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Synthesis and Cytotoxic Evaluation of Sanjoseolide and Representative Analogues by Tian, Tian ;Zhu, Zhiming ;Ding, Yalong ;Li, Guoli ;Li, Nan ;Shen, Tong is a Engineering article available to read on EtoBox.
What is Synthesis and Cytotoxic Evaluation of Sanjoseolide and Representative Analogues about?
The first total synthesis of sanjoseolide (1), which was originally obtained from Dalea frutescens A, was achieved via an efficient route with a longest linear sequence of six steps from the commercially available 2,4-dihydroxyacetophenone in 8.6% overall yield. Meanwhile, a series of sanjoseolide representative analogues were synthesized and assessed for their antiproliferative potency against cancer cells of different origins. Compound 8e inhibited the survival of all tested cancer cell lines in a dose-dependent manner, the IC 50 values of the treatment were about 12.8 μM for human cholangiocarcinoma cell lines RBE and 12.7 μM for human cholangiocarcinoma cell lines HCCC-9810, which was more active than sanjoseolide (1). Analysis of the structure-activity relationships revealed that the presence of a trifluoromethyl group may be beneficial in terms of both RBE and HCCC-9810 inhibition.
Who reads Synthesis and Cytotoxic Evaluation of Sanjoseolide and Representative Analogues?
It is typically read by researchers, students, and practitioners in Engineering.
- Author
- Tian, Tian ;Zhu, Zhiming ;Ding, Yalong ;Li, Guoli ;Li, Nan ;Shen, Tong
- Publisher
- American Chemical Society (ACS)
- Published
- 2020
- Language
- EN
- Field
- Engineering (Physical Sciences)
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