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3,4-Dihydroquinazoline frameworks which have frequently been encountered in natural products and bioactive molecules, prompted the development of creative pharmaceuticals owing to their prominent biological properties, such as trypanothione reductase inhibitor, Hepatitis B virus inhibitive activities, anticancer activities, etc. De novo assembling of chiral 3,4-dihydroquinazolines from simple chemical feedstocks via multicomponent reactions remains several great obstacles, and this scenario is capable of the divergent and flexible modulation of these skeletons which is urgently required for drug discovery. More details are discussed in the article by Yu et al. on page 2140—2146.