- THIOESTER CATIONIC LIPIDS
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Disclosed are cationic lipids which are compounds of Formula (I), (II), (III), (IV), (V), or (VI). Cationic lipids provided herein can be useful for delivery and expression of mRNA and encoded protein, e.g., as a component of liposomal delivery vehicle, a
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Paragraph 0389
(2019/12/15)
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- Thioether allyl isothiocyanate compounds, and preparation method and applications thereof
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The invention provides a series of novel thioether allyl isothiocyanate compounds with a general structure disclosed in the invention, and a simple method used for rapid synthesis of the thioether allyl isothiocyanate compounds. According to the method, double-terminal halogen-substituted alkanes are taken as initial raw materials, are reacted with phthalimide potassium so as to introduce N atoms, are reacted with sodium hydrosulfide so as to produce mercaptan, and mercaptan is reacted with benzyl bromide or is reacted with a heterocyclic compound with sulfydryl so as to introduce the thioether structure, an obtained product is reacted with hydrazine hydrate so as to obtain a primary amine, and the primary amine is reacted with an alkali, carbon disulfide, and methylsufonyl chloride so as to prepare the thioether allyl isothiocyanate compounds with heterocyclic nitrogen structures. The method contains few steps; operation is simple; the obtained products can be easily purified; and yield is high. The series of novel thioether allyl isothiocyanate compounds possess obvious killing activity on tumor cells, and possess obvious killing activity on cervical carcinoma cells and lung cancer cells.
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Paragraph 0051; 0066; 0067; 0068
(2016/10/08)
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- Synthesis and biological evaluation of sulforaphane derivatives as potential antitumor agents
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A series of sulforaphane derivatives were synthesized and evaluated in vitro for their cytotoxicity against five cancer cell lines (HepG2, A549, MCF-7, HCT-116 and SH-SY5Y). The pharmacological results showed that many of the derivatives displayed more potent cytotoxicity than sulforaphane (SFN). Furthermore, SFN and derivative 85 could induce cell cycle arrest at S or G2/M phase and cell apoptosis. SFN and 85 exhibited time- and dose-dependent activation on Nrf2 transcription factor, and 85 acted as a more potent Nrf2 inducer than SFN.
- Hu, Kun,Qi, Yan-Jie,Zhao, Juan,Jiang, He-Fei,Chen, Xin,Ren, Jie
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p. 529 - 539
(2013/07/11)
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- Building units for N-backbone cyclic peptides. 2. Synthesis of protected N-(ω-thioalkylene) amino acids and their incorporation into dipeptide units
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A new family of amino acids which contain an ω-thioalkylene group on the N(α)-amino nitrogen was synthesized by alkylation of ω-thioalkylamines with triflates of α-hydroxy acids. The reaction proceeded with inversion of configuration yielding optically pure products. The N(α)-(ω-thioalkylene)amino acids were orthogonally protected to allow their incorporation into peptides by solid-phase peptide synthesis (SPPS) methodology. In addition some of these new protected N(α)-(ω-thioalkylene)amino acids were incorporated into dipeptides by 'solution' techniques.
- Bilan, Gal,Gilon, Chaim
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p. 10513 - 10522
(2007/10/02)
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- Dimethyl tyrosyl amide sulfides, sulfoxides and sulfones
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The present invention relates to new compounds of the formula STR1 and the pharmaceutically acceptable salts thereof and the enantiomers thereof, wherein R1 is H, lower alkyl, alkenyl, aralkyl, or C(O)R2 wherein R2 is lowe
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- Photochemistry of the Phthalimide System, 37. - Thiazacycloalkanols by Photocyclization of S-Substituted N-(Thioalkyl)phthalimides
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N-Substituted phthalimides (1,2) possessing a terminal thioether function in their side chain were irradiated with a high-pressure mercury lamp to give a variety of thiazacycloalkanol derivatives (3,7,9-13,16,17) with favored γ-, δ-, ε-, and ζ-hydrogen abstractions (Table 1), in moderate to fairly good yields.
- Sato, Yasuhiko,Nakai, Hideo,Wada, Masao,Mizoguchi, Tomishige,Hatanaka, Yasumaru,et al.
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p. 1099 - 1118
(2007/10/02)
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