- Exploring the tetrahydroisoquinoline thiohydantoin scaffold blockade the androgen receptor as potent anti-prostate cancer agents
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Prostate cancer (PC) is a major cause of cancer-related male death in worldwide and the identification of new and improved potent anti-PC molecules is constantly required. A novel scaffold of tetrahydroisoquinoline thiohydantoin was rationally designed based on the enzalutamide structures and our pre-work, leading to the discovery of a series of new antiproliferative compounds. Several new analogues displayed improved androgen receptor (AR) antagonistic activity, while maintaining the higher selective toxicity toward LNCaP cells (AR-rich) versus DU145 cells (AR-deficient) compared to enzalutamide. In fact, compound 55 exhibited promising in vitro antitumor activity by impairing AR unclear translocation. More importantly, 55 showed better pharmacokinetic properties compared to the compound 1 reported in our pre-work. These results demonstrate a step towards the development of novel and improved AR antagonists.
- Xu, Xi,Ge, Raoling,Li, Lei,Wang, Jubo,Lu, Xiaoyu,Xue, Siqi,Chen, Xijing,Li, Zhiyu,Bian, Jinlei
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p. 1325 - 1344
(2017/11/13)
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- Composition of matter having bioactive properties
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Particles of coordinated complex comprising a basic, hydrous polymer and a capacitance adding compound, as well as methods for their production, are described. These complexes exhibit a high degree of bioactivity making them suitable for a broad range of applications through their incorporation into conventional vehicles benefiting from antimicrobial and similar properties.
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- Regioselective iodination of tyrosine in a liquid membrane system, in the presence of crown ether type macrocyclic ligands. I obtention of monoiodotyrosine
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The experiments performed have shown that, when using a "liquid membrane" system (aqueous phase source containing KI + I2 K+I3-, the receiving aqueous phase containing tyrosine, the "liquid membrane" being represented by dichloroethane, which contains the crown ether CE =18-crown-6), the selective iodination of tyrosine can be controlled so as to obtain, after four hours, monoiodotyrosine with a 100% yield.
- Luca, Constantin,Zarna, Adriana,Anghel, Dan,Constantinescu, Titus
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p. 125 - 130
(2007/10/03)
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- Regioselective iodination of tyrosine in a liquid membrane system in the presence of crown ether type, macrocyclic ligands. II: The factors which influence regioselective iodination
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The regioselective iodination of tyrosine 1 in a "liquid membrane" system - aqueous phase source/dichloroethane/aqueous receiving phase - in view of obtaining preferentially, first, monoiododerivative 2 and then diiododerivative 3 is controlled by the exclusive existence in the "liquid membrane" of the complex species [CE?I]+I3- (with no free I2). The highest yield (100%) of derivative 2 is obtained when CE=18-crown-6. The process is considered to be of the electophilic aromatic substitution type (through "phase transfer catalysis") the experiments suggesting that the reactive iodine species results from the [CE?I]+I3- complex decomposition at the "membrane"/receiving aqueous phase (containing tyrosine) interface.
- Luca, Constantin,Zarnǎ, Adriana,Anghel, Dan,Constantinescu, Titus
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p. 601 - 608
(2007/10/03)
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