2. Academic Validation
  3. Synthesis and antiproliferative activities of novel quartenary ammonium spinosyn derivatives

Synthesis and antiproliferative activities of novel quartenary ammonium spinosyn derivatives

  • Bioorg Med Chem Lett. 2018 Nov 1;28(20):3346-3349. doi: 10.1016/j.bmcl.2018.09.005.
Da-You Ma 1,  Long-Long Wang 2,  Qin Lai 2,  Kun-Jian Peng 3,  Xuan Li 3,  Zeng-Xia Li 4,  Li-Jun Liu 3,  Zhi-Yong Luo 3,  Su-You Liu 5
Affiliations

Affiliations

  • 1 School of Pharmaceutical Sciences, Central South University, Changsha 410013, China. Electronic address: madayou@hotmail.com.
  • 2 School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
  • 3 School of Life Sciences, Central South University, Changsha 410013, China.
  • 4 Key Laboratory of Metabolism and Molecular Medicine, Ministry of Education and Department of Biochemistry and Molecular Biology, School of Basic Medical Sciences, Fudan University, Shanghai 200032, China.
  • 5 School of Pharmaceutical Sciences, Central South University, Changsha 410013, China. Electronic address: liusuyou@hotmail.com.
PMID: 30201293 DOI: 10.1016/j.bmcl.2018.09.005
Abstract

In order to enhance the mitochondria-targeting ability of spinosad. A series of quartenary ammonium spinosyn derivatives was designed and synthesized. Some of the derivatives displayed greatly enhanced antiproliferative ability towards tested human Cancer cell lines. The structure activity relationship study indicated that lipophilicity has a great influence on the antiproliferative effects of these derivatives. The most active compound 11d exhibited remarkably enhanced OXPHS inhibition and Apoptosis inducing ability than spinosyn A.

Keywords

Antiproliferative activity; Derivatives; Mitochondria; Respiration; Spinosad.

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