关键词: Anticancer activity Ferrocene Imidazole Pyrazole Thiazole Triazole

Mesh : Azoles / chemistry pharmacology chemical synthesis Ferrous Compounds / chemistry pharmacology chemical synthesis Antineoplastic Agents / pharmacology chemistry chemical synthesis Humans Metallocenes / chemistry pharmacology chemical synthesis Heterocyclic Compounds / chemistry pharmacology chemical synthesis

来  源:   DOI:10.1002/tcr.202300347

Abstract:
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.
摘要:
二茂铁的药物化学在发现了铁氟芬和铁喹的生物活性后获得了发展。这些二茂铁药物是通过取代有机药物的芳香部分来设计的,他莫昔芬和氯喹,有一个二茂铁单元。这些二茂铁基药物的有希望的生物活性为探索几种二茂铁基结合物的医学应用铺平了道路。在这些共轭中,二茂铁基部分在增强或赋予分子抗癌活性中起着至关重要的作用。二茂铁基缀合物通过产生活性氧并由此破坏DNA来诱导细胞毒性。在药物化学中,五元氮杂环(唑类)由于其刚性的环结构和与生物分子的氢键键合能力而发挥重要作用。几种具有唑类基团的有效候选药物已被用作化学治疗剂。考虑到二茂铁基部分和唑基的重要性,已经合成了几种二茂铁基唑共轭物,并筛选了它们的生物活性。因此,鉴于开发基于二茂铁基唑共轭物的有效药物的范围很广,本文介绍了带有唑基的二茂铁基化合物如咪唑的合成和抗癌活性的细节,三唑类,噻唑和异恶唑。
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