Heterocycle-functional gramine analogues: solvent- and catalyst-free synthesis and their inhibition activities against cell proliferation

  • Eur J Med Chem. 2012 Aug:54:248-54. doi: 10.1016/j.ejmech.2012.05.003.
Shaoyong Ke  1 ,  Liqiao Shi ,  Xiufang Cao ,  Qingyu Yang ,  Ying Liang ,  Ziwen Yang
Affiliations
  • 1. National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, No. 6 Nanhu Yaoyuan, Wuhan 430064, PR China. [email protected]
PMID: 22647218 DOI: 10.1016/j.ejmech.2012.05.003
Abstract

A series of novel gramine analogues were designed and synthesized via a convenient three-component reaction, and which were evaluated for their inhibition activities against cell proliferation. Their structures were confirmed by satisfactory spectra analyses mainly including (1)H NMR, and ESI-MS analyses. The preliminary assays indicated that some of the newly synthesized compounds displayed significantly good inhibition activities against human lung Cancer (NCI-H460), hepatocellular liver carcinoma (HepG2), gastric Cancer (SGC-7901 and BGC-823) cell lines compared with the control 5-Fluorouracil (5-FU), which might be developed as novel lead scaffold for potential Anticancer agents.