Health & Environmental Research Online (HERO)


Print Feedback Export to File
7203514 
Journal Article 
Synthesis and biological evaluation of marine alkaloid-oriented β-carboline analogues 
Xu, T; Shi, L; Zhang, Y; Wang, K; Yang, Z; Ke, S; , 
2019 
Yes 
European Journal of Medicinal Chemistry
ISSN: 0223-5234
EISSN: 1768-3254 
English 
30826506 
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.