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

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

Affiliation

  • 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.

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