A novel isoquinoline derivative anticancer agent and its targeted delivery to tumor cells using transferrin-conjugated liposomes

Xuewei Yang, Shuang Yang, Hongyu Chai, Zhaogang Yang, Robert J. Lee, Weiwei Liao, Lesheng Teng

Research output: Contribution to journalArticle

44 Scopus citations


We have screened 11 isoquinoline derivatives and α-methylene-?-butyrolactones using the 3-(4,5-dimethylthi-azol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cytotoxicity assay in HeLa and HEK-293T cells. Compound 2 was identified as potential anticancer agent. To further improve its therapeutic potential, this agent was incorporated into transferrin (Tf)-conjugated liposomes (LPs) for targeted delivery to tumor cells. We have demonstrated Tf-LP-Compound 2 have superior antitumor activity compared to non-targeted controls and the free drug. These data show Tf-LP-Compound 2 to be a promising agent that warrants further evaluation.

Original languageEnglish (US)
Article numbere0136649.
JournalPloS one
Issue number8
StatePublished - Aug 26 2015
Externally publishedYes


ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Agricultural and Biological Sciences(all)

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