Department of Studies in Chemistry, Mangalore University, Mangalagangotri 574 199, India.
Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, India.
Eur J Med Chem. 2015 Nov 2;104:25-32. doi: 10.1016/j.ejmech.2015.09.029. Epub 2015 Sep 28.
Breast cancer is probably the most prevalent cancer in women. The development of resistance to therapeutic agents and lack of targeted therapy for breast cancer cells provide motivation to identify new compounds for the treatment. With this objective in mind, a new series of 3-fluoro-4-methoxyphenyl group based 1,3,5-trisubstituted aryl-5-hydroxypyrazoline analogues 4a-l was synthesized through multi-step reaction sequence. The structures of the newly synthesized compounds were confirmed by IR, (1)H NMR, (13)C NMR, LC-MS and elemental analysis. They were screened for their in vitro anticancer and in vitro antioxidant activities. Among the tested compounds 4h, 4c and particularly 4i displayed promising cytotoxic effect on breast cancer cell lines. The compounds were also found to possess antioxidant activity when tested against DPPH free radical. Overall, this work has contributed to the development of promising leads for anticancer and antioxidant activities.
乳腺癌可能是女性最常见的癌症。乳腺癌细胞对治疗药物的耐药性的发展和缺乏靶向治疗提供了动力,促使人们寻找新的化合物来治疗。基于这一目标,通过多步反应序列合成了一系列基于 3-氟-4-甲氧基苯基基团的新型 1,3,5-三取代芳基-5-羟吡唑啉类似物 4a-l。新合成化合物的结构通过 IR、(1)H NMR、(13)C NMR、LC-MS 和元素分析得到确认。它们被筛选用于体外抗癌和体外抗氧化活性。在所测试的化合物中,4h、4c 特别是 4i 对乳腺癌细胞系表现出有希望的细胞毒性作用。当用 DPPH 自由基测试时,这些化合物也被发现具有抗氧化活性。总的来说,这项工作为开发具有抗癌和抗氧化活性的有前途的先导化合物做出了贡献。