2,3-位四氢-β-咔啉并二酮哌嗪类化合物合成及抗肿瘤活性研究

doi:10.6023/cjoc202603026

有机化学 ›› 2026, Vol. 46 ›› Issue (8): 3089-3103.DOI: 10.6023/cjoc202603026 上一篇下一篇

研究论文

2,3-位四氢-β-咔啉并二酮哌嗪类化合物合成及抗肿瘤活性研究

杨苗^a, 赵银九^a, 龚燕川^b, 张洁^a^,^*(), 郭亮^a^,^*()

^a 石河子大学化学化工学院化工绿色过程兵团重点实验室新疆石河子 832003
^b 新疆华世丹药物研究有限责任公司乌鲁木齐 830011

收稿日期:2026-03-19 修回日期:2026-04-20 发布日期:2026-06-03
通讯作者: 张洁, 郭亮
基金资助:
兵团指导计划(2022ZD019); 兵团指导计划(2023ZD073); 兵团科技攻关(2023AB047); 新疆科技重大专项(2024A03004-4); 兵团面上项目(2025DA061); 新疆青年科学基金(2024D01B23)

Synthesis and Antitumor Activity Study of 2,3-Substituted Tetrahydro- β-carboline Fused Diketopiperazine Derivatives

Miao Yang^a, Yinjiu Zhao^a, Yanchuan Gong^b, Jie Zhang^a^,^*(), Liang Guo^a^,^*()

^a Key Laboratory for Green Processing of Chemical Engineering of Xinjiang Bingtuan, School of Chemistry and Chemical Engineering, Shihezi University, Shihezi, Xinjiang 832003
^b Xinjiang Huashidan Pharmaceutical Research Co. Ltd., Urumqi 830011

Received:2026-03-19 Revised:2026-04-20 Published:2026-06-03
Contact: Jie Zhang, Liang Guo
Supported by:
Corps Guidance Plan(2022ZD019); Corps Guidance Plan(2023ZD073); Corps Science and Technology Breakthrough(2023AB047); Xinjiang Major Science and Technology Projects(2024A03004-4); Corps General Projectst(2025DA061); Xinjiang Youth Science Foundation(2024D01B23)

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摘要/Abstract

利用药物拼合原理合成了30个含不同取代基的四氢-β-咔啉并二酮哌嗪类衍生物. 采用噻唑蓝(MTT)法测试了目标化合物对三种肿瘤细胞株(LLC、A-549、NCI-H1666)增殖的抑制活性. 结果显示, 大多数化合物对这三种肿瘤细胞株表现出中等至良好的抑制活性, 且多数化合物的IC₅₀值低于20 μmmol/L. 其中, 所得目标化合物对A549细胞系表现出良好的抑制活性, 特别是(S)-2,7-双(4-氟苄基)-1,2,3,6,7,12-六氢吡嗪-4H-并[1,2-a]四氢-β-咔啉-1,4-二酮(6o)和(S)-7-(4-氟苄基)-2-己基-1,2,3,6,7,12-六氢-4H-吡嗪并[1,2-a]四氢-β-咔啉-1,4-二酮(6y)对A549细胞表现出优异的抑制活性, 且IC₅₀值均低于10 μmmol/L. 整体来说, 化合物6o、(S)-2-(4-氟苄基)-7-(4-三氟甲基苄基)-1,2,3,6,7,12-六氢- 4H-吡嗪并[1,2-a]四氢-β-咔啉-1,4-二酮(6p)、化合物6y和(S)-2-己基-7-(4-三氟甲基苄基)-1,2,3,6,7,12-六氢-4H-吡嗪并[1,2-a]四氢-β-咔啉-1,4-二酮(6z)对LLC、A549和NCI-H1666细胞系表现出良好的抑制活性, 且IC₅₀值均低于20 μmmol/L, 具有潜在的抗肿瘤研究价值. 分子对接结果表明, 化合物6o和6p与血管内皮生长因子受体2 (VEGFR-2) (PDB:4AGD)的多个氨基酸残基之间存在良好的相互作用. 同时, 分子动力学模拟结果表明, 化合物6p与4AGD之间能保持二者的结合稳定性和构象一致性.

