Laxmi S Vijaya, Anil P, Rajitha G, Rao Asha Jyothi, Crooks Peter A, Rajitha B
Department of Chemistry, K L University, Guntur, 522502 India.
Department of Chemistry, National Institute of Technology, Warangal, 506004 India.
J Chem Biol. 2016 Jul 15;9(4):97-106. doi: 10.1007/s12154-016-0154-8. eCollection 2016 Oct.
In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives () have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer activity of compound (NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound was active against all the cell lines, it has shown potential activity against leukemia SR (GI: 2.04 μM), non-small cell lung cancer NCI-H522 (GI: 1.36 μM), colon cancer COLO 205 (GI: 1.64 μM), CNS cancer SF-539 (GI: 1.87 μM), melanoma SK-MEL-2 (GI: 1.64 μM), ovarian cancer OVCAR-3 (GI: 1.87 μM), renal cancer RXF 393 (GI: 1.15 μM), prostate cancer PC-3 (GI: 1.90 μM), and breast cancer MDA-MB-468(GI: 1.11 μM). DNA cleavage studies revealed that at 50 μg/mL concentration, partial DNA digestion was observed and when the concentration is increasing to threefold (150 μg/mL), complete linear DNA digestion and partial supercoiled DNA digestion was observed. Further antimicrobial studies indicate that all the synthesized compounds except compound possess prominent activity against all the screened microbial species. This study throws a ray of light in the field of anticancer drugs.
在寻找高效抗癌药物的过程中，本文成功合成并表征了新型5-(4-烷基亚苄基)噻唑烷-2,4-二酮衍生物（），并通过DNA裂解研究对其抗癌和抗菌活性进行了评估。对化合物（NSC: 768619/1）的抗癌活性进行了针对60种人类肿瘤细胞系的全组体外研究。五级剂量活性结果显示，该化合物对所有细胞系均有活性，对白血病SR（生长抑制浓度GI：2.04 μM）、非小细胞肺癌NCI-H522（GI：1.36 μM）、结肠癌COLO 205（GI：1.64 μM）、中枢神经系统癌SF-539（GI：1.87 μM）、黑色素瘤SK-MEL-2（GI：1.64 μM）、卵巢癌OVCAR-3（GI：1.87 μM）、肾癌RXF 393（GI：1.15 μM）、前列腺癌PC-3（GI：1.90 μM）和乳腺癌MDA-MB-468（GI：1.11 μM）均显示出潜在活性。DNA裂解研究表明，在50 μg/mL浓度下，观察到部分DNA消化，当浓度增加到三倍（150 μg/mL）时，观察到完全线性DNA消化和部分超螺旋DNA消化。进一步的抗菌研究表明，除化合物外，所有合成化合物对所有筛选的微生物物种均具有显著活性。这项研究为抗癌药物领域带来了一线曙光。
