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2,5-二酮哌嗪衍生物的设计合成及构效关系研究; Study on 2,5-diketopiperazine derivatives designed synthesized and structure-antitumor activity
Thesis Advisor刘永宏
Degree Discipline海洋化学
Keyword2 5-二酮哌嗪 结构修饰 一锅法 细胞毒活性 构效关系
Abstract2,5-二酮哌嗪类化合物(Diketopiperazines, DKPs)的基本结构是由2 个氨基酸缩合而成的环二肽(DKP), 是结构最小的环二肽,因其骨架具有稳定的六元环结构(图一),且有2 个氢键给体和2 个氢键受体,提示着二酮哌嗪类化合物在药物化学中可能是个重要的药效团,它们的研究为多肽化学方向的研究奠定了基础。2,5-二酮哌嗪类化合物首先从陆源性微生物中,此后, 人们陆续地从海洋微生物代谢产物中分离到。到目前为止,具有活性的DKPs在真菌、细菌、植物甚至动物均有对其发现的报道。 2,5-二酮哌嗪类化合物比起多肽拥有物理化学上的优势:刚性环型骨架,同时拥有氢键给体和受体结构,不容易蛋白质水解、能模拟多肽的药效团、能控制支链的立体化学构型,这些优势赋予了2,5-二酮哌嗪类化合物新颖结构,丰富的支链,及广泛的生物活性。 然而,正是由于这样的结构特征,2,5-二酮哌嗪类化合物容易由于氢键...
Other Abstract2,5-diketopiperazine(DKPs) is a privileged and promising scaffold which is the smallest cyclodipeptide obtained by condensation of two α-amino acids. The 2,5-diketopiperazines occur in numerous natural products, and this subunit is often found alone or embedded in larger, more complex architectures in a variety of natural products from fungi, bacteria, the plant kingdom, and mammals. DKPs displayed a wide range of bioactivities, such as antitumor, antifungi, antivirus and many other kinds of vitro activities such as work as PDE inhibitors, Oxytocin antagonist, Neuroprotective Agents and so on. DKPs poesses various activities possibly due to its small, conformationally constrained heterocyclic ring structure with 2 hydrogen acceptors and 2 hydrogen doners, stable to enzymes and diverse side...
Document Type学位论文
Recommended Citation
GB/T 7714
李晋昇. 2,5-二酮哌嗪衍生物的设计合成及构效关系研究, Study on 2,5-diketopiperazine derivatives designed synthesized and structure-antitumor activity[D],2015.
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