Progress in the Total Synthesis of Antitumor Tetrahydroisoquinoline Alkaloids

Among the tetrahydroisoquinoline(THIQ) of natural products, a family of THIQ alkaloids has the characteristics of similar biosynthetic pathway. Such THIQ alkaloids family mainly include Renieramycins, Ecteinasicdins, Tetrazaomine, Lemonomycin, etc. Most of these natural compounds have strong antitumor activities, and its family member Ecteinasicdins743 (ET-743, Trabectedin) has been marketed in the European Union and the United States for the treatment of advanced soft tissue tumors and ovarian cancer. Because of the excellent biological activity and complex chemical structure of this kind of THIQ products, it has aroused great interest of biologists and chemists, and many synthetic chemists have paid considerable efforts to their total synthesis over the past decade. Based on this, the recent advances in the total synthesis of such THIQ alkaloids are reviewed.

Automated summary

This article summarizes a family of tetrahydroisoquinoline (THIQ) alkaloids among natural products, including Renieramycins, Ecteinasicdins, Tetrazaomine, and Lemonomycin. Most of these natural compounds have strong antitumor activities, and the family member ET-743 has been marketed for the treatment of advanced soft tissue tumors and ovarian cancer. Due to the excellent biological activity and complex chemical structure, these THIQ alkaloids have attracted great interest from biologists and chemists, with many synthetic chemists dedicating significant efforts to their total synthesis in the past decade. The recent advances in the total synthesis of these THIQ alkaloids are reviewed in this article.