关键词: 四氢-β-咔啉, 二酮哌嗪, 抗肿瘤, 分子对接, 分子动力学模拟

A series of 30 tetrahydro-β-carboline fused diketopiperazine derivatives containing different substituents were synthesized using the principle of drug combination. Their antiproliferative activities were evaluated against three tumor cell lines (LLC, A-549, NCI-H1666) via methyl thiazolyl tetrazolium (MTT) assay. The results showed that most compounds exhibited moderate to good inhibitory activity against these three tumor cell lines, and the IC₅₀ values of most compounds were below 20 μmol/L. Among them, the target compounds showed good inhibitory activity against A549 cell line, especially (S)-2,7-bis(4-fluorobenzyl)-1,2,3,6,7,12-hexahydropyrazine-4)-perhydro-β-carboline-1,4-dione (6o) and (S)-7-(4-fluorobenzyl)- 2-hexyl-1,2,3,6,7,12-hexahydro-4H-pyrazino[1,2-a]tetrahydro-β-carboline-1,4-dione (6y) showed excellent inhibitory activity against A549 cell line, with IC₅₀ values below 10 μmol/L. Overall, compound 6o, (S)-2-(4-fluorobenzyl)-7-(4-trifluoromethyl- benzyl)-1,2,3,6,7,12-hexahydro-4H-pyrazino[1,2-a]tetrahydro-β-carboline-1,4-dione (6p), 6y, and (S)-2-hexyl-7-(4-trifluoro- methylbenzyl)-1,2,3,6,7,12-hexahydro- 4H-pyrazino[1,2-a]tetrahydro-β-carboline-1,4-dione (6z) exhibit good inhibitory activity against LLC, A549, and NCI-H1666 cell lines, with IC₅₀ values all below 20 μmol/L, indicating potential anti-tumor research value. The molecular docking results indicate that compounds 6o and 6p have good interactions with multiple amino acid residues of VEGFR-2 (PDB:4AGD). Meanwhile, the molecular dynamics simulation results indicate that the binding stability and conformational consistency between compound 6p and 4AGD can be maintained.

Key words: tetrahydro-β-carboline, diketopiperazine, antitumor, molecular docking, molecular dynamics simulation

引用此文

杨苗, 赵银九, 龚燕川, 张洁, 郭亮. 2,3-位四氢-β-咔啉并二酮哌嗪类化合物合成及抗肿瘤活性研究[J]. 有机化学, 2026, 46(8): 3089-3103.

Miao Yang, Yinjiu Zhao, Yanchuan Gong, Jie Zhang, Liang Guo. Synthesis and Antitumor Activity Study of 2,3-Substituted Tetrahydro- β-carboline Fused Diketopiperazine Derivatives[J]. Chinese Journal of Organic Chemistry, 2026, 46(8): 3089-3103.

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图/表 12

图1. 靶向VEGFR-2的抗肿瘤药物

Figure 1. Antitumor drugs targeting VEGFR-2

图2. 含二酮哌嗪支架的药物

Figure 2. Drugs containing diketopiperazine scaffold

图式1. 本文目标化合物的设计思路

Scheme 1. Design concept of the target compounds in this article

图式2. 化合物5a~5e和6b~6z的合成路线

Scheme 2. Synthetic route of compounds 5a~5e and 6b~6z Reagents and conditions: (i) H2O, NaOH, HCHO, 120 ℃, reflux, yield 89%; (ii) C2H5OH, SOCl2, 85 ℃, reflux, yield 92%; (iii) THF, C2H2Cl2O, DIPEA, stirred at r.t., yield 96%; (iv) THF, RNH2, DIPEA, stirred at r.t.; (v) DMF, NaH, alkyl halogenide, stirred at 0 ℃~r.t.

