Article(id=1322246436876571277, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, articleNumber=null, orderNo=null, doi=null, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=null, receivedDateStr=null, revisedDate=null, revisedDateStr=null, acceptedDate=1594051200000, acceptedDateStr=2020-07-07, onlineDate=1793177716702, onlineDateStr=2026-10-28, pubDate=1623686400000, pubDateStr=2021-06-15, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1793177716702, onlineIssueDateStr=2026-10-28, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1793177716702, creator=13701087609, updateTime=1793177716702, updator=13701087609, issue=Issue{id=1322246381633389353, tenantId=1146029695717560320, journalId=1235980733773295621, year='2021', volume='30', issue='11', pageStart='961', pageEnd='1056', issueExtLink='null', onlineDate='null', pubDate='1623686400000', pubDateStr='2021-06-15', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1793177703531, creator='13701087609', updateTime=1793178125547, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1322248152208486593, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1322248152212680898, tenantId=1146029695717560320, journalId=1235980733773295621, issueId=1322246381633389353, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=1017, endPage=1021, ext={EN=ArticleExt(id=1322246437077897870, articleId=1322246436876571277, tenantId=1146029695717560320, journalId=1235980733773295621, language=EN, title=Design, synthesis and antitumor activity of vanillin derivatives, columnId=null, journalTitle=Chinese Journal of New Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=
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.

, authors=Ya BAO1, 2, 3, Min-ru JIAO2, 3, Jian-qi LI2, 3, Qing-wei ZHANG2, 3, authorsList=Ya BAO, Min-ru JIAO, Jian-qi LI, Qing-wei ZHANG, authorCompany=null, correspAuthors=Qing-wei ZHANG, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1322246437337944719, articleId=1322246436876571277, tenantId=1146029695717560320, journalId=1235980733773295621, language=CN, title=香兰素衍生物的设计、合成及抗肿瘤活性, columnId=1236330556003242277, journalTitle=中国新药杂志, columnName=实验研究, runingTitle=null, highlight=null, articleAbstract=
目的:

设计合成系列香兰素衍生物,并测试化合物体外抗HeLa细胞(人宫颈癌细胞)增殖活性。

方法:

以香草素衍生物SBE-13为先导,采用电子等排、骨架迁越等方法引入2-氯喹啉片段设计新结构类型化合物。以2-氯-3-氯甲基喹啉与香兰素为原料,经醚化、还原胺化合成目标化合物4a~4k。

结果:

共合成11个未见文献报道的香兰素衍生物,结构经1H-NMR和MS确证,体外抗HeLa细胞增殖活性实验显示大部分化合物具有较好的抗肿瘤细胞增殖活性,其中化合物4b的活性相比SBE-13提高10倍。

结论:

香兰素衍生物4b具有较好的抗HeLa细胞增殖活性,值得进一步深入研究。

, authors=包亚1, 2, 3, 焦民茹2, 3, 李建其2, 3, 张庆伟2, 3, authorsList=包亚, 焦民茹, 李建其, 张庆伟, authorCompany=null, correspAuthors=张庆伟, authorNote=

