Streamlined
Total Synthesis of Trioxacarcins
and Its Application to the Design, Synthesis, and Biological Evaluation
of Analogues Thereof. Discovery of Simpler Designed and Potent Trioxacarcin
Analogues
Posted on 2017-10-19 - 20:45
A streamlined total synthesis of
the naturally occurring antitumor
agents trioxacarcins is described, along with its application
to the construction of a series of designed analogues of these complex
natural products. Biological evaluation of the synthesized compounds
revealed a number of highly potent, and yet structurally simpler,
compounds that are effective against certain cancer cell lines, including
a drug-resistant line. A novel one-step synthesis of anthraquinones
and chloro anthraquinones from simple ketone precursors and
phenylselenyl chloride is also described. The reported work,
featuring novel chemistry and cascade reactions, has potential applications
in cancer therapy, including targeted approaches as in antibody–drug
conjugates.
CITE THIS COLLECTION
DataCite
3 Biotech
3D Printing in Medicine
3D Research
3D-Printed Materials and Systems
4OR
AAPG Bulletin
AAPS Open
AAPS PharmSciTech
Abhandlungen aus dem Mathematischen Seminar der Universität Hamburg
ABI Technik (German)
Academic Medicine
Academic Pediatrics
Academic Psychiatry
Academic Questions
Academy of Management Discoveries
Academy of Management Journal
Academy of Management Learning and Education
Academy of Management Perspectives
Academy of Management Proceedings
Academy of Management Review
Nicolaou, K. C.; Chen, Pengxi; Zhu, Shugao; Cai, Quan; Erande, Rohan D.; Li, Ruofan; et al. (2017). Streamlined
Total Synthesis of Trioxacarcins
and Its Application to the Design, Synthesis, and Biological Evaluation
of Analogues Thereof. Discovery of Simpler Designed and Potent Trioxacarcin
Analogues. ACS Publications. Collection. https://doi.org/10.1021/jacs.7b08820
or
Select your citation style and then place your mouse over the citation text to select it.
SHARE
Usage metrics
AUTHORS (12)
KN
K. C. Nicolaou
PC
Pengxi Chen
SZ
Shugao Zhu
QC
Quan Cai
RE
Rohan D. Erande
RL
Ruofan Li
HS
Hongbao Sun
KP
Kiran Kumar Pulukuri
SR
Stephan Rigol
MA
Monette Aujay
JS
Joseph Sandoval
JG
Julia Gavrilyuk
KEYWORDS
cancer cell linesseriesconjugateagentApplicationPotenttrioxaanaloguenovel chemistrySimplerdrug-resistant lineanthracascade reactionsBiological Evaluationapplicationapproachketone precursorsTrioxasynthesisphenylantitumorBiological evaluationconstructionStreamlinedcompoundAnalogues ThereofchlorideSynthesiantibodycancer therapychloro