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Contents is a Chemistry article available to read on EtoBox.
What is Contents about?
A total synthesis of 17-membered macrocyclolipopeptide dysoxylactam A (1), a potent agent reversing P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) in cancer cells, was developed from the starting material (S)-2-methylbutanal in a linear sequence of 12 steps. The compound 1 and its side chain simplified analog 15 at 10 μmol•L -1 in combination with vinorelbine against vinorelbine-resistant KBV200 tumor cells exhibited promising reversal activity with IC50 values in the low nanomolar range (IC50 = 3.5 and 8.7 nmol•L -1 ; RF = 85.0 and 34.2), respectively. This practical total synthesis method and promising reversal activity enable us to obtain a large amount of compound 1 and/or the side chain modified analog 15 in a short time for the in-depth biological tests and/or structure-activity relationship study.
Who reads Contents?
It is typically read by researchers, students, and practitioners in Chemistry.
- Publisher
- Wiley
- Published
- 2022
- Language
- EN
- Field
- Chemistry (Physical Sciences)