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首页> 外文期刊>Journal of Medicinal Chemistry >Transforming Rhinacanthin Analogues from Potent Anticancer Agents into Potent Antimalarial Agents
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Transforming Rhinacanthin Analogues from Potent Anticancer Agents into Potent Antimalarial Agents

机译：将Rhinacanthin类似物从有效的抗癌药转变为有效的抗疟药

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Twenty-six novel naphthoquinone aliphatic esters were synthesized by esterification of 1,4-naphthoquinone alcohols with various aliphatic acids. The 1,4-naphthoquinone alcohols were prepared from 1-hydroxy-2-naphthoic acid in nine steps with excellent yields. Twenty-four of the novel synthetic naphthoquinone esters showed significant antimalarial activity with IC50 values in the range of 0.03-16.63 mu M. The length of the aliphatic chain and the presence of C-2' substituents on the propyl chain affected the activity. Interestingly, compounds 31 and 37 showed very good antimalarial activity and were not toxic to normal Vero cells, and the PTI values of 31 (> 1990.38) and 37 (1825.94) are excellent. Both 31 and 37 showed potent inhibition against P.falciparum 3D7 cyt be, and no inhibition on rat cyt be,. They showed IC50 values in the nanomolar range, providing full inhibition of cyt bc(1) with one molecule inhibitor bound per cyt be, monomer at the Q(o) site.
机译：通过将1，4-萘醌醇与各种脂肪酸酯化，合成了26种新颖的萘醌脂族酯。由1-羟基-2-萘甲酸分九步制备1,4-萘醌醇，收率​​很高。 24种新颖的合成萘醌酯显示出显着的抗疟活性，IC50值在0.03-16.63μM范围内。脂族链的长度和丙基链上C-2'取代基的存在影响了活性。有趣的是，化合物31和37显示出非常好的抗疟活性，并且对正常的Vero细胞无毒，而且31（> 1990.38）和37（1825.94）的PTI值非常好。 31和37均显示出对恶性疟原虫3D7 cyt be的有效抑制，而对大鼠cyt be的抑制均没有。他们显示出IC50值在纳摩尔范围内，并通过在Q（o）位点与每个cyt be，单体结合的一种分子抑制剂完全抑制了cyt bc（1）。

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