Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmaceutical Chemistry, Thessaloniki 54124, Greece.
Expert Opin Ther Pat. 2011 Oct;21(10):1575-96. doi: 10.1517/13543776.2011.596529. Epub 2011 Jun 28.
Chalcones are a group of plant-derived polyphenolic compounds belonging to the flavonoids family that possess a wide variety of cytoprotective and modulatory functions, which may have therapeutic potential for multiple diseases. Their physicochemical properties seem to define the extent of their biological activity.
A comprehensive synopsis of recent patent literature (2005 - 2011) describing chalcones and their derivatives on selected activities (e.g., anti-inflammatory, antimitotic, cytotoxic, antioxidant, anti-infection) is provided in this paper. Synthesis, combinatorial techniques, biological evaluation in vitro/in vivo, and new biological assays are discussed. In addition to selected biological data, a wide range of pharmaceutical applications and pharmaceutical compositions are also summarized.
Several natural and synthetic chalcones and their derivatives appear as promising anti-inflammatory and anticancer activities. Their clinical evaluation will be critical to assess their therapeutic utility. Those for which the mechanism of action is well defined can serve as lead compounds for the design of new, more promising molecules.
查耳酮是一类植物来源的多酚类化合物，属于黄酮类家族，具有广泛的细胞保护和调节功能，可能对多种疾病具有治疗潜力。它们的物理化学性质似乎决定了其生物活性的程度。
本文综合了 2005 年至 2011 年期间有关查耳酮及其衍生物在选定活性（如抗炎、抗有丝分裂、细胞毒性、抗氧化、抗感染）方面的专利文献，讨论了合成、组合技术、体外/体内生物评价以及新的生物测定。除了选定的生物学数据外，还总结了广泛的药物应用和药物组合物。
一些天然和合成的查耳酮及其衍生物表现出有希望的抗炎和抗癌活性。对它们的临床评估对于评估其治疗用途至关重要。那些作用机制明确的药物可以作为设计新的、更有前途的分子的先导化合物。
