Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa.
Chem Biol Drug Des. 2022 Aug;100(2):267-279. doi: 10.1111/cbdd.14097. Epub 2022 Jun 21.
Leishmaniasis and cancer are two deadly diseases that plague the human population. There are a limited number of drugs available for the treatment of these diseases; however, their overuse has resulted in pathogenic resistance. Recent studies have indicated the repurposing of nitro-containing compounds to be a new avenue into finding new treatments. In this study, new nitrofuranyl sulfonohydrazide derivatives were synthesized and evaluated for their in vitro antileishmanial and anticancer activities. The analogue 2h, featuring biphenyl moiety exhibited selective (SI > 10) submicromolar activity (IC 0.97 μM) against acute promyelocytic leukemia cells hence was identified anticancer hit. This study revealed no antileishmanial hit. However, several promising analogues were uncovered and are worthy of further structural modifications to improve their toxicity and bioactivity profiles.
利什曼病和癌症是两种困扰人类的致命疾病。目前用于治疗这些疾病的药物数量有限；然而，它们的过度使用导致了致病性耐药性。最近的研究表明，重新利用含硝基的化合物是寻找新治疗方法的新途径。在这项研究中，合成了新的硝基呋喃基磺酰腙衍生物，并评估了它们的体外抗利什曼原虫和抗癌活性。具有联苯部分的类似物 2h 对急性早幼粒细胞白血病细胞表现出选择性（SI>10）亚微摩尔活性（IC0.97μM），因此被鉴定为抗癌命中。本研究未发现抗利什曼原虫命中。然而，发现了几种有前途的类似物，值得进一步进行结构修饰，以改善它们的毒性和生物活性谱。
