摘要
查耳酮是一类有趣的化合物,具有多种有益于人类健康的生物活性。多年来,这些化学型继续引起越来越多的研究关注。因此,通过抑制各种分子靶标,包括 ABCG2、BCRP、P-糖蛋白、5α-还原酶、雄激素受体 (AR)、组蛋白脱乙酰酶 (HDAC)、Sirtuin 1、蛋白酶体、血管内皮生长因子 (VEGF)、组织蛋白酶-K、微管蛋白、CDC25B 磷酸酶、拓扑异构酶、EBV、NF-κB、mTOR、BRAF 和 Wnt/β-连环蛋白。此外,对内在作用机制的研究,特别是与特定细胞通路和分子靶标参与模式相关的研究,可能有助于药物化学家开发更有效、选择性和成本效益更高的查尔酮类抗癌药物。因此,本综述阐明了结构变异对 2018-2019 年报道的查耳酮杂交体抗癌效力的影响,以及它们的作用机制、分子靶点和对有效癌症化疗的潜在影响。
关键词: 查尔酮,抗癌杂合体,癌症,分子靶点,作用机制,构效关系。
Current Medicinal Chemistry
Title:Recent Advances in Chalcone-Based Anticancer Heterocycles: A Structural and Molecular Target Perspective
Volume: 28 Issue: 33
关键词: 查尔酮,抗癌杂合体,癌症,分子靶点,作用机制,构效关系。
摘要: Chalcones are an interesting class of compounds endowed with a plethora of biological activities beneficial to human health. These chemotypes have continued to attract increased research attention over the years; hence, numerous natural and synthetic chalcones have found with interesting anticancer activities through the inhibition of various molecular targets including ABCG2, BCRP, P-glycoprotein, 5α-reductase, Androgen Receptor (AR), Histone Deacetylases (HDAC), Sirtuin 1, proteasome, Vascular Endothelial Growth Factor (VEGF), Cathepsin-K, tubulin, CDC25B phosphatase, Topoisomerase, EBV, NF-κB, mTOR, BRAF, and Wnt/β-catenin. Moreover, the study of intrinsic mechanisms of action, particularly relating to specific cellular pathways and modes of engagement with molecular targets, may help medicinal chemists to develop more effective, selective, and cost-effective chalcone-based anticancer drugs. This review, therefore, sheds light on the effect of structural variations on the anticancer potency of chalcone hybrids reported in 2018-2019 alongside their mechanism of action, molecular targets, and potential impacts on effective cancer chemotherapy.
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Cite this article as:
Recent Advances in Chalcone-Based Anticancer Heterocycles: A Structural and Molecular Target Perspective, Current Medicinal Chemistry 2021; 28 (33) . https://dx.doi.org/10.2174/0929867328666210322102836
DOI https://dx.doi.org/10.2174/0929867328666210322102836 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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