AUTHOR=Wan Minghui , Zhang Lei , Chen Yiming , Li Qiang , Fan Wenli , Xue Qingxia , Yan Fang , Song Weiguo 

TITLE=Synthesis and Anticancer Activity Evaluation of Novel Phenanthridine Derivatives

JOURNAL=Frontiers in Oncology

VOLUME=Volume 9 - 2019

YEAR=2019

URL=https://www.frontiersin.org/journals/oncology/articles/10.3389/fonc.2019.00274

DOI=10.3389/fonc.2019.00274

ISSN=2234-943X

ABSTRACT=In structural modification of sanguinarine, fourteen phenanthridine derivatives were designed and synthesized. The cytotoxic activities of synthesized compounds were evaluated against five human cancer cell lines (MCF-7, PC3, Hela, A549 and HepG2 cell lines) in vitro by MTT assay. Among all the compound tested, molecule 8a showed significant cytotoxic activity against MCF-7 cells with IC50 value of 0.28 µM. The enzymatic assay exhibited that compound 8a could inhibit the activity of DNA topoisomerase Ⅰ/Ⅱ. Further MCF-7 cell based mechanism studies revealed that compound 8a could lead cell cycle arrest in S phase, and induce cell apoptosis via downregulating the expression of Bcl-2 and upregulating the expression of Bax.