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Synthesis and antiproliferative activities of novel quartenary ammonium spinosyn derivatives
Da-You Ma1, Long-Long Wang1, Qin Lai1
1School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
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.
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