共轭不饱和酮的细胞毒性被硫醇灭活了吗?

IF 1.5 4区医学 Q4 CHEMISTRY, MEDICINAL

Pharmazie Pub Date : 2023-07-01 DOI:10.1691/ph.2023.3542

A Doroudi, P K Roayapalley, S Das, U Das, J R Dimmock

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引用次数: 0

摘要

本研究的重点是研究细胞毒性共轭不饱和酮(或烯酮)转化为相应的硫醇加合物是否会导致细胞毒性的减少或消除。一些烯酮和相关的硫醇加合物对人HCT116和HT29结肠癌细胞的作用进行了评估。约63%的IC50值小于10 μM，一些化合物的毒性大于5-FU。巯基加合物与相应的烯酮或强或弱。许多化合物对HCT116和HT29肿瘤的毒性远高于非恶性CRL1790细胞，这导致了令人印象深刻的选择性指数数字。这些化合物的另一个积极特征是它们具有良好的ADME特性。

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Are the Cytotoxic Properties of Conjugated Unsaturated Ketones Inactivated by Thiols?

The focus of this study was to examine whether the conversion of cytotoxic conjugated unsaturated ketones (or enones) into the corresponding thiol adducts leads to a reduction or abolition of cytotoxic potencies. A number of enones and related thiol adducts were evaluated against human HCT116 and HT29 colon cancer cells. Some 63% of the IC₅₀ values are less than 10 μM and several compounds are more toxic than 5-FU. The thiol adducts are either more potent or are equipotent with the corresponding enones. A number of compounds are far more toxic to HCT116 and HT29 neoplasms than non-malignant CRL1790 cells leading to impressive Selectivity Index figures. An additional positive feature of these compounds is that they have favorable ADME properties.

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来源期刊

Pharmazie 医学-化学综合

CiteScore

3.10

自引率

0.00%

发文量

审稿时长

1.2 months

期刊介绍： The journal DiePharmazie publishs reviews, experimental studies, letters to the editor, as well as book reviews. The following fields of pharmacy are covered: Pharmaceutical and medicinal chemistry; Pharmaceutical analysis and drug control; Pharmaceutical technolgy; Biopharmacy (biopharmaceutics, pharmacokinetics, biotransformation); Experimental and clinical pharmacology; Pharmaceutical biology (pharmacognosy); Clinical pharmacy; History of pharmacy.