Synthesis and biological evaluation of marine alkaloid-oriented β-carboline analogues

Eur J Med Chem. 2019 Apr 15:168:293-300. doi: 10.1016/j.ejmech.2019.02.060.

Tingting Xu ¹, Liqiao Shi ², Yani Zhang ², Kaimei Wang ², Ziwen Yang ³, Shaoyong Ke ⁴

Affiliations

1 College of Life Sciences, Wuhan University, Wuhan 430072, PR China.
2 National Biopesticide Engineering Research Centre, Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, Wuhan 430064, PR China.
3 National Biopesticide Engineering Research Centre, Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, Wuhan 430064, PR China; College of Life Sciences, Wuhan University, Wuhan 430072, PR China. Electronic address: ziwen.yang@nberc.com.
4 National Biopesticide Engineering Research Centre, Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, Wuhan 430064, PR China. Electronic address: keshaoyong@163.com.

PMID: 30826506 DOI: 10.1016/j.ejmech.2019.02.060

Abstract

Pityriacitrin is a marine alkaloid with typical β-carboline scaffold, and which has been proven to exhibit diverse biological functions. During the course of our research for highly active compounds from Natural Products, the pityriacitrin have also been isolated and identified from a Chinese Burkholderia sp. NBF227. So, in order to explore the potential Functional Molecules, a series of β-carboline analogues derived from pityriacitrin were designed and synthesized, and their in vitro cytotoxic activities against SGC-7901, A875, HepG2, and MARC145 cell lines were evaluated. The results demonstrated that some of these β-carboline derivatives exhibited moderate to good cytotoxic activities, especially, compound 9o with a special sulfonyl group presented the highest inhibitory activities against all tested cell lines with the IC₅₀ values of 6.82 ± 0.98, 8.43 ± 1.93, 7.69 ± 2.17, 7.19 ± 1.43 μM, respectively, which might be used as lead compound for discovery of novel cytotoxic agents.

Keywords

Analogues; Biological evaluation; Marine alkaloid; Pityriacitrin; SARs; Synthesis.

Name
Email *

	Sorry, but the email address you supplied was invalid.