对称和不对称环状磺胺类化合物抗癌活性的研究
Investigation on the Anticancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides.
作者信息
Jun Jaden Jungho, Duscharla Divya, Ummanni Ramesh, Hanson Paul R, Malhotra Sanjay V
机构信息
Department of Pharmaceutical Sciences and Computational Chemical Genomics Screening Center, National Institutes of Health (NIH) National Center of Excellence for Computational Drug Abuse Research, Drug Discovery Institute, School of Pharmacy, University of Pittsburgh, Pittsburgh, Pennsylvania 15261, United States.
Department of Chemistry, University of Kansas, 1567 Irving Hill Road, Lawrence, Kansas 66045-7582, United States.
出版信息
ACS Med Chem Lett. 2021 Jan 15;12(2):202-210. doi: 10.1021/acsmedchemlett.0c00460. eCollection 2021 Feb 11.
The sulfamide functional group has been extensively employed in organic synthesis to discover probes and drugs in various applications such as cancer, human immunodeficiency virus (HIV), virus, and diabetes. Herein, we describe the synthesis of 7-membered symmetric and unsymmetric sulfamide compounds and their biological evaluation through the National Cancer Institute (NCI) panel of 60 human tumor cell lines (NCI-60) and the mechanism of action study. The results of a study from the NCI-60 cell line exhibited that many synthesized cyclic sulfamide compounds inhibited breast cancer (MDA-MB-468). The mechanism of action study of a representative compound showed the inhibition of proliferation and apoptosis in A549 lung cancer cells.
磺酰胺官能团已广泛应用于有机合成中，以发现用于癌症、人类免疫缺陷病毒（HIV）、病毒和糖尿病等各种应用的探针和药物。在此，我们描述了七元对称和不对称磺酰胺化合物的合成及其通过美国国立癌症研究所（NCI）的60种人类肿瘤细胞系（NCI-60）进行的生物学评价以及作用机制研究。来自NCI-60细胞系的一项研究结果表明，许多合成的环状磺酰胺化合物抑制乳腺癌（MDA-MB-468）。对一种代表性化合物的作用机制研究表明其对A549肺癌细胞的增殖和凋亡具有抑制作用。
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