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引用次数: 0
摘要
二茂铁的药物化学在发现二茂铁昔芬和二茂铁喹的生物活性后获得了发展势头。这些二茂铁药物是通过用二茂铁单元分别取代有机药物他莫昔芬和氯喹的芳香分子而设计出来的。这些二茂铁药物具有良好的生物活性,为探索几种二茂铁共轭物的药物应用铺平了道路。在这些共轭物中,二茂铁在增强或赋予分子抗癌活性方面发挥了重要作用。二茂铁共轭物通过产生活性氧从而破坏 DNA 来诱导细胞毒性。在药物化学中,五元氮杂环(唑类)因其刚性环结构和与生物大分子的氢键能力而发挥着重要作用。一些含有唑基的强效候选药物已被用作化疗药物。考虑到二茂铁基团和唑基团的重要性,人们合成了几种二茂铁基唑共轭物,并对其生物活性进行了筛选。因此,鉴于二茂铁基唑共轭物在开发强效药物方面的广阔前景,我们在此详细介绍了含唑基(如咪唑、三唑、噻唑和异噁唑)的二茂铁化合物的合成和抗癌活性。
Ferrocenyl Azoles: Versatile N-Containing Heterocycles and their Anticancer Activities
The medicinal chemistry of ferrocene has gained its momentum after the discovery of biological activities of ferrocifen and ferroquine. These ferrocenyl drugs have been designed by replacing the aromatic moiety of the organic drugs, tamoxifen and chloroquine respectively, with a ferrocenyl unit. The promising biological activities of these ferrocenyl drugs have paved a path to explore the medicinal applications of several ferrocenyl conjugates. In these conjugates, the ferrocenyl moiety has played a vital role in enhancing or imparting the anticancer activity to the molecule. The ferrocenyl conjugates induce the cytotoxicity by generating reactive oxygen species and thereby damaging the DNA. In medicinal chemistry, the five membered nitrogen heterocycles (azoles) play a significant role due to their rigid ring structure and hydrogen bonding ability with the biomolecules. Several potent drug candidates with azole groups have been in use as chemotherapeutics. Considering the importance of ferrocenyl moiety and azole groups, several ferrocenyl azole conjugates have been synthesized and screened for their biological activities. Hence, in the view of a wide scope in the development of potent drugs based on ferrocenyl azole conjugates, herein we present the details of synthesis and the anticancer activities of ferrocenyl compounds bearing azole groups such as imidazole, triazoles, thiazole and isoxazoles.
期刊介绍:
The Chemical Record (TCR) is a "highlights" journal publishing timely and critical overviews of new developments at the cutting edge of chemistry of interest to a wide audience of chemists (2013 journal impact factor: 5.577). The scope of published reviews includes all areas related to physical chemistry, analytical chemistry, inorganic chemistry, organic chemistry, polymer chemistry, materials chemistry, bioorganic chemistry, biochemistry, biotechnology and medicinal chemistry as well as interdisciplinary fields.
TCR provides carefully selected highlight papers by leading researchers that introduce the author''s own experimental and theoretical results in a framework designed to establish perspectives with earlier and contemporary work and provide a critical review of the present state of the subject. The articles are intended to present concise evaluations of current trends in chemistry research to help chemists gain useful insights into fields outside their specialization and provide experts with summaries of recent key developments.