- 2,3-dihydro-1H-quinoline-4-ketone thiosemicarbazone derivatives as well as preparation method and application thereof
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The invention discloses 2,3-dihydro-1H-quinoline-4-ketone thiosemicarbazone derivatives as well as a preparation method and application thereof. The structural formula of the derivatives is as shown in a formula (I): (the formula is as shown in the description), wherein R1 is halogen, alkyl or alkoxy; R2 is hydrogen, halogen or alkoxy; R3 is hydrogen or halogen; R4 is hydrogen or halogen; X is hydrogen, acetyl or nitryl; and Y is hydrogen or phenyl. The derivatives can obviously inhibit proliferation of tumor cells, and has significant inhibition effect on multiple cancer cell strains such asbreast cancer cells, melanoma cells and prostatic cancer cells; and the anti-tumor activity is obviously better than that of a broad-spectrum anti-cancer medicine cis-platinum. In addition, the preparation process of the derivatives is simple, the conditions are mild, the sources of the raw materials are rich, the production cost is low, and potential medicinal value and good application prospectin the aspect of preparing a novel anti-tumor medicine are achieved.
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Paragraph 0076-0079; 0137-0140
(2019/04/04)
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- Quinolinoneacetic acid derivatives as novel glutathione S-transferase P1-1 inhibitors: Insights into the interaction modes by molecular modeling
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Glutathione S-transferase P1-1 (GSTP1-1, EC 2.5.1.18) is generally conceived to be an important player in the acquired resistance of tumor to anticancer agents, thus a series of quinolinoneacetic acid derivatives were synthesized and their inhibitory effe
- Wang, Jian,Wang, Shao-Jie,Song, Dan-Dan,Jing, Yong-Kui,Cheng, Mao-Sheng
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p. 2823 - 2826
(2012/10/30)
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- Process for the preparation of 4-quinolinones
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1,2,3,4-Tetrahydro-4-quinolinones of the formula STR1 are prepared from a 3-anilinopropionic acid of general for formula STR2 which is treated successively with phosgene, with a base or by heating, and then with a Lewis acid or a strong acid. In the formulae (I) and (II), R denotes a hydrogen atom, a halogen atom, an alkyl radical (1 to 4 carbon atoms) or an alkoxy radical (1 to 4 carbon atoms), and R1 denotes a hydrogen atom or any alkyl radical (1 to 4 carbon atoms). The compounds of formula I are useful as intermediates in the production of known drugs.
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- Process for the preparation of 4-quinolinones
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1,2,3,4-Tetrahydro-4-quinolinone of formula: STR1 are prepared from a 3-anilinopropionic acid of formula: STR2 which is treated successively with phosgene, phosgene in the presence of dimethylformamide, a Lewis acid or a strong acid, and a base. In the fo
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