The unique physicochemical properties invest fused heterocyclic compounds with wide applications in the synthesis of natural products, drugs, superconducting materials, energy storage materials, polymer materials, organic dyes, etc. In recent years, the rapid development of transition metal-catalyzed reactions of unsaturated hydrocarbons has developed rapidly. Owing to the advantages of high step-and atom-economy, easy availability of raw starting materials, and efficient construction of carbon-carbon bonds or/and carbon-hetero bonds, it is a vital way to synthesize fused heterocyclic compounds. Herein, the recent progress on the reaction development of transition metal-catalyzed cyclizations involving unsaturated hydrocarbons for the synthesis of fused heterocyclic compounds including benzofurans, indoles, quinolines in the last five years has been summarized, as well as their applications in the field of medicinal chemistry with antitumor activities. Keywords unsaturated hydrocarbons; transition metal-catalysis; fused heterocyclic compounds; antitumor activity 稠杂环化合物是指苯环与杂环或杂环与杂环稠合 在一起的化合物(如吲哚、喹啉、嘌呤等 [1][2][3] ). 由于稠杂 环化合物通常具有独特的生物活性、低毒性和高内吸收 性 [4][5][6][7] , 经常用作医药活性分子和农药的结构单元 [8][9][10][11] . 到目前为止, 全球销售额前 200 的药物中许多化合物含 有稠杂环结构(图 1).