- Quinazoline substituted 1, 2, 3-triazole derivative as well as pharmaceutical composition, preparation method and application thereof
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The invention discloses a quinazoline substituted 1, 2, 3-triazole derivative, the derivative is shown as a general formula (I), and the definition of each substituent group is shown in the specification. In addition, the invention also discloses a preparation method of the compound. The compound shown in the general formula (I) has an inhibiting effect on proliferation of tumor cells, also has an inhibiting effect on proliferation of human colon cancer (HCT-116) and human lung cancer cell strain (A549) cells, and can be used as an antitumor drug.
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Paragraph 0068-0072
(2022/03/31)
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- 1,2,3-Triazole analogs of combretastatin A-4 as potential microtubule-binding agents
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A series of cis-restricted 1,4- and 1,5-disubstituted 1,2,3-triazole analogs of combretastatin A-4 (1) have been prepared. Cytotoxicity and tubulin inhibition studies showed that 2-methoxy-5-((5-(3,4,5-trimethoxyphenyl)-1H-1,2, 3-triazol-1-yl)methyl)aniline (5e) and 2-methoxy-5-(1-(3,4,5-trimethoxybenzyl)- 1H-1,2,3-triazol-5-yl)aniline (6e) were two of the most active compounds. Molecular modeling studies revealed that the N-2 and N-3 atoms in the triazole rings in 5e and 6e did not form hydrogen bonds with the amino acids in the anticipated pharmacophore.
- Odlo, Kristin,Fournier-Dit-Chabert, Jérémie,Ducki, Sylvie,Gani, Osman A.B.S.M.,Sylte, Ingebrigt,Hansen, Trond Vidar
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scheme or table
p. 6874 - 6885
(2010/10/19)
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- 1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin
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A series of cis-restricted 1,5-disubstituted 1,2,3-triazole analogues of combretastatin A-4 (1) have been prepared. The triazole 12f, 2-methoxy-5-(1-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazol-5-yl)aniline, displayed potent cytotoxic activity against severa
- Odlo, Kristin,Hentzen, Jean,dit Chabert, Jeremie Fournier,Ducki, Sylvie,Gani, Osman A.B.S.M.,Sylte, Ingebrigt,Skrede, Martina,Florenes, Vivi Ann,Hansen, Trond Vidar
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p. 4829 - 4838
(2008/12/22)
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- Rapid synthesis of triazole-modified resveratrol analogues via click chemistry
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Resveratrol is a phytoalexin able to display an array of biological activities. We decided to replace the double bond with a triazole ring using the archetypical click reaction: the Huisgen [3 + 2] cycloaddition. Seventy-two triazole derivatives were synt
- Pagliai, Francesca,Pirali, Tracey,Del Grosso, Erika,Di Brisco, Riccardo,Tron, Gian Cesare,Sorba, Giovanni,Genazzani, Armando A.
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p. 467 - 470
(2007/10/03)
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