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Synthesis and cytotoxic evaluation of new terpenylpurines

机译:新萜烯基嘌呤的合成与细胞毒性评价

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Several new terpenylpurine derivatives were prepared through alkylation of different purines with halogenated reagents derived from natural terpenoids, commercially available or isolated from cones of C. sempervirens L. and further transformed into appropriate alkylated agents. Alkylation of the purines gave mixtures of 9- and 7-alkylpurines, being the 9-alkylpurines the major regioisomers. The presence of the terpenyl residue induced cytotoxicity on simple purines and, in general, that activity improved as the substituent was larger. The 7-diterpenyl-6-chloropurine E - 21b was the most cytotoxic in the series and it can be considered an analogue of the marine natural compounds agelasines and agelasimines, which were taken as models for this work.
机译:通过不同嘌呤的烷基化制备几种新的萜烯基嘌呤衍生物,其衍生自衍生自天然三萜烯的卤代试剂,从C. Sempervirens L的锥体市售或分离。并进一步转化为适当的烷基化试剂。嘌呤的烷基化产生了9-和7-烷基脲的混合物,是主要的重组体的9-烷基呋喃。在简单的嘌呤上存在萜烯基残基的存在诱导细胞毒性,并且通常,随着取代基改善的活性较大。 7-二萜-6-氯嘌呤E-21b是该系列中最多细胞毒性,可考虑海洋天然化合物的类似物和agelasimines的类似物,这被作为这项工作的模型。

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