22666-84-8Relevant academic research and scientific papers
Application of novel pH sensitive isoniazid-heptamethine carbocyanine dye conjugates against prostate cancer cells
KONG, RUI-HENG,LI, YAN-FENG,WANG, DUN,WANG, YAN-JUN,YANG, XIAO-GUANG
, p. 412 - 416 (2020)
Recent studies have shown that monoamine oxidase A (MAOA) is significantly expressed in malignant prostate cancer (PCa) and plays an important role in tumorigenesis indicating its potential to serve as a target for PCa treatment. Here, we choose the small molecule isoniazid as the MAOA inhibition functionality and incorporated it in the tumor-targeting moiety of heptamethine carbocyanine dyes via a pH sensitive hydrazone bond to design and synthesize novel MAOA inhibitor isoniazid-heptamethine carbocyanine dye conjugates. Cytotoxicity assay in PC-3 cells shows that all conjugates possessed improved antitumor efficacy compared with isoniazid. The tested compounds also demonstrated a moderate MAOA inhibitory effect. In conclusion, these results indicate that these conjugates exert antitumor effects by delivering the MAOA-inhibiting moiety to PCa cells.
Isoniazide-heptamethine indocyanine coupling compound as well as preparation method and application thereof
-
Paragraph 0062; 0070-0072, (2020/05/11)
The invention belongs to the technical field of medicines. The invention relates to an isoniazide-heptamethine indocyanine coupling compound as well as preparation and application of the isoniazide-heptamethine indocyanine coupling compound. According to the invention, a splicing principle is adopted, isoniazidee is connected with a heptamethine indocyanine dye with excellent in-vivo fluorescenceimaging characteristic and tumor targeting function through hydrazone bonds; the novel tumor-targeting isoniazide-heptamethine indocyanine isoniazide coupling compound is designed and obtained, the structural formula of the compound is shown in the formulas (I)-(III), and R1, R2, R3, R4, m and n are shown in the claims and the specification. An in-vitro tumor cell growth inhibition test proves that the compound has a good inhibition effect on prostate tumor cells. A monoamine oxidase inhibitory activity test shows that the compound has a moderate inhibitory effect on monoamine oxidase A, and the inhibitory effect is obviously stronger than that of the isoniazide.
Synthesis of aromatic functionalized cage-rearranged silsesquioxanes (T8, T10, and T12) via nucleophilic substitution reactions
Chimjarn, Supansa,Kunthom, Rungthip,Chancharone, Prapassorn,Sodkhomkhum, Rapheepraew,Sangtrirutnugul, Preeyanuch,Ervithayasuporn, Vuthichai
supporting information, p. 916 - 919 (2015/02/19)
Organic-inorganic hybrid nano-building blocks of aromatic nitro-, aldehyde-, and bromo-functionalized polyhedral oligomeric silsesquioxanes were easily prepared through nucleophilic substitutions, starting from the reactions between octakis(3-chloropropyl)octasilsesquioxane and phenoxide derivatives. These phenoxide anions not only supply the substitution functions to a silsesquioxane cage, but can also induce a cage-rearrangement leading to the formation of octa-, deca-, and dodecahedral silsesquioxane cages. This journal is
Kinetics and mechanism of alkaline hydrolysis of Y-substituted phenyl phenyl carbonates
Kim, Song-I,Hwang, So-Jeong,Jung, Eun-Mi,Um, Ik-Hwan
experimental part, p. 2015 - 2018 (2010/12/19)
Second-order rate constants (kOH-) have been measured spectrophotometrically for alkaline hydrolysis of Y-substituted phenyl phenyl carbonates (2a-j) and compared with the kOH- values reported previously for the corresponding reactions of Y-substituted phenyl benzoates (1a-j). Carbonates 2a-j are 8 ～ 16 times more reactive than benzoates 1a-j. The Hammett plots correlated with σ- and σo constants exhibit many scattered points, while the Yukawa-Tsuno plot results in excellent linear correlation with ρ = 1.21 and r = 0.33. Thus, the reaction has been concluded to proceed through a concerted mechanism in which expulsion of the leaving group is advanced only a little. However, one cannot exclude a possibility that the current reaction proceeds through a forced concerted mechanism with a highly unstable intermediate.
Fused pyridine derivatives
-
Example 198, (2010/01/30)
The present provides a condensed pyridine compound (I) represented by the following formula: (wherein, R2represents ring A represents benzene ring, pyridine ring, thiophene ring or furan ring; and B represents its pharmaceutically acceptable salt or hydrates thereof, which is a clinically useful medicament having a serotonin antagonism, in particular, that for treating, ameliorating or preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
Process for the isolation of p-hydroxybenzaldehyde
-
, (2008/06/13)
The invention relates to a process for the isolation of p-hydroxybenzaldehyde from the reaction mixture obtained by oxidizing p-cresol with oxygen or oxygen-containing gases in methanol in the presence of Na or K hydroxide and an Mn, Ni, Cr or Co salt. The procedure in this process is optionally to add water to the reaction mixture, to heat the resulting solution and to filter off the precipitated Mn, Ni, Cr or Co oxide-hydrate, to remove the methanol from the filtrate by distillation, to cool the residual aqueous solution and thus to allow the p-hydroxybenzaldehyde to crystallize out in the form of the Na or K salt. Alternatively, the reaction mixture is first dried by atomization, the soluble constituents of the dry substance are then dissolved in hot water, the undissolved Mn, Ni, Cr or Co oxide-hydrate is filtered off and the salt of p-hydroxybenzaldehyde is again allowed to crystallize out by cooling the filtrate. A further method consists in diluting the reaction mixture with methanol, filtering off the undissolved Mn, Ni, Cr or Co oxide-hydrate, drying the filtrate by atomization, dissolving the resulting dry substance in hot water, and again allowing the p-hydroxybenzaldehyde to crystallize out as the Na or K salt by cooling the solution.
