51114-94-4Relevant articles and documents
A Cisplatin-Selective Fluorescent Probe for Real-Time Monitoring of Mitochondrial Platinum Accumulation in Living Cells
Ong, Jun Xiang,Le, Hai Van,Lee, Violet Eng Yee,Ang, Wee Han
, p. 9264 - 9269 (2021)
Mitochondria have emerged as important targets for cisplatin in cancer therapy. Apart from cisplatin, anticancer Pt complexes based on similar scaffolds have also been developed to target mitochondria. Yet cellular processing of cisplatin or these mitocho
Crystal structure of new carboxylate phosphabetaines and phosphonium salts conjugated with them
Bakhtiyarova, Yu. V.,Aksunova,Galkina,Galkin,Lodochnikova,Kataeva
, p. 1313 - 1318 (2016)
Earlier unknown crystalline forms of three carboxylate phosphabetaines and conjugated with them phosphonium salts differing by β substituent with respect to the carboxylate group were studied. The structure of studied compounds in crystal is determined by
Azole-triphenylphosphonium conjugates combat antifungal resistance and alleviate the development of drug-resistance
Wang, Xin,Liu, Jun,Chen, Jinyao,Zhang, Ming,Tian, Chuan,Peng, Xiaoping,Li, Gang,Chang, Wenqiang,Lou, Hongxiang
, (2021/03/16)
Azole antifungals are commonly used to treat fungal infections but have resulted in the occurrence of drug resistance. Therefore, developing azole derivatives (AZDs) that can both combat established drug-resistant fungal strains and evade drug resistance is of great importance. In this study, we synthesized a series of AZDs with a fluconazole (FLC) skeleton conjugated with a mitochondria-targeting triphenylphosphonium cation (TPP+). These AZDs displayed potent activity against both azole-sensitive and azole-resistant Candida strains without eliciting obvious resistance. Moreover, two representative AZDs, 20 and 25, exerted synergistic antifungal activity with Hsp90 inhibitors against C. albicans strains resistant to the combination treatment of FLC and Hsp90 inhibitors. AZD 25, which had minimal cytotoxicity, was effective in preventing C. albicans biofilm formation. Mechanistic investigation revealed that AZD 25 inhibited the biosynthesis of the fungal membrane component ergosterol and interfered with mitochondrial function. Our findings provide an alternative approach to address fungal resistance problems.
Triazole compounds, preparation method and application of triazole compounds in antifungal drugs
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Paragraph 0030; 0034-0035, (2020/09/20)
The invention discloses a series of novel triazole compounds obtained by coupling a triazole drug skeleton and diversified lipophilic cations through different chains, and also discloses a preparationmethod of the compounds and application of the compound
