85862-79-9Relevant academic research and scientific papers
Quinazoline substituted 1, 2, 3-triazole derivative as well as pharmaceutical composition, preparation method and application thereof
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Paragraph 0068-0072, (2022/03/31)
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.
Phosphino-Triazole Ligands for Palladium-Catalyzed Cross-Coupling
Zhao, Yiming,Van Nguyen, Huy,Male, Louise,Craven, Philip,Buckley, Benjamin R.,Fossey, John S.
supporting information, p. 4224 - 4241 (2018/10/25)
Twelve 1,5-disubtituted and fourteen 5-substituted 1,2,3-triazole derivatives bearing diaryl or dialkyl phosphines at the 5-position were synthesized and used as ligands for palladium-catalyzed Suzuki-Miyaura cross-coupling reactions. Bulky substrates wer
In vitro antiplasmodial efficacy of synthetic coumarin-triazole analogs
Yadav, Neesha,Agarwal, Drishti,Kumar, Satyanand,Dixit,Gupta, Rinkoo D.,Awasthi, Satish K.
, p. 735 - 745 (2018/02/06)
Twenty two diverse coumarin-triazole derivatives were synthesized by alkylation of 7-hydroxy-4-methyl-coumarin followed by click chemistry at 7-position. These compounds were evaluated for their in vitro antiplasmodial activity against chloroquine sensitive strain of Plasmodium falciparum (3D7). Compound 9 (7-[1-(2, 4-dimethoxy-phenyl)-1H- [1–3] triazol-4-ylmethoxy]-4-methyl-chromen-2-one) was found most active with IC50 value 0.763 ± 0.0124 μg/mL. Further, the structure of compound 20 was characterized by single crystal X-ray diffraction. In view of impressive results, we considered it worthwhile to validate the results of in vitro antiplasmodial activity by assessing whether these compounds are capable of hampering the catalytic activity of DNA gyrase, thus preventing its supercoiling function.
BROAD SPECTRUM ANTIVIRAL COMPOUNDS AND USES THEREOF
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Paragraph 0455; 0466, (2017/03/21)
Disclosed herein, inter alia, are agents having antiviral activity and methods of use thereof.
1,2,3-triazoles as amide bioisosteres: Discovery of a new class of potent HIV-1 Vif antagonists
Mohammed, Idrees,Kummetha, Indrasena Reddy,Singh, Gatikrushna,Sharova, Natalia,Lichinchi, Gianluigi,Dang, Jason,Stevenson, Mario,Rana, Tariq M.
, p. 7677 - 7682 (2016/09/04)
RN-18 based viral infectivity factor (Vif), Vif antagonists reduce viral infectivity by rescuing APOBEC3G (A3G) expression and enhancing A3G-dependent Vif degradation. Replacement of amide functionality in RN-18 (IC50 = 6 μM) by isosteric heterocycles resulted in the discovery of a 1,2,3-trizole, Id (IC50 = 1.2 μM). We identified several potent HIV-1 inhibitors from a Id based library including 5ax (IC50 = 0.01 μM), 5bx (0.2 μM), 2ey (0.4 μM), 5ey (0.6 μM), and 6bx (0.2 μ M).
Synthesis of bioactive 1-alkyl-1H-naphtho[2,3-d][1,2,3]triazole-4,9-diones and N-aryl-2-aminomethylene-1,3-indanediones using water as the solvent
Zhang, Qian,Shrestha, Jaya P.,Chang, Cheng-Wei Tom
supporting information, p. 1839 - 1842 (2014/03/21)
Through a [2+3] cycloaddition reaction, a new environmentally friendly method was developed to enable the synthesis of bioactive 1-alkyl-1H-naphtho[2, 3-d][1,2,3]triazole-4,9-diones and N-aryl-2-aminomethylene-1,3-indanediones using water as the solvent w
Synthesis and anticancer structure activity relationship investigation of cationic anthraquinone analogs
Shrestha, Jaya P.,Fosso, Marina Y.,Bearss, Jeremiah,Chang, Cheng-Wei Tom
, p. 96 - 102 (2014/04/03)
We have synthesized a series of novel 4,9-dioxo-4,9-dihydro-1H-naphtho[2,3- d][1,2,3]triazol-3-ium salts, which can be viewed as analogs of cationic anthraquinones. Unlike the similar analogs that we have reported previously, these compounds show relative
Parallel synthesis of "Click" chalcones as antitubulin agents
Utsintong, Maleeruk,Massarotti, Alberto,Caldarelli, Antonio,Theeramunkong, Sewan
, p. 510 - 516 (2013/07/28)
It has been shown that some chalcones are able to inhibit tubulin polymerization, giving cytotoxicity and destruction of tumoral vasculature. A library of 180 novel chalcone analogs has been synthesized via click chemistry and screened for their cytotoxic
Rapid synthesis of triazole-modified resveratrol analogues via click chemistry
Pagliai, Francesca,Pirali, Tracey,Del Grosso, Erika,Di Brisco, Riccardo,Tron, Gian Cesare,Sorba, Giovanni,Genazzani, Armando A.
, p. 467 - 470 (2007/10/03)
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
