009 and 93 references are cited.