41115-30-4Relevant academic research and scientific papers
Tuning thiol addition to squaraines by ortho-substitution and the use of serum albumin
Diehl, Katharine L.,Bachman, J. Logan,Anslyn, Eric V.
, p. 316 - 324 (2017)
Tuning the reactivity of squaraine dyes toward nucleophilic addition of thiols was investigated. A series of water soluble, aniline-derived squaraines were synthesized with various ortho substitutions to the squaraine ring. As hypothesized, we found that placing moderately electron donating groups in the ortho position conveyed intermediate reactivity to thiols between the essentially non-reactive hydroxyl-substituted squaraines and very reactive non-substituted squaraines. Furthermore, serum albumin was tested for its influence on the addition of thiols to the squaraines. The dyes bind in the hydrophobic cavities of the protein, and thus we expected serum albumin to affect the squaraines' reactivity. Rather than a protective effect by the protein, we found a cooperative effect for thiol addition.
Orthogonal Self-Assembly of a Two-Step Fluorescence-Resonance Energy Transfer System with Improved Photosensitization Efficiency and Photooxidation Activity
Jia, Pei-Pei,Xu, Lin,Hu, Yi-Xiong,Li, Wei-Jian,Wang, Xu-Qing,Ling, Qing-Hui,Shi, Xueliang,Yin, Guang-Qiang,Li, Xiaopeng,Sun, Haitao,Jiang, Yanrong,Yang, Hai-Bo
supporting information, p. 399 - 408 (2021/01/12)
During the past few decades, fabrication of multistep fluorescence-resonance energy transfer (FRET) systems has become one of the most attractive topics within supramolecular chemistry, chemical biology, and materials science. However, it is challenging t
Synthesis of mitochondria-targeted coumarin-3-carboxamide fluorescent derivatives: Inhibiting mitochondrial TrxR2 and cell proliferation on breast cancer cells
Li, Yuanyuan,Tang, Qun,Xie, Yu,He, Dian,Yang, Kun,Zheng, Lifang
supporting information, (2021/01/18)
Targeting specific mitochondrial alterations to kill cancer cells without affecting their normal counterparts emerges as a feasible strategy. Coumarin derivatives have demonstrated the potential anti-breast cancer activities. By coupling coumarin-3-carbox
Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy
Zhao, Chenxi,Tang, Chu,Li, Changhao,Ning, Wentao,Hu, Zhiye,Xin, Lilan,Zhou, Hai-Bing,Huang, Jian
, (2021/05/10)
Hormone therapy targeting estrogen receptors is widely used clinically for the treatment of breast cancer, such as tamoxifen, but most of them are partial agonists, which can cause serious side effects after long-term use. The use of selective estrogen receptor down-regulators (SERDs) may be an effective alternative to breast cancer therapy by directly degrading ERα protein to shut down ERα signaling. However, the solely clinically used SERD fulvestrant, is low orally bioavailable and requires intravenous injection, which severely limits its clinical application. On the other hand, double- or multi-target conjugates, which are able to synergize antitumor activity by different pathways, thus may enhance therapeutic effect in comparison with single targeted therapy. In this study, we designed and synthesized a series of novel dual-functional conjugates targeting both ERα degradation and histone deacetylase inhibiton by combining a privileged SERD skeleton 7-oxabicyclo[2.2.1]heptane sulfonamide (OBHSA) with a histone deacetylase inhibitor side chain. We found that substituents on both the sulfonamide nitrogen and phenyl group of OBHSA unit had significant effect on biological activities. Among them, conjugate 16i with N-methyl and naphthyl groups exhibited potent antiproliferative activity against MCF-7 cells, and excellent ERα degradation activity and HDACs inhibitory ability. A further molecular docking study indicated the interaction patterns of these conjugates with ERα, which may provide guidance to design novel SERDs or PROTAC-like SERDs for breast cancer therapy.
OXAZINE-BASED WATER-SOLUBLE FLUOROPHORE COMPOUNDS FOR IN VIVO NERVE IMAGING
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, (2021/07/10)
This invention provides novel oxazine-based, water soluble fluorophore compounds useful in in vivo nerve imaging, as well as compositions comprising them and methods for their use.
OXAZINE-BASED FLUOROPHORE COMPOUNDS FOR NERVE-SPECIFIC IMAGING
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, (2021/07/31)
This invention concerns novel oxazine-based fluorophore compounds useful in invivo nerve imaging, as well as compositions comprising them and methods for their use.
NEAR-INFRARED NERVE-SPARING FLUOROPHORES
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, (2020/02/17)
Provided are far red to near-infrared nerve-sparing fluorescent compounds, compositions comprising them, and methods of their use in medical procedures.
NERVE-SPECIFIC FLUOROPHORE FORMULATIONS FOR DIRECT AND SYSTEMIC ADMINISTRATION
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, (2020/03/02)
Nerve-specific fluorophore formulations for direct or systemic administration are described. The formulations can be used in fluorescence-guided surgery (FGS) to aid in nerve preservation during surgical interventions.
Hydrogenation and: N-Alkylation of anilines and imines via transfer hydrogenation with homogeneous nickel compounds
Benitez-Medina, G. Eliad,García, Juventino J.
supporting information, p. 17579 - 17587 (2019/12/23)
The nickel-catalyzed N-Alkylation of a variety of arylamines via transfer hydrogenation in the absence of pressurized hydrogen and basic or acidic additives was achieved in a tandem reaction. This process was further extended to the CN bond reduction and N-Alkylation of a variety of imines with ethanol, the latter acting as a hydrogen and acetaldehyde source, which allowed for the reduction and subsequent condensation to yield the corresponding N-Alkylated products.
Cobalt-Catalyzed Reductive Alkylation of Amines with Carboxylic Acids
Emayavaramban, Balakumar,Chakraborty, Priyanka,Sundararaju, Basker
, p. 3089 - 3093 (2018/12/11)
Direct reductive alkylation of amines with carboxylic acid is carried out by using an inexpensive, air-stable cobalt/triphos catalytic system with molecular hydrogen as the reductant. This efficient synthetic method proceeds through reduction and condensation, followed by reduction of the in situ-generated imine into the amine in a green catalytic process.
