51114-94-4Relevant academic research and scientific papers
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
Mitochondria-Targeting Magnetic Composite Nanoparticles for Enhanced Phototherapy of Cancer
Guo, Ranran,Peng, Haibao,Tian, Ye,Yang, Wuli,Shen, Shun
, p. 4541 - 4552 (2016)
Photothermal therapy (PTT) and photodynamic therapy (PDT) are promising cancer treatment modalities in current days while the high laser power density demand and low tumor accumulation are key obstacles that have greatly restricted their development. Here
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
Synthesis and pharmacological characterization of mitochondrial KATP channel openers with enhanced mitochondriotropic effects
Testai, Lara,Sestito, Simona,Martelli, Alma,Gorica, Era,Flori, Lorenzo,Calderone, Vincenzo,Rapposelli, Simona
, (2021/01/11)
Mitochondria play a key role for deciding fate of cells and thus are considered an attractive target for pharmacological interventions focused on containment of myocardial ischemia/reperfusion (I/R) injury. Notably, the activation of mitochondrial potassi
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.
Synthesis of Allylboranes via Cu(I)-Catalyzed B-H Insertion of Vinyldiazoacetates into Phosphine-Borane Adducts
Drikermann, Denis,M??el, Robert S.,Al-Jammal, Walid K.,Vilotijevic, Ivan
supporting information, p. 1091 - 1095 (2020/02/15)
Cu(I) catalysts enable C-B bond formation via direct insertion of vinyldiazoacetates into B-H bonds of borane-phosphine Lewis adducts to form phosphine-protected allylboranes under mild conditions. The resulting allylborane-phosphine Lewis adducts can be used in the diastereoselective allylation of aldehydes directly without the need for removal of the phosphine. The allylation reaction proceeds with high diastereoselectivity and yields 5,6-disubstituted dihydropyranones after treatment with an appropriate acid.
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
Asymmetric Construction of Cyclobutanes via Direct Vinylogous Michael Addition/Cyclization of β,γ-Unsaturated Amides
Chen, Yuzhen,Huang, Huicai,Ma, Yan-Yan,Wang, Shuzhong,Wang, Yichen,Zhan, Ruoting,Zhao, Deng-Gao
supporting information, p. 7135 - 7140 (2020/10/12)
The construction of cyclobutanes has attracted much attention because of its unique four-membered ring skeleton. Herein, we report the highly enantioselective direct vinylogous Michael reaction of β,γ-unsaturated pyrazole amides and nitroolefin using a squaramide catalyst. Cyclobutane derivatives were obtained by subsequent cyclization in good yields (up to 85%) with excellent enantioselectivities (up to 99% ee). Importantly, the large-scale reaction experiment confirmed the reliability of the vinylogous reaction. Furthermore, the synthetic utility of the vinylogous adducts and cyclobutane derivatives has been realized.
Synthesis of [18 F]-γ-Fluoro-α,β-unsaturated Esters and Ketones via Vinylogous 18 F-Fluorination of α-Diazoacetates with [18 F]AgF
Brooks, Allen F.,Ichiishi, Naoko,Jackson, Isaac M.,Lee, So Jeong,Sanford, Melanie S.,Scott, Peter J. H.,Thompson, Stephen
supporting information, p. 4401 - 4407 (2019/11/21)
This communication reports a method for the vinylogous radiofluorination of α-diazoacetates to generate [18 F]-γ-fluoro-α,β-unsaturated esters and ketones in moderate to good radiochemical yields. The method uses no-carrier-added [18 F]AgF and is compatible with aromatic and non-aromatic substrates and a number of different functional groups. The labeling method is showcased in the synthesis of a fluorinated cholest-5-en-3-one derivative as well as a difluorinated product pertinent to drug discovery.
BETA-2 SELECTIVE ADRENERGIC RECEPTOR AGONISTS
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Page/Page column 66, (2019/06/23)
Aspects of the present disclosure include conformationally restricted analogs of catecholamine type compounds (e.g., isoprenaline, adrenaline, noradrenaline) which activate β2AR with high selectivity over β1AR. The subject beta-2 selective adrenergic rece
