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Ciprofloxacin and Norfloxacin Hybrid Compounds: Potential Anticancer Agents
Current Topics in Medicinal Chemistry ( IF 3.4 ) Pub Date : 2024-02-15 , DOI: 10.2174/0115680266288319240206052223
Sijongesonke Peter 1 , Blessing A. Aderibigbe 1
Affiliation  

Background:: The concept of utilizing drug repurposing/repositioning in the development of hybrid molecules is an important strategy in drug discovery. Fluoroquinolones, a class of antibiotics, have been reported to exhibit anticancer activities. Although anticancer drug development is achieving some positive outcomes, there is still a need to develop new and effective anticancer drugs. Some limitations associated with most of the available anticancer drugs are drug resistance and toxicity, poor bio-distribution, poor solubility, and lack of specificity, which hamper their therapeutic outcomes. Objectives:: Fluoroquinolones, a known class of antibiotics, have been explored by hybridizing them with other pharmacophores and evaluating their anticancer activity in silico and in vitro. Hence, this review provides an update on new anticancer drugs development containing fluoroquinolones moiety, Ciprofloxacin and Norfloxacin between 2020 and 2023, their structural relationship activity, and the future strategies to develop potent chemotherapeutic agents. Methods:: Fluoroquinolones were mostly hybridized via the N-4 of the piperazine ring on position C-7 with known pharmacophores characterized, followed by biological studies to evaluate their anticancer activity. Results:: The hybrid molecules displayed promising and interesting anticancer activities. Factors such as the nature of the linker, the presence of electron-withdrawing groups, nature, and position of the substituents influenced the anticancer activity of the synthesized compounds Conclusion:: The hybrids were selective towards some cancer cells. However, further in vivo studies are needed to fully understand their mode of action

中文翻译:

环丙沙星和诺氟沙星混合化合物:潜在的抗癌药物

背景:在混合分子开发中利用药物重新利用/重新定位的概念是药物发现的重要策略。据报道,氟喹诺酮类药物是一类抗生素,具有抗癌活性。尽管抗癌药物的开发正在取得一些积极成果,但仍然需要开发新的有效的抗癌药物。大多数可用抗癌药物的一些局限性是耐药性和毒性、生物分布差、溶解度差和缺乏特异性,这些限制了它们的治疗效果。目的:氟喹诺酮类药物是一类已知的抗生素,人们通过将其与其他药效基团杂交并在计算机和体外评估其抗癌活性来对其进行探索。因此,本综述提供了 2020 年至 2023 年含氟喹诺酮类、环丙沙星和诺氟沙星的新抗癌药物开发的最新情况、它们的结构关系活性以及开发强效化疗药物的未来策略。方法:: 氟喹诺酮类药物大多通过哌嗪环 C-7 位上的 N-4 与已知药效团进行杂交,然后进行生物学研究以评估其抗癌活性。结果:杂合分子显示出有前景且有趣的抗癌活性。连接体的性质、吸电子基团的存在、取代基的性质和位置等因素影响合成化合物的抗癌活性结论:杂合体对某些癌细胞具有选择性。然而,需要进一步的体内研究以充分了解其作用方式
更新日期:2024-02-15
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