nifurtimox

Nifurtimox (BAY-A-2502) 是一种用于锥虫病的抗虫剂，可影响乳酸脱氢酶活性。它有潜力研究神经母细胞瘤细胞。

12-methyl Myristic acid methyl ester is a methylated fatty acid methyl ester that has been found in vermicomposts of cattle manure, carica papaya leaves, and cuticular wax of K. africana. It is a volatile compound in lipid-lowering granulated tea. Levels of 12-methyl myristic acid methyl ester are decreased in T. cruzi treated with nifurtimox compared to non-treated controls.

Antitrypanosomal agent 6 (compound 18a) 是一种有效的抗锥体虫剂，表现出良好的 ADME 特性。Antitrypanosomal agent 6 抗布氏锥虫 (T. brucei) 的活性比 Nifurtimox 高两倍以上，IC50为 0.47 μM。Antitrypanosomal agent 6 与 DNA 具有很强的相互作用，可以选择性的结合富含 AT 碱基的 DNA。

Antitrypanosomal agent 7 (compound 18c) 是一种有效的抗锥体虫剂，显示出良好的 ADME 特性。Antitrypanosomal agent 7 的抗布氏锥虫 (T. brucei) 的活性 (IC50: 0.71 μM)，比 Nifurtimox 高两倍以上。Antitrypanosomal agent 7 与 DNA 有很强的相互作用，且能够选择性结合富含 AT 碱基的 DNA。

RKS262 is a specific cyclin CDK inhibitor. RKS262 was identified by structural optimization of Nifurtimox which is currently undergoing phase II clinical trials to treat high-risk neuroblastoma. In a NCI(60) cell-line assay RKS262 exhibited significant cytotoxicity in ovarian cancer cells and a variety of other cell lines exceeding effects of commercial drugs such as cisplatin, 5-FU, cyclophosphamide or sapacitabine. Various leukemia cell-lines were most sensitive (GI(50): ~ 10 nM) while several non-small cell lung cancer cell lines and few cell lines from other tissues were relatively resistant (GI(50) > 1 µM) to RKS262 treatment.