Correlation Engine 2.0
Clear Search sequence regions

Sizes of these terms reflect their relevance to your search.

A short total synthesis of tunicamycin V (1), a non-selective phosphotransferase inhibitor, is achieved via a Büchner-Curtius-Schlotterbeck type reaction. Tunicamycin V can be synthesized in 15 chemical steps from D-galactal with 21 % overall yield. The established synthetic scheme is operationally very simple and flexible to introduce building blocks of interest. The inhibitory activity of one of the designed analogues 28 against human dolichyl-phosphate N-acetylglucosaminephosphotransferase 1 (DPAGT1) is 12.5 times greater than 1. While tunicamycins are cytotoxic molecules with a low selectivity, the novel analogue 28 displays selective cytostatic activity against breast cancer cell lines including a triple-negative breast cancer. © 2022 Wiley-VCH GmbH.


Katsuhiko Mitachi, David Mingle, Wendy Effah, Antonio Sánchez-Ruiz, Kirk E Hevener, Ramesh Narayanan, William M Clemons, Francisco Sarabia, Michio Kurosu. Concise Synthesis of Tunicamycin V and Discovery of a Cytostatic DPAGT1 Inhibitor. Angewandte Chemie (International ed. in English). 2022 Aug 01;61(31):e202203225

Expand section icon Mesh Tags

Expand section icon Substances

PMID: 35594368

View Full Text