Anti-cancer pyrimidines in diverse scaffolds: a review of patent literature.
Anti-cancer pyrimidines in diverse scaffolds: a review of patent literature.
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DOI：
10.2174/1574892809666140917104502
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发表时间：
2014-12
影响因子：
2.8
通讯作者：
R. Kaur;Prabhkirat Kaur;Sahil Sharma;Gurpreet Singh;Samir Mehndiratta;P. Bedi;K. Nepali
中科院分区：
文献类型：
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作者：
R. Kaur;Prabhkirat Kaur;Sahil Sharma;Gurpreet Singh;Samir Mehndiratta;P. Bedi;K. Nepali
嘧啶环是DNA和RNA的结构单元，因此基于嘧啶的化学结构表现出多种药理活性。在已报道的嘧啶类药物属性中，抗癌活性是最广泛报道的。嘧啶在融合支架中的抗癌潜力也已通过大量的研究文章和专利文献得到证明。基于嘧啶的支架通过不同的机制发挥其细胞杀伤作用，这表明它们与不同的酶/靶标/受体相互作用的潜力。这篇综述文章严格关注2009年以来的专利文献。本汇编中列出了强效化合物的结构、其IC 50值、用于抗癌评价的模型/试验以及涉及的酶/受体/靶标。从2009年到2014年（从2009年至今），已经发表了大量关于嘧啶类抗癌剂的专利，即59项，这清楚地表明这种杂环是目前地球仪研究人员关注的领域。此外，在此期间公布的59项专利中，有32项是从2012年起公布的，这进一步突出了研究人员目前对基于嘧啶的抗癌剂的兴趣。这些基于嘧啶的支架显示出的有希望的活性显然使它们成为潜在的未来候选药物。本汇编对从事抗肿瘤药物设计和合成的药物化学家非常有益。
Pyrimidine ring is the building unit of DNA and RNA and thus pyrimidine based chemical architectures exhibit diverse pharmacological activities. Among the reported medicinal attributes of pyrimidines, anticancer activity is the most extensively reported. The anticancer potential of pyrimidines in fused scaffolds has also been evidenced through number of research article and patent literature. The pyrimidines based scaffolds have exerted their cell killing effects through varied mechanisms which indicate their potential to interact with diverse enzymes/ targets/receptors. This review article strictly focuses on the patent literature from 2009 onwards. The structure of the potent compounds, their IC50 values, models/assays used for the anticancer evaluation and the enzymes/ receptors/ targets involved have been presented in this compilation. Significant number of patents i.e. 59 have been published on pyrimidine based anticancer agents from 2009-2014 (from 2009 through the present date) which clearly indicate that this heterocycle is an area of focus at present for researchers all over the globe. Moreover, out of the 59 patents published during this period, 32 have been published from 2012 onwards which further highlights the present interest of the researcher towards pyrimidine based anticancer agents. The promising activity displayed by these pyrimidine based scaffolds clearly places them in forefront as potential future drug candidates. The present compilation can be extremely beneficial for the medicinal chemists working on design and synthesis of anticancer drugs.