关键词: COX-2 cancer cell lines drug design hybrid molecules molecular docking

来  源:   DOI:10.3390/ph15121471

Abstract:
Cancer is a serious threat to human beings and is the second-largest cause of death all over the globe. Chemotherapy is one of the most common treatments for cancer; however, drug resistance and severe adverse effects are major problems associated with anticancer therapy. New compounds with multi-target inhibitory properties are targeted to surmount these challenges. Cyclooxygenase-2 (COX-2) is overexpressed in cancers of the pancreas, breast, colorectal, stomach, and lung carcinoma. Therefore, COX-2 is considered a significant target for the synthesis of new anticancer agents. This review discusses the biological activity of recently prepared dual anticancer and COX-2 inhibitory agents. The most important intermolecular interactions with the COX-2 enzyme have also been presented. Analysis of these agents in the active area of the COX-2 enzyme could guide the introduction of new lead compounds with extreme selectivity and minor side effects.
摘要:
癌症是对人类的严重威胁,是全球第二大死亡原因。化疗是癌症最常见的治疗方法之一;然而,耐药性和严重的不良反应是与抗癌治疗相关的主要问题。具有多靶标抑制特性的新化合物旨在克服这些挑战。环氧合酶-2(COX-2)在胰腺癌中过度表达,乳房,结直肠,胃,和肺癌。因此,COX-2被认为是合成新抗癌剂的重要靶标。本文综述了最近制备的双重抗癌和COX-2抑制剂的生物学活性。还提出了与COX-2酶的最重要的分子间相互作用。在COX-2酶的活性区域中分析这些试剂可以指导引入具有极端选择性和较小副作用的新先导化合物。
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