Home Journals Articles Updates About
CN
image
收藏切换
Design, synthesis and antitumor activity of vanillin derivatives
收藏切换
Ya BAO1, 2, 3, Min-ru JIAO2, 3, Jian-qi LI2, 3, Qing-wei ZHANG2, 3
Chinese Journal of New Drugs | 2021, 30(11) : 1017 - 1021
Less
收藏切换
Chinese Journal of New Drugs | 2021, 30(11): 1017-1021
Design, synthesis and antitumor activity of vanillin derivatives
Full
Ya BAO1, 2, 3, Min-ru JIAO2, 3, Jian-qi LI2, 3, Qing-wei ZHANG2, 3
Affiliations
  • 1School of Chemical Engineering, Shanghai University of Engineering and Technology, Shanghai 201620, China
  • 2Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai 201203, China
  • 3Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai 201203, China
Published: 2021-06-15
Outline
收藏切换
Objective:

To design and synthesize novel vanillin derivatives and evaluate their anti-proliferation effect against HeLa cells.

Methods:

Taking vanillin derivative SBE-13 as lead, 2-chloroquinoline fragment were introduced into the new compounds by the methods of electronic isosteric and skeleton transition. 2-Chloro-3-chloromethylquinoline and vanillin were used as raw materials to obtain the target compounds 4a~4k by etherification and reductive amination.

Results:

A total of 11 novel vanillin derivatives were designed and synthesized, and their structures were confirmed by 1H NMR and ESI-MS. Most of the compounds exhibited good antiproliferative activities against HeLa cells. Notably, compound 4b potently inhibited HeLa cells with an IC50=9.79 μmol·L-1, a 10-fold improvement over SBE-13 (IC50=78.30 μmol·L-1).

Conclusion:

Compound 4b displayed significant antiproliferative effect in vitro, which is worthy of further study.

vanillin  /  derivatives  /  antitumor  /  synthesis
包亚, 焦民茹, 李建其, 张庆伟. 香兰素衍生物的设计、合成及抗肿瘤活性. 中国新药杂志, 2021 , 30 (11) : 1017 -1021 .
Ya BAO, Min-ru JIAO, Jian-qi LI, Qing-wei ZHANG. Design, synthesis and antitumor activity of vanillin derivatives[J]. Chinese Journal of New Drugs, 2021 , 30 (11) : 1017 -1021 .
Appendix
Less
Year 2021 volume 30 Issue 11
35
8
Cite this Article
BibTeX
Article Info
  • Online Date：2026-10-28
  • Published：2021-06-15
Article Data
Affiliations
History
  • Accepted：2020-07-07
Funding
Affiliations
    1School of Chemical Engineering, Shanghai University of Engineering and Technology, Shanghai 201620, China
    2Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai 201203, China
    3Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai 201203, China
References
Share
https://castjournals.cast.org.cn/joweb/zgxyzz/EN/
Share to
QR

Scan QR to access full text

Cite this article
BibTeX
Citations
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
关闭全屏
  • BibTeX
  • EndNote
  • RefWorks
  • TxT
Links
Articles
Latest Articles
Most Read
Collections
Updates
Events
News
Multimedia
About
About Us
Contact
No. 86 Xueyuan South Road, Haidian District, Beijing
100081
010-62662699(Operation and Technical Support)
qkjq@cast.org.cn

Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House