Kasaboina Suresh, Ramineni Venkatesh, Banu Saleha, Bandi Yadagiri, Nagarapu Lingaiah, Dumala Naresh, Grover Paramjit
Organic Chemistry Division-II (C P C Division), CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, Telangana, India.
Organic Chemistry Division-II (C P C Division), CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, Telangana, India.
Bioorg Med Chem Lett. 2018 Feb 15;28(4):664-667. doi: 10.1016/j.bmcl.2018.01.023. Epub 2018 Feb 4.
A novel series of substituted pyrazolo-quinoline derivatives 7pa-7qg were synthesized efficiently by using molecular iodine in DMSO and further characterized based on H NMR, C NMR, IR and HRMS spectral studies. All the synthesized derivatives were screened for their in vitro cytotoxic activity against a panel of five different cancer cell lines such as A549, HeLa, SKNSH, HepG2 and MCF7. The compounds 7pc, 7pd, and 7pj exhibited considerable to promising anti-proliferative activity with IC values of 3.76, 3.87 and 3.83 µM against SKNSH cancer cell line. It was revealed that the compounds 7pa and 7pg have shown very close IC values of 2.43 and 6.01 µM, against A549 and MCF7 cancer cell lines respectively, which compared to positive control of Doxorubicin. This is the first report on the synthesis and in vitro anti-proliferative evaluation of pyrazolo-quinoline derivatives.
通过在二甲基亚砜（DMSO）中使用分子碘高效合成了一系列新型的取代吡唑并喹啉衍生物7pa - 7qg，并基于氢核磁共振（¹H NMR）、碳核磁共振（¹³C NMR）、红外光谱（IR）和高分辨质谱（HRMS）光谱研究对其进行了进一步表征。对所有合成的衍生物针对一组五种不同的癌细胞系（如A549、HeLa、SKNSH、HepG2和MCF7）进行了体外细胞毒性活性筛选。化合物7pc、7pd和7pj对SKNSH癌细胞系表现出相当可观至有前景的抗增殖活性，IC值分别为3.76、3.87和3.83 μM。结果表明，化合物7pa和7pg分别对A549和MCF7癌细胞系显示出非常接近的IC值，即2.43和6.01 μM，与阳性对照阿霉素相比。这是关于吡唑并喹啉衍生物的合成及体外抗增殖评估的首次报道。
