Panduranga Padyala, Makam Parameshwar, Kumar Katari Naresh, Gundla Rambabu, Babu Jonnalagadda Sreekantha, Kumar Tripuramallu Bharat
Department of Chemistry, VFSTR (Deemed to be University), Vadlamudi, Guntur, Andhra Pradesh, 522213, India.
Division of Research and Innovation, Department of Chemistry, Uttaranchal University,Arcadia Grant, P.O. Chandanwari, Premnagar, Dehradun Uttarakhand, 248007, India.
ChemistryOpen. 2025 Mar;14(3):e202400334. doi: 10.1002/open.202400334. Epub 2024 Nov 26.
Molecular hybrids of diversely functionalized quinoline and sulfonamide have been designed. Multistep synthetic strategies have been used for the synthesis. The anti-cancer properties have been evaluated against various cancer cell lines including HCT116, A549, U2OS, CCRF-CEM, Jurkat, MOLT-4, RAMOS, and K562. Non-cancer cell lines MRC-5 and BJ were also included for comparison. When examining the effects on A549, HCT116, and U2OS cells, all tested compounds exhibited limited potency with IC values exceeding 50 μM, indicating weak activity against these cell lines. Against the ITK high cells Viz. are Jurkat, CCRF-CEM and MOLT-4, 9 e, 9 p and 9 j found to the maximum potent compounds with IC values of 7.43±7.40 μM, 13.19±1.25 μM and 5.57±7.56 μM respectively. Similarly, in the BTK high cells screenings, 9 n and 9 e molecules with an IC value of 2.76±0.79 μM and 5.47±1.71 μM against RAMOS and K562 respectively are highly potent. Interestingly, all the molecules have exhibited IC value >50 μM against the non-cancer cells (MRC-5 and BJ), which indicates the promising non-cytotoxic nature of the molecules.
已设计出具有不同功能化喹啉和磺酰胺的分子杂化物。采用多步合成策略进行合成。已针对包括HCT116、A549、U2OS、CCRF - CEM、Jurkat、MOLT - 4、RAMOS和K562在内的多种癌细胞系评估了其抗癌特性。还纳入了非癌细胞系MRC - 5和BJ进行比较。在检测对A549、HCT116和U2OS细胞的影响时,所有测试化合物的效力均有限,IC值超过50 μM,表明对这些细胞系的活性较弱。对于ITK高表达细胞,即Jurkat、CCRF - CEM和MOLT - 4,发现9e、9p和9j是效力最强的化合物,IC值分别为7.43±7.40 μM、13.19±1.25 μM和5.57±7.56 μM。同样,在BTK高表达细胞筛选中,9n和9e分子对RAMOS和K562的IC值分别为2.76±0.79 μM和5.47±1.71 μM,具有高效力。有趣的是,所有分子对非癌细胞(MRC - 5和BJ)的IC值均>50 μM,这表明这些分子具有良好的非细胞毒性特性。