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Synthesis and evaluation of new dinitrobenzamide mustards in human prostate cancer
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-11-18 , DOI: 10.1016/j.bmcl.2020.127697
Alireza Basiri 1 , Wenting Zhang 1 , Jered Garrison 2
Affiliation  

Tumor hypoxia has been widely explored over the years as a diagnostic and therapeutic marker. Herein, we have reported the design and synthesis of a series of dinitrobenzamide mustards (DNBM) based on the PR-104A hypoxia-selective prodrug. Specifically, we explored the impact of various leaving groups and the introduction of a carboxylic acid group on the biological performance of the DNBM constructs. Once in hand, the Log D values, cytotoxicity in PC-3 and DU-145 human prostate cancer cells lines and the hypoxia selectivities of the DNBM analogs were examined. Overall, the DNBM constructs were found to be tolerant to modifications with none of the explored modifications substantially degrading the cytotoxic potential of the constructs.



中文翻译:

新型二硝基苯甲酰胺芥子气治疗人前列腺癌的合成与评价

多年来,肿瘤缺氧作为诊断和治疗标志物得到了广泛的探索。在此,我们报道了一系列基于 PR-104A 缺氧选择性前药的二硝基苯甲酰胺芥 (DNBM) 的设计和合成。具体而言,我们探讨了各种离去基团和羧酸基团的引入对 DNBM 构建体的生物学性能的影响。一旦掌握,就检查了 Log D 值、PC-3 和 DU-145 人前列腺癌细胞系的细胞毒性以及 DNBM 类似物的缺氧选择性。总体而言,发现 DNBM 构建体对修饰具有耐受性,所探索的修饰均未显着降低构建体的细胞毒性潜力。

更新日期:2020-12-01
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