Abbas Ashraf A, Farghaly Thoraya A, Dawood Kamal M
Department of Chemistry, Faculty of Science, Cairo University Giza 12613 Egypt
Department of Chemistry, Faculty of Science, Umm Al-Qura University Makkah Saudi Arabia.
RSC Adv. 2024 Jun 19;14(28):19752-19779. doi: 10.1039/d4ra01387e. eCollection 2024 Jun 18.
Due to the importance of the fluorinated heterocycles as main components of marketed drugs where 20% of the anticancer and antibiotic drugs contain fluorine atoms, this review describes the reported five-membered heterocycles and their benzo-fused systems having directly connected fluorine atom(s). The and anticancer and antimicrobial activities of these fluorinated heterocycles are well reported. Some fluorinated heterocycles were found to be lead structures for drug design developments where their activities were almost equal to or exceeded the potency of the reference drugs. In most cases, the fluorine-containing heterocycles showed promising safety index their reduced cytotoxicity in non-cancerous cell lines. SAR study assigned that fluorinated heterocycles having various electron-donating or electron-withdrawing substituents significantly affected the anticancer and antimicrobial activities.
由于氟化杂环作为市售药物的主要成分非常重要,其中20%的抗癌和抗生素药物含有氟原子,本综述描述了已报道的具有直接连接氟原子的五元杂环及其苯并稠合体系。这些氟化杂环的抗癌和抗菌活性已有充分报道。一些氟化杂环被发现是药物设计开发的先导结构,其活性几乎等于或超过参考药物的效力。在大多数情况下,含氟杂环显示出有前景的安全指数,因为它们在非癌细胞系中的细胞毒性降低。构效关系研究表明,具有各种供电子或吸电子取代基的氟化杂环显著影响抗癌和抗菌活性。