Abstract

Natural products and their semisynthetic derivatives continue to be an important source of potential drug leads. Natural products and their analogues structures possess the characteristics of high chemical diversity, zenith biochemical specificity, and other significant molecular activities as well as pharmacological properties that create them favorably as lead structures for new drug discovery and continue to motivate novel inventions in medicine, chemistry, and biology. Natural products were employed as very good starting materials for analogue design and synthesis as semisynthetic derivatives exhibit higher biological activities in several cases. Such beneficial quality of semisynthetic derivatives as a whole have motivated the organic chemist and biological community to explore the application of semisynthetic derivatives in more heights and as a result, the present review is aimed to offer an overview of natural sources of the starting natural compounds, semisynthesis and biological activities of semisynthetic derivatives during the last decade. • Semisynthesis and biological activities of semisynthetic derivatives have been explored during the last decade. • A semisynthesis is an essential tool for enhancing the biological property of parent natural products. • Inserting halogen atoms in natural products are excellent examples of chemical modifications. • The chemical derivatization represents the only practical means to study structure-activity relationships. • Natural products and their analogues continue to be the monumental source of potential drug leads.

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