2. Academic Validation
  3. Synthesis and anticancer activity of novel quinoline-docetaxel analogues

Synthesis and anticancer activity of novel quinoline-docetaxel analogues

  • Bioorg Med Chem Lett. 2014 Jul 1;24(13):2867-70. doi: 10.1016/j.bmcl.2014.04.091.
Ming Chen 1,  Hui Chen 1,  Jiangwei Ma 1,  Xueying Liu 2,  Shengyong Zhang 3
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Fourth Military Medical University, 169 Changle Road, Xian 710032, People's Republic of China.
  • 2 Department of Medicinal Chemistry, School of Pharmacy, Fourth Military Medical University, 169 Changle Road, Xian 710032, People's Republic of China. Electronic address: wqwlxy@fmmu.edu.cn.
  • 3 Department of Medicinal Chemistry, School of Pharmacy, Fourth Military Medical University, 169 Changle Road, Xian 710032, People's Republic of China. Electronic address: syzhang@fmmu.edu.cn.
PMID: 24835987 DOI: 10.1016/j.bmcl.2014.04.091
Abstract

A series of novel quinoline-docetaxel analogues (6a-6g, 13a-13g) were designed and synthesized by introducing bioactive quinoline scaffold to C2'-OH of docetaxel. The Anticancer activities of these novel analogues were investigated against different human Cancer cell lines including Hela, A549, A2780, MCF-7 and two resistant strains A2780-MDR and MCF-7-MDR. The data showed these analogues possessed similar to better cytotoxicity than docetaxel. Compound 6c was found to be the most potent one, and its IC50 value against MCF-7-MDR was 8.8 nM (IC50 of docetaxel was 180 nM). The work indicated that the introduction of quinolyl group in docetaxel could enhance cytotoxicity and reduce drug-resistance.

Keywords

Anticancer; Cytotoxicity; Docetaxel; Drug-resistance; Quinoline.

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