In this tutorial review, an effort towards presentation of a comprehensive account of the recent developments on various kinds of artemisinin derivatives including artemisinin dimers, trimers and tetramers has been made and their efficacy towards malaria parasites and different cancer cells lines was compared with that of artemisinins, and various other anti-malarial and anti-cancer drugs. It is expected that this review will provide first-hand information on artemisinin chemistry to organic/medicinal chemists, and pharmacologists working on anticancer and anti-malarial drug development.