142356-33-0Relevant articles and documents
Zn(2+) fluorescent chemosensors and the influence of their spacer length on tuning Zn(2+) selectivity
Kim, Tae Woo,Park, Jung-hyun,Hong, Jong-In
, p. 923 - 927 (2002)
Zn(2+) fluorescent chemosensors based on the chelation-enhanced fluorescence (CHEF) mechanism were prepared and fine-tuning of their Zn(2+) selectivity was achieved by control of the spacer length. The fluorescence emission response to metal ions shows a fluorescence decrease for Co(2+), Cu(2+) and Ni(2+) and an increase for Ca(2+), Cd(2+) and Zn(2+). Maximum Zn(2+) selectivity over Ca(2+) and Cd(2+) was achieved with 3. The basic binding properties (stoichiometry, apparent dissociation constant, and pH dependence) were measured by fluorescence spectroscopy. Analysis of the Job plot for the 3-Zn(2+) complex indicates the formation of a 1 :1 complex. The apparent dissociation constant Kd was determined as 0.98 (+/-0.43) nM for 3-Zn(2+) at pH 7.5 [50 mM HEPES buffer I = 0.1 (NaNO3)]. The plateaus in the fluorescence intensity of 2 and the 2-Zn(2+) complex in regions with a pH exceeding 7 imply that the fluorescence measurements should be little affected by physiological pH changes.
Gd(III)-nanodiamond conjugates for MRI contrast enhancement
Manus, Lisa M.,Mastarone, Daniel J.,Waters, Emily A.,Zhang, Xue-Qing,Schultz-Sikma, Elise A.,MacRenaris, Keith W.,Ho, Dean,Meade, Thomas J.
, p. 484 - 489 (2010)
A Gd(III)-nanodiamond conjugate [Gd(III)-ND] was prepared and characterized, enabling detection of nanodiamonds by MR imaging. The Gd(III)-ND particles significantly reduced the T1 of water protons with a per-Gd(III) relaxlvity of 58.82 ± 1.18 mM-1 s-1 at 1.5 T (60 MHz). This represents a 10-fold increase compared to the monomer Gd(III) complex (r1= 5.42 ± 0.20 mM-1 s -1) and is among the highest per-Gd(III) relaxivities reported.
Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer
Zhang, Wanheng,Zhang, Kuojun,Yao, Yiwu,Liu, Yunyao,Ni, Yong,Liao, Chenzhong,Tu, Zhengchao,Qiu, Yatao,Wang, Dexiang,Chen, Dong,Qiang, Lei,Li, Zheng,Jiang, Sheng
, (2021)
Multitarget drugs have emerged as a promising treatment modality in modern anticancer therapy. Taking advantage of the synergy of NAMPT and EGFR inhibition, we have developed the first compounds that serve as dual inhibitors of NAMPT and EGFR. On the basis of CHS828 and erlotinib, a series of hybrid molecules were successfully designed and synthesized by merging of the pharmacophores. Among the compounds that were synthesized, compound 28 showed good NAMPT and EGFR inhibition, and excellent in vitro anti-proliferative activity. Compound 28, which is a new chemotype devoid of a Michael receptor, strongly inhibited the proliferation of several cancer cell lines, including H1975 non-small cell lung cancer cells harboring the EGFRL858R/T790M mutation. More importantly, it imparted significant in vivo antitumor efficacy in a human NSCLC (H1975) xenograft nude mouse model. This study provides promising leads for the development of novel antitumor agents and valuable pharmacological probes for the assessment of dual inhibition in NAMPT and EGFR pathway with a single inhibitor.
THERAPEUTIC METAL COMPLEXES AND LIGANDS AND METHODS OF MAKING AND USING SAME
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Page/Page column 56; 57, (2019/03/17)
Disclosed herein are compound embodiments that are useful for treating a variety of diseases, particularly neurological diseases, motor neuron diseases, copper deficiency-related diseases, and/or mitochondrial deficiencies. The compound embodiments described herein also can be used in PET methods. Also disclosed herein are embodiments of methods of making and using the compound embodiments, as well as pharmaceutical formulations comprising the disclosed compound embodiments.
BICYCLIC AND TRICYCLIC CAP BEARING MERCAPTOACETAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
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Paragraph 0154; 0157; 0158, (2017/04/11)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
