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天然和合成查耳酮的抗癌活性。

Anticancer Activity of Natural and Synthetic Chalcones.

机构信息

Department of Chemistry, Faculty of Pharmacy, Iuliu Hatieganu University, 400012 Cluj-Napoca, Romania.

Department of Surgery, Country Emergency Hospital Braila, 810249 Braila, Romania.

出版信息

Int J Mol Sci. 2021 Oct 20;22(21):11306. doi: 10.3390/ijms222111306.

Abstract

Cancer is a condition caused by many mechanisms (genetic, immune, oxidation, and inflammatory). Anticancer therapy aims to destroy or stop the growth of cancer cells. Resistance to treatment is theleading cause of the inefficiency of current standard therapies. Targeted therapies are the most effective due to the low number of side effects and low resistance. Among the small molecule natural compounds, flavonoids are of particular interest for theidentification of new anticancer agents. Chalcones are precursors to all flavonoids and have many biological activities. The anticancer activity of chalcones is due to the ability of these compounds to act on many targets. Natural chalcones, such as licochalcones, xanthohumol (XN), panduretin (PA), and loncocarpine, have been extensively studied and modulated. Modification of the basic structure of chalcones in order to obtain compounds with superior cytotoxic properties has been performed by modulating the aromatic residues, replacing aromatic residues with heterocycles, and obtaining hybrid molecules. A huge number of chalcone derivatives with residues such as diaryl ether, sulfonamide, and amine have been obtained, their presence being favorable for anticancer activity. Modification of the amino group in the structure of aminochalconesis always favorable for antitumor activity. This is why hybrid molecules of chalcones with different nitrogen hetercycles in the molecule have been obtained. From these, azoles (imidazole, oxazoles, tetrazoles, thiazoles, 1,2,3-triazoles, and 1,2,4-triazoles) are of particular importance for the identification of new anticancer agents.

摘要

癌症是由多种机制(遗传、免疫、氧化和炎症)引起的一种疾病。抗癌疗法旨在破坏或阻止癌细胞的生长。治疗耐药性是当前标准疗法效率低下的主要原因。靶向治疗由于副作用少、耐药性低而最为有效。在小分子天然化合物中,类黄酮特别受到关注,因为它们可能成为新的抗癌药物。查耳酮是所有类黄酮的前体,具有许多生物活性。查耳酮的抗癌活性归因于这些化合物能够作用于许多靶点。天然查耳酮,如甘草查耳酮、黄腐醇(XN)、 panduretin(PA)和 loncocarpine,已经得到了广泛的研究和调节。为了获得具有更高细胞毒性的化合物,通过调节芳基残基、用杂环取代芳基残基以及获得杂合分子,对查耳酮的基本结构进行了修饰。已经获得了大量带有二芳基醚、磺酰胺和胺等残基的查尔酮衍生物,它们的存在有利于抗癌活性。在结构中修饰氨基查耳酮的氨基总是有利于抗肿瘤活性。这就是为什么在分子中含有不同氮杂环的查尔酮杂合分子被获得的原因。其中,唑(咪唑、噁唑、四唑、噻唑、1,2,3-三唑和 1,2,4-三唑)对于鉴定新的抗癌药物尤为重要。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3510/8582663/458e4f615daf/ijms-22-11306-g001.jpg

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