Synthesis and Cytotoxic Evaluation of Sanjoseolide and Representative Analogues.

ABSTRACT: 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 IC₅₀ 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-act

SUBMITTER: Tian T 

PROVIDER: S-EPMC7774250 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature