4.7 Article

Fluorinated Rhodacyanine (SJL-01) Possessing High Efficacy for Visceral Leishmaniasis (VL)

期刊

JOURNAL OF MEDICINAL CHEMISTRY
卷 53, 期 1, 页码 368-373

出版社

AMER CHEMICAL SOC
DOI: 10.1021/jm9013086

关键词

-

向作者/读者索取更多资源

Anti-Leishmania in vitro and in vivo activities of various rhodacyanine derivatives have been examined. Among them, the fluorinatied variant SJL-01 (8) showed IC50 OfO-01 I PM against Lcishniania (Ionovani strain MHOM/ET/67/1_82 (selective index of > 15000) and 95-97% inhibition against L. clonovani strain MHOM/ET/67/HIJ in fernale BALB/c mice by 1.3-12.5 mg/kg x 5 iv administrations. Negative results on chromosonial aberration test and in vitro micronucleus test Suggest that compound 8 is a hopeful candidate for visceral leislinianiasis (VIL).

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.7
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

Article Chemistry, Multidisciplinary

Leveraging Electron-Deficient Iminium Intermediates in a General Synthesis of Valuable Amines

Che-Sheng Hsu, Carlos R. Goncalves, Veronica Tona, Amandine Pons, Marcel Kaiser, Nuno Maulide

Summary: The article presents a method of synthesizing amine compounds using highly electron-deficient iminium ions and highlights its broad applicability through a specific case study.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2022)

Article Chemistry, Medicinal

Laboratory Selection of Trypanosomatid Pathogens for Drug Resistance

Sabina Beilstein, Radhia El Phil, Suzanne Sherihan Sahraoui, Leonardo Scapozza, Marcel Kaiser, Pascal Maser

Summary: This article discusses the experimental methods and strategies for selecting drug-resistant parasites, using African trypanosomes as an example. Researchers need to consider factors such as the environmental conditions, life stages, and pressure for selecting drug resistance, while taking into account the laboratory settings.

PHARMACEUTICALS (2022)

Article Chemistry, Applied

Several Golgi targeting fluorescence markers based on 1,8-naphthalimide derivatives with amide and long carbon chain

Xu-Chen Feng, Gang Zhang, Ru Sun, Yu-Jie Xu, Jian-Feng Ge

Summary: This study designed and synthesized three new Golgi markers for monitoring the normal functioning of the Golgi apparatus. The experiments showed that these markers were able to rapidly and accurately label the Golgi apparatus, and they had low cytotoxicity.

DYES AND PIGMENTS (2023)

Article Biochemical Research Methods

Methylated Chromenoquinoline as a Novel Nucleus Fluorescent Probe for Nucleic Acid Imaging

Zhi-Hao Zhang, Qing Yu, Gang Zhang, Hai-Yan Peng, Ru Sun, Yu-Jie Xu, Jian-Feng Ge

Summary: Two chromenoquinoline-based fluorescent probes 1a-b were synthesized and studied, showing good photostability and selectivity after 6 h irradiation, strong absorption and emission in organic solvents, and the influence of alkylation on the optical properties of 1b.

JOURNAL OF FLUORESCENCE (2023)

Article Biochemistry & Molecular Biology

Synthesis and Antiprotozoal Activity of Azabicyclo-Nonane Pyrimidine Hybrids

Clemens Hinteregger, Johanna Dolensky, Werner Seebacher, Robert Saf, Pascal Maeser, Marcel Kaiser, Robert Weis

Summary: 2,4-Diaminopyrimidines and (dialkylamino)azabicyclo-nonanes have activity against protozoan parasites. A series of fused hybrids were synthesized and tested in vitro against malaria tropica and sleeping sickness pathogens. The activities and selectivities of compounds strongly depended on the substitution pattern of both ring systems as well as the position of the nitrogen atom in the bicycles.

MOLECULES (2023)

Article Chemistry, Multidisciplinary

Benzyl- and dibenzyl tetrahydropyridinylidene ammonium salts with antiplasmodial and antitrypanosomal activity

Werner Seebacher, Marcel Kaiser, Pascal Maeser, Robert Saf, Eva-Maria Pferschy-Wenzig, Robert Weis

Summary: Several 1-benzyl and 1,3-dibenzyl derivatives of tetrahydropyridinylidene salts with varying electron withdrawing substituents at the aromatic residues have been synthesized and investigated for their biological activities and cytotoxicity. Characterization of these compounds was carried out using FT-IR, HRMS and NMR spectroscopy.

MONATSHEFTE FUR CHEMIE (2023)

Article Chemistry, Organic

Conjugated structures based on quinazolinones and their application in fluorescent labeling

Ming-Sen Zhu, Gang Zhang, Yu-Jie Xu, Ru Sun, Jian-Feng Ge

Summary: In this study, probes 5a-c and 6b were synthesized by introducing quinazolinone into aldehydes with different double bond numbers. These probes exhibited absorption and emission maxima in different polar solvents. Probe 5c showed significant fluorescence enhancement with increased viscosity. Moreover, probes 5a-c and 6b showed pH-sensitive fluorescence intensity enhancement in alkaline solution. Cell experiments demonstrated the ability of probes 5a-b to target mitochondria and probes 5c-6b to target lysosomes.

ORGANIC & BIOMOLECULAR CHEMISTRY (2023)

Article Chemistry, Multidisciplinary

Fluorescence Enhancement of Adamantane-Modified Dyes in Aqueous Solution via Supramolecular Interaction with Methyl-β-cyclodextrin and Their Application in Cell Imaging

Hong-Jiao Liu, Gang Zhang, Yu-Jie Xu, Ru Sun, Jian-Feng Ge

Summary: A novel strategy based on host-guest interaction was proposed for fluorescence enhancement in aqueous solution and cell imaging. By modifying the dyes and forming covalent bonds with methylated beta-cyclodextrin, fluorescent supramolecular nanoparticles were formed, leading to improved fluorescence quantum yields.

CHEMISTRY-A EUROPEAN JOURNAL (2023)

Article Multidisciplinary Sciences

Cyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections

Srinivasa P. S. Rao, Matthew K. Gould, Jonas Noeske, Manuel Saldivia, Rajiv S. Jumani, Pearly S. Ng, Olivier Rene, Yen-Liang Chen, Marcel Kaiser, Ryan Ritchie, Amanda Fortes Francisco, Nila Johnson, Debjani Patra, Harry Cheung, Colin Deniston, Andreas D. Schenk, Wilian A. Cortopassi, Remo S. Schmidt, Natalie Wiedemar, Bryanna Thomas, Rima Palkar, Nahdiyah A. Ghafar, Vanessa Manoharan, Catherine Luu, Jonathan E. Gable, Kah Fei Wan, Elmarie Myburgh, Jeremy C. Mottram, Whitney Barnes, John Walker, Charles Wartchow, Natasha Aziz, Colin Osborne, Juergen Wagner, Christopher Sarko, John M. Kelly, Ujjini H. Manjunatha, Pascal Maeser, Jan Jiricek, Suresh B. Lakshminarayana, Michael P. Barrett, Thierry T. Diagana

Summary: Millions of people in Latin America and sub-Saharan Africa are at risk of trypanosomatid infections. Researchers have identified a class of cyanotriazoles (CTs) that have potent trypanocidal activity and can potentially be used for the treatment of Chagas disease and human African trypanosomiasis. These CT compounds act by selectively and irreversibly inhibiting trypanosomal topoisomerase II and stabilizing DNA:enzyme cleavage complexes.

SCIENCE (2023)

Article Spectroscopy

ESIPT-based fluorescent enhanced probes prompted by methylated beta-cyclodextrin for the detection of thiophenols

Hai-Yan Peng, Gang Zhang, Ru Sun, Yu-Jie Xu, Jian-Feng Ge

Summary: In order to detect the level of thiophenols in the environment and biological samples, probes 1a-b were synthesized by introducing the 2,4-dinitrophenyl ether group into diethylcoumarin-salicylaldehyde based compounds. These probes can form host-guest compounds with methylated beta-cyclodextrin, showing significant increase in fluorescence intensity in thiophenols detection. The hydrophobic cavity of methylated beta-cyclodextrin enhances the fluorescence intensity of probes 1a-b and reduces their detection limits to thiophenols, without affecting their selectivity and response time.

SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY (2023)

Article Chemistry, Analytical

Viscosity probes towards different organelles with red emission based on an identical hemicyanine structure

Hong-Jiao Liu, Ming-Sen Zhu, Gang Zhang, Ru Sun, Yu-Jie Xu, Jian-Feng Ge

Summary: A series of viscosity probes targeting different organelles were obtained using a single hemicyanine dye as the matrix structure. These probes had relatively large molar absorption coefficients in the red light region and their fluorescence intensity in glycerol was 35-184 times higher than that in phosphate buffer solution (PBS). Cell staining experiments demonstrated that these probes could target lysosomes, endoplasmic reticulum and mitochondria, and undergo viscosity-detectable changes in the corresponding organelles.

ANALYST (2023)

Article Materials Science, Biomaterials

Multiple organelle-targeted 1,8-naphthyridine derivatives for detecting the polarity of organelles

Hao-Chi Hao, Gang Zhang, Ru Sun, Yu-Jie Xu, Jian-Feng Ge

Summary: Four 1,8-naphthyridine derivatives (1a-1d) with different organelle targeting abilities were synthesized. The optical properties of the derivatives were characterized, showing a red-shift of fluorescence emission with increasing system polarity. Colocalization imaging experiments confirmed the organelle-targeting capabilities of the derivatives and their ability to monitor organelle polarity fluctuation. This work proposes a new molecular design idea for developing polarity-sensitive fluorescent probes with organelle targeting.

JOURNAL OF MATERIALS CHEMISTRY B (2023)

Article Chemistry, Analytical

Fluorescent probes based on quinoline and naphthidine derivatives with NIR and AIE properties for real-time monitoring mitochondrial viscosity during mitophagy

Jing-Yu Zhao, Gang Zhang, Hao-Chi Hao, Ru Sun, Yu-Jie Xu, Jian-Feng Ge

Summary: This study presents the discovery of mitochondria probes for real-time monitoring of mitophagy process. The probes showed excellent fluorescence performance and targeting capability, and were able to detect changes in mitochondrial viscosity. These probes have significant potential for investigating dynamic pathological processes related to mitophagy.

SENSORS AND ACTUATORS B-CHEMICAL (2024)

Article Chemistry, Organic

Improved emission performance of benzo[a]phenoxazine in aqueous solution through host-guest interaction

Shu-Yi Li, Wen-Li Wang, Chang Wang, Ru Sun, Jian-Feng Ge

Summary: This study evaluates the contribution of host-guest chemistry in fluorescence enhancement under aqueous conditions. Two benzo[a]phenoxazine derivatives with the adamantyl group were synthesized and formed stable complexes with methyl-beta-cyclodextrin. The emissions of these complexes were greatly increased in aqueous solution, with fluorescence quantum yields reaching 11.5-12.6%. Furthermore, they were successfully applied in fluorescence labeling of organelles in HeLa cells.

ORGANIC & BIOMOLECULAR CHEMISTRY (2023)

Article Chemistry, Applied

Naphthyridine-based neutral fluorescent probes for dynamic monitoring lipid droplet polarity

Meng-Nan Li, Jing-Yu Zhao, Gang Zhang, Yu-Jie Xu, Jian-Feng Ge, Ru Sun

Summary: This paper reports the design and synthesis of novel nitrogen-containing heterocycle dyes with large conjugated planar structures. These dyes exhibited excellent optical properties and potential biological applications. They showed fluorescence intensity changes and high fluorescence quantum yields in different solvents, with the polarity of the solvents affecting their excited-state lifetime. The dyes demonstrated toxicity towards cancer cells and growth-promoting effects on normal cells. Additionally, they could be used for long-term observation of targeted cellular physiological activity and dynamic monitoring of changes in lipid droplets polarity. The results have important implications for understanding the physiological functions of lipid droplets.

DYES AND PIGMENTS (2023)

暂无数据