Compd.	(IC₅₀±SD)^a/(μmol•L^－1)
Compd.	LLC	A549	NCI-H1666
5a	>50	>50	>50
5b	>50	>50	>50
5c	21.5±0.9	16.8±0.7	21.8±0.8
5d	>50	>50	15.4±2.3
5e	>50	24.7±1.1	32.3±1.3
Cisplatin	5.4±0.7	17.8±0.5	8.6±0.3

表1. 化合物5a~5e对3种癌细胞系的体外抗肿瘤活性

Table 1. In vitro anti-tumor activity of compounds 5a~5e against three cancer cell lines

Compd.	(IC₅₀±SD)^a/(μmol•L^－1)
Compd.	LLC	A549	NCI-H1666
6b	>50	>50	>50
6c	23.6±0.6	21.3±0.5	17.2±0.2
6d	18.7±0.3	>50	>50
6e	21.2±0.4	15.2±0.6	19.8±07
6f	29.2±0.3	12.9±0.5	15.6±0.7
6g	>50	>50	>50
6h	47.0±0.3	>50	>50
6i	>50	>50	16.4±1.5
6j	22.2±0.5	36.2±0.3	44.4±0.6
6k	24.7±0.3	17.5±0.5	13.8±0.2
6l	>50	34.8±0.4	14.0±0.1
6m	12.4±0.3	23.3±0.2	11.4±0.4
6n	13.7±0.4	28.2±1.3	12.9±1.1
6o	12.1±0.6	8.4±0.3	17.2±1.7
6p	7.9±0.6	13.4±1.4	14.2±0.6
6q	>50	>50	>50
6r	30.7±0.6	27.4±1.3	17.1±2.6
6s	17.4±0.5	9.9±0.1	15.8±1.3
6t	9.7±0.9	18.9±1.4	12.3±0.3
6u	14.4±0.3	13.5±0.6	18.6±1.6
6v	>50	39.3±0.9	23.0±1.1
6w	>50	34.3±0.3	18.3±0.5
6x	>50	25.4±0.7	16.0±0.4
6y	12.8±0.6	5.2±0.1	11.6±0.3
6z	13.4±0.4	13.3±0.7	14.7±0.7
Cispyatin	5.4±0.7	17.8±0.5	8.6±0.3

表2. 化合物6b~6z对3种癌细胞系的体外抗肿瘤活性

Table 2. In vitro anti-tumor activity of compounds 6b~6z against three cancer cell lines

图3. 舒尼替尼与VEGFR-2 (PDB:4AGD)的分子对接研究

Figure 3. Molecular docking study of sunitinib with VEGFR-2 (PDB:4AGD)

图4. 化合物6o与VEGFR-2 (PDB:4AGD)的分子对接研究

Figure 4. Molecular docking studies of compound 6o with VEGFR-2 (PDB:4AGD)

图5. 化合物6p与VEGFR-2 (PDB:4AGD)的分子对接研究

Figure 5. Molecular docking studies of compound 6p and VEGFR-2 (PDB:4AGD)

Compd.	Protein	Hydrophobic interaction	Hydrogen bond	π-Cation interaction
Sunitinib	4AGD	ASP-46、VAL-80、ALA-98、GLU-117、ILE-121、 VAL-131、VAL-148、ASP-228	LYS-100、 GLU-117	LYS-100
6o	4AGD	GLU-117、LEU-121、ILE-121、VAL-130、LEU-201、 ASP-210、ILE-226、LEU-231	ARG-209
6p	4AGD	ALA-113、LEU-121、ILE-124、LEU-201、ASP-210、LEU-231	GLU-110	HIS-208

表3. 舒尼替尼、化合物6o和6p与4AGD分子对接模式异同表

Table 3. Comparison of molecular docking modes of sunitinib, compounds 6o and 6p with 4AGD

图6. 化合物6p的(a)氢键图、(b)残基均方根波动(RMSF)图、(c)均方根偏差(RMSD)图及(d)回转半径(Rg)图

Figure 6. (a) Hydrogen bond diagram, (b) root mean square fluctuation (RMSF) diagram, (c) root mean square deviation (RMSD) diagram, and (d) radius of gyration (Rg) diagram of compound 6p

图7. 化合物6p的(a)二维和(b)三维自由能地貌图

Figure 7. (a) 2D and (b) 3D free energy landscapes of compound 6p

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2,3-位四氢-β-咔啉并二酮哌嗪类化合物合成及抗肿瘤活性研究

Synthesis and Antitumor Activity Study of 2,3-Substituted Tetrahydro- β-carboline Fused Diketopiperazine Derivatives

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