title: Total Synthesis and Biological Evaluation of Apratoxin E and Its C30 Epimer: Configurational Reassignment of the Natural Product.
abstract: Apratoxin E provided the inspiration for the design of apratoxin A/E hybrids under preclinical development. Through total synthesis using two different strategies, it was determined that the originally proposed configuration of the thiazoline at C30 is opposite from that in apratoxin A, in contrast to previous assumptions on biosynthetic grounds. The epimer and true natural apratoxin E were synthesized, and the biological activities were evaluated.
authors.affiliation: School of Pharmacy, Fudan University , Shanghai, China.
authors.forename: Ping
authors.initials: P
authors.lastname: Wu
authors.affiliation: Department of Medicinal Chemistry, University of Florida , Gainesville, Florida 32610, United States.|Center for Natural Products, Drug Discovery and Development (CNPD3), University of Florida , Gainesville, Florida 32610, United States.
authors.forename: Weijing
authors.initials: W
authors.lastname: Cai
authors.affiliation: Department of Medicinal Chemistry, University of Florida , Gainesville, Florida 32610, United States.|Center for Natural Products, Drug Discovery and Development (CNPD3), University of Florida , Gainesville, Florida 32610, United States.
authors.forename: Qi-Yin
authors.initials: QY
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Fudan University , Shanghai, China.
authors.forename: Senhan
authors.initials: S
authors.lastname: Xu
authors.affiliation: School of Pharmacy, Fudan University , Shanghai, China.
authors.forename: Ruwen
authors.initials: R
authors.lastname: Yin
authors.affiliation: School of Pharmacy, Fudan University , Shanghai, China.
authors.forename: Yingxia
authors.initials: Y
authors.lastname: Li
authors.affiliation: School of Pharmacy, Fudan University , Shanghai, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.affiliation: Department of Medicinal Chemistry, University of Florida , Gainesville, Florida 32610, United States.|Center for Natural Products, Drug Discovery and Development (CNPD3), University of Florida , Gainesville, Florida 32610, United States.
authors.forename: Hendrik
authors.initials: H
authors.lastname: Luesch