62482-26-2Relevant articles and documents
Quinoline substituted chalcone compound as well as preparation method and application thereof
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Paragraph 0027; 0100; 0105, (2019/03/29)
The invention discloses a novel quinoline substituted chalcone compound as well as pharmaceutically acceptable salts and a preparation method thereof. The invention further discloses a pharmaceuticalcomposition which comprises a therapeutically effective amount of the novel quinoline substituted chalcone compound and/or the pharmaceutically acceptable salts and a pharmaceutically acceptable carrier. The invention further discloses a tubulin inhibitor which comprises the novel quinoline substituted chalcone compound and/or the pharmaceutically acceptable salts. The invention further disclosesapplication of the novel quinoline substituted chalcone compound and/or the pharmaceutically acceptable salts in preparing drugs for treating but not limited to colon cancer, leukemia, liver cancer, breast cancer and other diseases. The compound in the application shows excellent anti-tumor activity, and has more stable metabolic properties and better druggability prospect.
In silico, In Vitro and docking applications for some novel complexes derived from new quinoline derivatives
Ali, Ibrahim A.I.,El-Sakka, Sahar S.A.,Soliman, Mohamed H.A.,Mohamed, Omayma E.A.
, p. 8 - 32 (2019/06/27)
The new quinoline derivatives: 2-oxo-1,2-dihydroquinoline-4-carbohydrazide (1), 2-(allyloxy) quinoline-4-carbohydrizde (2), 1-allyl-2-oxo-1,2-dihydroquinoline-4-carbohydrazid (3) and 2-(allyl-thio)quinoline-4-carbohydrazide (4) and their Cu(II), Ni(II) and Co(II) complexes were synthesized and characterized by using elemental analysis (CHNM%), FTIR, UV/Vis, 1H NMR, 13C NMR spectra, DTA, TGA, magnetic susceptibility and the conductivity of 0.001 M in DMSO. The obtained results revealed the formation of the Cu(II) complexes in the square planar form, meanwhile Ni(II) and Co(II) complexes as octahedral structure. The FTIR spectra of the synthesized ligands and their complexes were giving the characteristic stretching vibration bands. The weight loss which appeared in the TG analysis indicates that there are different types of water molecules in the formed complexes. The theoretical calculations which are carried out using different computer programs permit proposing an optimized geometry for the formed complexes. The molecular modeling for the free ligands and their complexes were evaluated and discussed. The energy of the HOMO and LUMO was calculated and discussed. The most stable structure of the synthesized compounds was suggested and its energy was evaluated. The most benefit properties, which play a very important role in drug synthesis with reference to the surface properties of the compounds, were evaluated and discussed. The application of the DFT on the target compounds, gave dipole value around 1.73 D. This result turns out well with the requirement properties of the new drug. Docking the synthesized compounds with HepG2-code: 5EQG protein; e.g. liver carcinoma cell, gave a promising inhibition in Silico level. The antimicrobial activity of the target compounds with E. Coli, B. Subtils and Asp. Niger, in Vitro level, gave promising result. The interaction of the compounds with the microorganisms was tested in Silico level. E. Coli was used as an example for the target microorganism. The protein used for docking process was 5C9T.
A novel method for heterocyclic amide-thioamide transformations
Fathalla, Walid,Ali, Ibrahim A. I.,Pazdera, Pavel
supporting information, p. 174 - 181 (2017/02/15)
In this paper, we introduce a novel and convenient method for the transformation of heterocyclic amides into heteocyclic thioamides. A two-step approach was applied for this transformation: Firstly, we applied a chlorination of the heterocyclic amides to afford the corresponding chloroheterocycles. Secondly, the chloroherocycles and N-cyclohexyl dithiocarbamate cyclohexylammonium salt were heated in chloroform for 12 h at 61°C to afford heteocyclic thioamides in excellent yields.
STAT3 INHIBITOR CONTAINING QUINOLINECARBOXAMIDE DERIVATIVE AS ACTIVE INGREDIENT
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Page/Page column 61, (2011/06/24)
The present invention provides a STAT3 inhibitor containing as an active ingredient, a quinolinecarboxamide derivative represented by the formula (I) (in the formula, W represents a bond or an alkylene chain; X represents O, S, or NR34; and Rs
Synthesis of the pentacyclic core of lihouidine
Feldman, Ken S.,Coca, Adiel
, p. 2136 - 2138 (2008/09/19)
The pentacyclic base of the sponge-derived alkaloid lihouidine has been assembled from two quinoline fragments. The key step is a nitration-promoted cyclization to form the C-C bond between the two quinoline units.
Antiinflammation agents
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, (2008/06/13)
Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.
Antiviral thiazoles
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, (2008/06/13)
Compounds of formula (I) are active antiviral compounds useful in the treatment of viral infections in mammals. The compounds of the invention are readily prepared by reaction of a suitable 2-thiothiazole derivative with an appropriate Het-(CH2)n -halide.
