Synthesis and biological evaluation of novel 1-O- and 14-O-derivatives of oridonin as potential anticancer drug candidates

  • Bioorg Med Chem Lett. 2008 Aug 15;18(16):4741-4. doi: 10.1016/j.bmcl.2008.06.097.
Jinyi Xu  1 ,  Jingyi Yang ,  Qian Ran ,  Lei Wang ,  Jie Liu ,  Zhixuan Wang ,  Xiaoming Wu ,  Weiyi Hua ,  Shengtao Yuan ,  Luyong Zhang ,  Mingqin Shen ,  Yongfang Ding
Affiliations
  • 1. Department of Medicinal Chemistry, China Pharmaceutical University, Tongjia Xiang 24, Nanjing 210009, China. [email protected]
PMID: 18644718 DOI: 10.1016/j.bmcl.2008.06.097
Abstract

Novel 1-O- and 14-O-derivatives of oridonin were synthesized and biologically evaluated. All of the derivatives exhibited stronger cytotoxicity against six Cancer cell lines (BGC-7901, SW-480, HL-60, BEL-7402, A549, and B16) than oridonin in vitro, and some of them were more potent than oridonin and cyclophosphamide in vivo. Compounds Ib and IIg were the most potent with the IC(50) values of 0.84 microM for Ib in HL-60 cell and 1.00 microM for IIg in BEL-7402 cell.