鉴定新的先导熔体抑制剂作为治疗神经胶质瘤的潜在疗法。
Identification of new hit to lead magmas inhibitors as potential therapeutics for glioblastoma.
机构信息
Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, USA; Department of Medicine and Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, NY 10029, USA.
Department of Pathology and Laboratory Medicine, School of Medicine, University of California, Irvine, USA.
出版信息
Bioorg Med Chem Lett. 2023 Jul 15;91:129330. doi: 10.1016/j.bmcl.2023.129330. Epub 2023 May 16.
In continuation of our previous efforts for the development of potent small molecules against brain cancer, herein we synthesized seventeen new compounds and tested their anti-gliomapotential against established glioblastoma cell lines, namely, D54MG, U251, and LN-229 as well as patient derived cell lines (DB70 and DB93). Among them, the carboxamide derivatives, BT-851 and BT-892 were found to be the most active leads in comparison to our established hit compound BT#9.The SAR studies of our hit BT#9 compound resulted in the development of two new lead compounds by hit to lead strategy. The detailed biological studies are currently underway. The active compounds could possibly act as template for the future development of newer anti-glioma agents.
继我们之前为开发针对脑癌的有效小分子药物所做的努力，我们在此合成了十七种新化合物，并测试了它们对已建立的神经胶质瘤细胞系（D54MG、U251 和 LN-229）以及患者来源细胞系（DB70 和 DB93）的抗神经胶质瘤活性。其中，与我们已有的有效化合物 BT#9 相比，羧酰胺衍生物 BT-851 和 BT-892 是最具活性的先导化合物。通过从命中到先导的策略对我们的命中 BT#9 化合物进行 SAR 研究，开发了两个新的先导化合物。目前正在进行详细的生物学研究。这些活性化合物可能可以作为未来开发新型抗神经胶质瘤药物的模板。
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