19813-90-2Relevant articles and documents
Characterization of the conductivity of organic thiols by field emission microscopy and field emission spectroscopy
Purcell,Garcia,Binh, Vu Thien,Jones II,Tour
, p. 11985 - 11989 (1994)
The conducting properties of two organic thiols (5-mercapto-2,2′-bithiophene and 4-mercaptobiphenyl) deposited by the self-assembly method on Pt tips have been characterized in ultrahigh vacuum by field emission microscopy and spectroscopy. It was shown that these two molecular species can be successfully adsorbed from solution on the Pt tip. The presence of the molecules causes a large decrease in the required field emission voltages by a factor of ～3-5. Measurement of the total energy distributions of the emitted electrons showed that the electrons are emitted from a narrow band which is not pinned at the Fermi level but which shifts to lower energy with increased applied field. The molecules thus appear more like an insulator than a conductor. Significant current-induced heating of the molecules was found: for example, ΔT ≈ 80 K for 0.3 nA. Taken together these properties pose problems for the use of these and similar one-dimensional molecules as current-carrying connections in proposed nanoscale electronic applications. However, when used in the subpicoampere range, the current through the wire may be sustainable and dissipation small. In general, these experiments open a door to exploring other molecules.
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Lester,Rodgers,Reid
, p. 1674 (1944)
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Discovery of 3,5-Dimethyl-4-Sulfonyl-1 H-Pyrrole-Based Myeloid Cell Leukemia 1 Inhibitors with High Affinity, Selectivity, and Oral Bioavailability
Zhu, Peng-Ju,Yu, Ze-Zhou,Lv, Yi-Fei,Zhao, Jing-Long,Tong, Yuan-Yuan,You, Qi-Dong,Jiang, Zheng-Yu
, p. 11330 - 11353 (2021/08/24)
Myeloid cell leukemia 1 (Mcl-1) protein is a key negative regulator of apoptosis, and developing Mcl-1 inhibitors has been an attractive strategy for cancer therapy. Herein, we describe the rational design, synthesis, and structure-activity relationship study of 3,5-dimethyl-4-sulfonyl-1H-pyrrole-based compounds as Mcl-1 inhibitors. Stepwise optimizations of hit compound 11 with primary Mcl-1 inhibition (52%@30 μM) led to the discovery of the most potent compound 40 with high affinity (Kd = 0.23 nM) and superior selectivity over other Bcl-2 family proteins (>40,000 folds). Mechanistic studies revealed that 40 could activate the apoptosis signal pathway in an Mcl-1-dependent manner. 40 exhibited favorable physicochemical properties and pharmacokinetic profiles (F% = 41.3%). Furthermore, oral administration of 40 was well tolerated to effectively inhibit tumor growth (T/C = 37.3%) in MV4-11 xenograft models. Collectively, these findings implicate that compound 40 is a promising antitumor agent that deserves further preclinical evaluations.
Preparation method for synthesizing thiophenol compound based on sodium sulfide nonahydrate
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Paragraph 0031; 0032, (2017/08/30)
The invention provides a preparation method for synthesizing a thiophenol compound based on sodium sulfide nonahydrate. In an inert gas protective atmosphere, substituted iodobenzene and a sulfhydrylation reagent are added into an aprotic polar solvent, then a copper salt catalyst and a ligand compound are orderly added into the solution, the mixed solution undergoes a reaction at a temperature of 90 to 120 DEG C for 12-24h, and the reaction solution is cooled to the room temperature and is acidized so that the product is obtained. The preparation method has the advantages of simple reaction conditions, good compatibility of functional groups, high yield and small environmental pollution. Thiophenol is an important intermediate for pharmaceutical chemical synthesis and has a very wide application range in fields of chemical raw materials, pesticides and medicines. The preparation method has a great use value and good social and economic benefits.
SINGLE-STEP SYNTHESIS METHOD OF ARYL THIOL AND APPLICATION THEREOF
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Paragraph 0032; 0033; 0063; 0067; 0068; 0070, (2017/09/02)
The present invention relates to a single-step synthesis method of aryl thiol, and more specifically, to a method of synthesizing aryl thiol in a single-step by making aryl halide react with alkane dithiol in the presence of a transition metal catalyst. According to the present invention, a single-step synthesis method using the transition metal catalyst, the synthesis method which is capable of synthesizing aryl thiol from aryl halide at a high yield, can be provided. Various aryl halides may be applied to the synthesis method. Further, the synthesis method has advantages that an easily usable reagent may be used, operations are simple, and reactions can be performed under mild conditions. In addition, the synthesized aryl thiol may be used in the synthesis of advanced molecules such as diaryl sulfides and benzothiophenes.COPYRIGHT KIPO 2017
