Peter Sijongesonke, Aderibigbe Blessing A
Department of Chemistry, Faculty of Science and Agriculture, University of Fort Hare, Private Bag X1314, Alice, Eastern Cape, South Africa.
Curr Top Med Chem. 2024;24(7):644-665. doi: 10.2174/0115680266288319240206052223.
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, thereby reducing their therapeutic outcomes.
Fluoroquinolones, a known class of antibiotics, have been explored by hybridizing them with other pharmacophores and evaluating their anticancer activity and . Hence, this review provides an update on new anticancer drugs containing fluoroquinolones moiety, Ciprofloxacin and Norfloxacin between 2020 and 2023, their structural relationship activity, and the future strategies to develop potent chemotherapeutic agents.
Fluoroquinolones were mostly hybridized the N-4 of the piperazine ring on position C-7 with known pharmacophores characterized, followed by biological studies to evaluate their anticancer activity.
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.
The hybrids were selective towards some cancer cells. However, further studies are needed to fully understand their mode of action.
在杂化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中的一项重要策略。氟喹诺酮类作为一类抗生素，已被报道具有抗癌活性。尽管抗癌药物开发取得了一些积极成果，但仍需要开发新的有效抗癌药物。大多数现有抗癌药物存在一些局限性，如耐药性和毒性、生物分布差、溶解度低以及缺乏特异性，从而降低了它们的治疗效果。
氟喹诺酮类作为一类已知的抗生素，已通过与其他药效基团杂交并评估其抗癌活性进行了探索。因此，本综述提供了2020年至2023年间含氟喹诺酮部分、环丙沙星和诺氟沙星的新型抗癌药物的最新信息，它们的结构关系活性，以及开发强效化疗药物的未来策略。
氟喹诺酮类大多在C-7位哌嗪环的N-4处与已知的药效基团杂交并进行表征，随后进行生物学研究以评估其抗癌活性。
杂化分子显示出有前景且有趣的抗癌活性。连接基团的性质、吸电子基团的存在、取代基的性质和位置等因素影响了合成化合物的抗癌活性。
这些杂化物对某些癌细胞具有选择性。然而，需要进一步研究以充分了解它们的作用方式。
