The efficient synthesis and biological evaluation of justicidin B

Nat Prod Res. 2021 Jul 6:1-7. doi: 10.1080/14786419.2021.1948843. Online ahead of print.ABSTRACTA facile new synthetic method for the preparation of a Type-A 1-arylnaphthalene lactone skeleton was developed and used to synthesise justicidin B and several derivatives. Key synthesis steps included Hauser-Kraus annulation of a phthalide intermediate and Suzuki-Miyaura cross coupling between a triflated naphthalene lactone intermediate and various potassium organotrifluoroborates. With two exceptions, the derivatives showed significant inhibitory effect on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in mouse macrophages. Moreover, several compounds, including justicidin B, had marked cytotoxicity towards six human tumour cell lines.PMID:34227447 | DOI:10.1080/14786419.2021.1948843

Source: Natural Product Research - July 6, 2021 Category: Biochemistry Authors: Taejung Kim Young-Joo Kim Kyu-Hyuk Jeong Young-Tae Park Hyukjoon Kwon Pilju Choi Ha-Neul Ju Cheol Hee Yoon Ji-Yool Kim Jungyeob Ham Source Type: research