Core Scaffold-Inspired Concise Synthesis of Chiral Spirooxindole-Pyranopyrimidines with Broad-Spectrum Anticancer Potency

Due to the lack of tumor‐specific anticancer agents, the discovery and development of new types of highly selective anticancer agents is still a very urgent topic. Herein, we present our contribution to concise construction of novel chiral spirooxindole‐type pyranopyrimidines exhibiting a unique profile of biological activities. We have found that this new type of spiro alkaloid could inhibit the proliferation of various cancer cells in a preliminary biological evaluation. These findings suggested that spirooxindole‐type pyranopyrimidines, developed by an asymmetric Michael/cyclization strategy, can potentially serve as a new kind of anticancer candidate.