包亚,女,硕士研究生,主要从事抗肿瘤新化合物设计与合成研究。联系电话:(021)20572000-5060,E-mail:。

, correspAuthorsNote=
张庆伟,男,副研究员,主要从事抗肿瘤、中枢神经新药设计与合成研究。联系电话:(021)20572000-5061,E-mail:。
, copyrightStatement=null, copyrightOwner=《中国新药杂志》有限公司, extLink=null, articleAbsUrl=null, sourceXml=aC4lrwJb6x/yFlvgQqgQUw==, magXml=UDitkTCnjz/6H2eXY44M3g==, pdfUrl=null, pdf=qlEu1gDbU/79r0RNILFRQQ==, pdfFileSize=820231, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=gAMmXKG2PJsaZFmYq3jm/A==, mapNumber=null, fund=null)}, authors=[Author(id=1322246437811901082, tenantId=1146029695717560320, journalId=1235980733773295621, articleId=1322246436876571277, orderNo=0, firstName=null, middleName=null, lastName=null, nameCn=null, orcid=null, stid=null, country=null, authorPic=null, dead=0, email=baoyaar@163.com, emailSecond=null, emailThird=null, correspondingAuthor=0, authorType=1, ext={EN=AuthorExt(id=1322246437967090334, tenantId=1146029695717560320, journalId=1235980733773295621, articleId=1322246436876571277, authorId=1322246437811901082, language=EN, stringName=Ya BAO, firstName=Ya, middleName=null, lastName=BAO, prefix=null, suffix=null, authorComment=null, nameInitials=null, affiliation=null, department=null, xref=1, 2, 3, address=1School of Chemical Engineering, Shanghai University of Engineering and Technology, Shanghai 201620, China
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包亚,女,硕士研究生,主要从事抗肿瘤新化合物设计与合成研究。联系电话:(021)20572000-5060,E-mail:。

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包亚,女,硕士研究生,主要从事抗肿瘤新化合物设计与合成研究。联系电话:(021)20572000-5060,E-mail:。

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香兰素衍生物的设计、合成及抗肿瘤活性
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包亚 1, 2, 3 , 焦民茹 2, 3 , 李建其 2, 3 , 张庆伟 2, 3
中国新药杂志 | 实验研究 2021,30(11): 1017-1021
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中国新药杂志 |实验研究 2021 , 30 (11) : 1017 -1021
香兰素衍生物的设计、合成及抗肿瘤活性
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包亚,女,硕士研究生,主要从事抗肿瘤新化合物设计与合成研究。联系电话:(021)20572000-5060,E-mail:。

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包亚1, 2, 3 , 焦民茹2, 3, 李建其2, 3, 张庆伟2, 3
作者信息
  • 1上海工程技术大学化学化工学院,上海 201620
  • 2中国医药工业研究总院上海医药工业研究院化学制药新技术中心,上海 201203
  • 3上海药物合成工艺过程工程技术研究中心,上海 201203
通讯作者:
张庆伟,男,副研究员,主要从事抗肿瘤、中枢神经新药设计与合成研究。联系电话:(021)20572000-5061,E-mail:。
作者简介:

包亚,女,硕士研究生,主要从事抗肿瘤新化合物设计与合成研究。联系电话:(021)20572000-5060,E-mail:。

Design, synthesis and antitumor activity of vanillin derivatives
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
出版时间: 2021-06-15
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目的:

设计合成系列香兰素衍生物,并测试化合物体外抗HeLa细胞(人宫颈癌细胞)增殖活性。

方法:

以香草素衍生物SBE-13为先导,采用电子等排、骨架迁越等方法引入2-氯喹啉片段设计新结构类型化合物。以2-氯-3-氯甲基喹啉与香兰素为原料,经醚化、还原胺化合成目标化合物4a~4k。

结果:

共合成11个未见文献报道的香兰素衍生物,结构经1H-NMR和MS确证,体外抗HeLa细胞增殖活性实验显示大部分化合物具有较好的抗肿瘤细胞增殖活性,其中化合物4b的活性相比SBE-13提高10倍。

结论:

香兰素衍生物4b具有较好的抗HeLa细胞增殖活性,值得进一步深入研究。

香兰素  /  衍生物  /  抗肿瘤  /  合成
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 .
  • 上海市科技创新行动计划资助项目(17431903900)
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2021年第30卷第11期
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  • 首发时间:2026-10-28
  • 出版时间:2021-06-15
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  • 录用日期:2020-07-07
基金
上海市科技创新行动计划资助项目(17431903900)
作者信息
    1上海工程技术大学化学化工学院,上海 201620
    2中国医药工业研究总院上海医药工业研究院化学制药新技术中心,上海 201203
    3上海药物合成工艺过程工程技术研究中心,上海 201203

通讯作者:

张庆伟,男,副研究员,主要从事抗肿瘤、中枢神经新药设计与合成研究。联系电话:(021)20572000-5061,E-mail:。
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2种不同金属材料的力学参数
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属
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种数
Number of
species
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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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