Cinnamic acid and its phenolic analogues are natural substances. Chemically, cinnamic acids or the 3-phenyl acrylic acids, offer three main reactive sites: substitution on the phenyl ring, addition on the α ,β -unsaturation and reactions of the carboxylic acid. Owing to these chemical aspects, cinnamic acid derivatives received much attention in medicinal research as traditional as well as valuable scaffolds in recent synthetic bioactive agents. In the last two decades, there has been huge attention towards various cinnamoyl derivatives and their biological efficacy. This review provides a comprehensive literature compilation concerning the synthesis of various cinnamoyl acids, esters, amides, hydrazides and related derivatives and their biological activity evaluations against diseases such as tuberculosis and malaria, which are frequent in developing countries and cardiovascular diseases, which cause a high mortality rate worldwide. We envisage that our effort in this review contributes a much needed and timely addition to the literature of medicinal research.