2. Academic Validation
  3. Synthesis and anticancer activity of 2,4-disubstituted furo[3,2-b]indole derivatives

Synthesis and anticancer activity of 2,4-disubstituted furo[3,2-b]indole derivatives

  • Eur J Med Chem. 2013 Aug:66:466-79. doi: 10.1016/j.ejmech.2013.06.012.
Shi-Hong Zhuang 1,  Yi-Chien Lin,  Li-Chen Chou,  Mei-Hua Hsu,  Hui-Yi Lin,  Chi-Hung Huang,  Jin-Cherng Lien,  Sheng-Chu Kuo,  Li-Jiau Huang
Affiliations

Affiliation

  • 1 Graduate Institute of Pharmaceutical Chemistry, China Medical University, No. 91 Hsueh-Shih Road, Taichung 40402, Taiwan ROC.
PMID: 23831809 DOI: 10.1016/j.ejmech.2013.06.012
Abstract

We synthesized and evaluated a series of 2,4-disubstituted furo[3,2-b]indole derivatives for Anticancer activity and established the structure-activity relationships (SARs) of these compounds. Among all tested compounds, we found (5-((2-(hydroxymethyl)-4H-furo[3,2-b]indol-4-yl)methyl)furan-2-yl)methanol (10a) to be the most promising agent. In screening against NCI-60 human tumor cell lines, 10a exhibited highly selective Anticancer activity and significant inhibitory activity against A498 renal Cancer cells. Our COMPARE analysis results suggest that the 10a fingerprint is similar to that of NSC-754549, which is an isostere of YC-1. We further confirmed the significant antitumor activity of compound 10a with tests in the A498 xenograft nude mice model. Therefore, compound 10a should be further developed as a new drug candidate for treating renal Cancer.

Keywords

A498 renal cancer cells; Anticancer activity; Furo[3,2-b]indole derivatives; Structure–activity relationships (SARs).

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