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Synthesis and Antitumor Activity of N-Phenyl-4-(Trifluoromethyl)-Quinazoline-2-Amine Derivatives
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Xing DAI1, 2, 3, Sha CHENG1, 2, Mingxiu CHEN1, 2, Jia YU1, 2, Heng LUO1, 2, Guangcan XU1, 2, *, Bixue XU1, 2, *
Chinese Pharmaceutical Journal | 2024, 59(15) : 1375 - 1383
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Chinese Pharmaceutical Journal | 2024, 59(15): 1375-1383
Synthesis and Antitumor Activity of N-Phenyl-4-(Trifluoromethyl)-Quinazoline-2-Amine Derivatives
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Xing DAI1, 2, 3, Sha CHENG1, 2, Mingxiu CHEN1, 2, Jia YU1, 2, Heng LUO1, 2, Guangcan XU1, 2, *, Bixue XU1, 2, *
Affiliations
  • 1 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China
  • 2 Natural Products Research Center of Guizhou Province, Guiyang 550014, China
  • 3 School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 561113, China
Published: 2024-08-08 doi: 10.11669/cpj.2024.15.003
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OBJECTIVE To find new arylaminoquinazoline-based antitumor target compounds with high efficacy and low toxicity. METHODS A series of N-phenyl-4-(trifluoromethyl)quinazoline-2-amine derivatives were synthesized starting from 2-nitrobenzaldehyde or 6-nitroveratraldehyde by a combination of nucleophilic addition, oxidation, reduction, cyclization, chlorination, and coupling reactions. The structures of the target compounds were characterized using NMR and MS. Their antitumor activities in vitro were then evaluated against four human cancer cell lines (PC3, LNCaP, K562, and HeLa) using MTT assay. The target prediction of active compound 8b was performed. RESULTS Compounds 8b and 8c exhibited promising anti-proliferative properties, particularly compound 8b, which exhibited excellent antitumor activity against PC3, LNCaP, and K562 with IC50 values of 5.51, 4.51 and 8.49 μmol·L-1, respectively. Molecular docking experiment demonstrated that PIM-1 is the potential target of 8b. CONCLUSION The piperazine ring containing compound 8b exhibits the strongest antitumor activity, which is worthy of further study.

arylaminoquinazoline  /  synthesis  /  antitumor activity  /  MTT assay  /  trifluoromethyl
Xing DAI, Sha CHENG, Mingxiu CHEN, Jia YU, Heng LUO, Guangcan XU, Bixue XU. Synthesis and Antitumor Activity of N-Phenyl-4-(Trifluoromethyl)-Quinazoline-2-Amine Derivatives[J]. Chinese Pharmaceutical Journal, 2024 , 59 (15) : 1375 -1383 . DOI: 10.11669/cpj.2024.15.003
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Year 2024 volume 59 Issue 15
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doi: 10.11669/cpj.2024.15.003
  • Receive Date：2023-10-16
  • Online Date：2026-01-14
  • Published：2024-08-08
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  • Received：2023-10-16
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Affiliations
    1 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China
    2 Natural Products Research Center of Guizhou Province, Guiyang 550014, China
    3 School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 561113, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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