TY - JOUR
T1 - Divergent Total Synthesis of Isoflavone Natural Products and Their Potential as Therapeutic Agents for TTR Amyloidosis
AU - Thanh Luan, Nguyen Ngoc
AU - Okada, Takuya
AU - Yokoyama, Takeshi
AU - Suzuki, Mie
AU - Nabeshima, Yuko
AU - Mizuguchi, Mineyuki
AU - Toyooka, Naoki
N1 - Publisher Copyright:
© 2024 The Authors. Published by American Chemical Society and American Society of Pharmacognosy.
PY - 2024/11/22
Y1 - 2024/11/22
N2 - We have achieved the divergent total synthesis of nine isoflavone natural products 1-9 starting from commercially available 2,4,6-trihydroxyacetophenone as a starting material. The isoflavone skeleton of 1-9 was constructed by the Suzuki-Miyaura coupling reaction as the key reaction. Investigation of the potential of 1-9 as therapeutic agents for transthyretin (TTR) amyloidosis revealed that millexatin F (3) showed the best efficacy in ex vivo competitive binding experiments and thioflavin-T fluorescence studies. Therefore, millexatin F (3) is promising as a seed compound for a novel TTR amyloidosis therapeutic agent.
AB - We have achieved the divergent total synthesis of nine isoflavone natural products 1-9 starting from commercially available 2,4,6-trihydroxyacetophenone as a starting material. The isoflavone skeleton of 1-9 was constructed by the Suzuki-Miyaura coupling reaction as the key reaction. Investigation of the potential of 1-9 as therapeutic agents for transthyretin (TTR) amyloidosis revealed that millexatin F (3) showed the best efficacy in ex vivo competitive binding experiments and thioflavin-T fluorescence studies. Therefore, millexatin F (3) is promising as a seed compound for a novel TTR amyloidosis therapeutic agent.
UR - http://www.scopus.com/inward/record.url?scp=85207806426&partnerID=8YFLogxK
U2 - 10.1021/acs.jnatprod.4c00812
DO - 10.1021/acs.jnatprod.4c00812
M3 - 学術論文
C2 - 39462254
AN - SCOPUS:85207806426
SN - 0163-3864
VL - 87
SP - 2604
EP - 2614
JO - Journal of Natural Products
JF - Journal of Natural Products
IS - 11
ER -