Synthesis of 1-benzyl-3-(5-hydroxymethyl-2-furyl)selenolo[3,2-c]pyrazole derivatives as new anticancer agents

  • Eur J Med Chem. 2010 Apr;45(4):1395-402. doi: 10.1016/j.ejmech.2009.12.039.
Li-Chen Chou  1 ,  Li-Jiau Huang ,  Mei-Hua Hsu ,  Mei-Chi Fang ,  Jai-Sing Yang ,  Shi-Hong Zhuang ,  Hui-Yi Lin ,  Fang-Yu Lee ,  Che-Ming Teng ,  Sheng-Chu Kuo
Affiliations
  • 1. Graduate Institute of Pharmaceutical Chemistry, China Medical University, 91 Shueh Shih Road, North Section, Taichung 40402, Taiwan.
PMID: 20097456 DOI: 10.1016/j.ejmech.2009.12.039
Abstract

As part of our continuing search for potential Anticancer drug candidates among YC-1 analogs, 1, 3-disubstituted selenolo[3,2-c]pyrazole derivatives were synthesized and evaluated for their cytotoxicity against NCI-H226 non-small cell lung Cancer and A-498 renal Cancer cell lines. Significant cytotoxicity was observed in 3-(5-hydroxymethyl-2-furyl) derivatives (2, 33, 36 and 37). Among them, compound 2 was found to have the most potent activity. The mode of action of compound 2 seems to differ from those of the 175 Anticancer agents listed in NCI's standard database and resembles that of YC-1. Thus, we recommend that compound 2 should be developed further as new drug candidate for treatment of non-small cell lung Cancer and renal Cancer.