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Anticancer Effect of Chlorambucil Enhanced by Chiral Phthalidyl Promoiety
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2022-11-25 , DOI: 10.1002/cbdv.202201025 Long Zhang 1 , Yisa Cheng 2 , Ying-Guo Liu 2 , Xingkuan Chen 3 , Hongmei Liu 1
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2022-11-25 , DOI: 10.1002/cbdv.202201025 Long Zhang 1 , Yisa Cheng 2 , Ying-Guo Liu 2 , Xingkuan Chen 3 , Hongmei Liu 1
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Phthalidyl promoiety has been used in several drugs, but they were all marketed in racemic form. The pharmaceutical effects of each enantiomer have not been clearly demonstrated. In this project, an anticancer chemotherapy drug, chlorambucil, was modified as enantiopure phthalidyl prodrugs. The enantiomers, together with phthalidyl unit and their racemic mixture, were then subject to the in vivo bioactivity tests against B16F10 melanoma cells. It was found that proper chirality within the promoiety had noticeably better in vivo pharmacological effects than the parent drug, the enantiomer and racemic mixture. This merit perhaps could be extended from the phthalidyl prodrugs to other chirality containing prodrugs.
中文翻译：
苯丁酸氮芥手性邻苯二甲酰基团增强苯丁酸氮芥的抗癌作用
Phthalidyl promoiety 已用于多种药物，但它们都以外消旋形式销售。每种对映异构体的药物作用尚未得到明确证明。在该项目中，抗癌化疗药物苯丁酸氮芥被修饰为对映体纯的邻苯二甲酰前药。然后将对映体连同邻苯二甲酰基单元及其外消旋混合物进行针对 B16F10 黑色素瘤细胞的体内生物活性测试。结果发现，前部分内适当的手性比母体药物、对映异构体和外消旋混合物具有明显更好的体内药理作用。这种优点也许可以从酞酰基前药扩展到其他含有手性的前药。
更新日期：2022-11-25
中文翻译：
苯丁酸氮芥手性邻苯二甲酰基团增强苯丁酸氮芥的抗癌作用
Phthalidyl promoiety 已用于多种药物，但它们都以外消旋形式销售。每种对映异构体的药物作用尚未得到明确证明。在该项目中，抗癌化疗药物苯丁酸氮芥被修饰为对映体纯的邻苯二甲酰前药。然后将对映体连同邻苯二甲酰基单元及其外消旋混合物进行针对 B16F10 黑色素瘤细胞的体内生物活性测试。结果发现，前部分内适当的手性比母体药物、对映异构体和外消旋混合物具有明显更好的体内药理作用。这种优点也许可以从酞酰基前药扩展到其他含有手性的前药。
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