Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety

We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed...
Ausführliche Beschreibung

Gespeichert in:

Autor*in:	Jun Zhang [verfasserIn] Weiyi Shen [verfasserIn] Xiaoning Li [verfasserIn] Yun Chai [verfasserIn] Senjun Li [verfasserIn] Kai Lv [verfasserIn] Huiyuan Guo [verfasserIn] Mingliang Liu [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2016

Schlagwörter:	5-bromo-7-azaindolin-2-ones synthesis antitumor activity

Übergeordnetes Werk:	In: Molecules - MDPI AG, 2003, 21(2016), 12, p 1674
Übergeordnetes Werk:	volume:21 ; year:2016 ; number:12, p 1674

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.3390/molecules21121674

Katalog-ID:	DOAJ002654369

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spelling	10.3390/molecules21121674 doi (DE-627)DOAJ002654369 (DE-599)DOAJa25ad3bf80f64e1fb87be593cb8a6848 DE-627 ger DE-627 rakwb eng QD241-441 Jun Zhang verfasserin aut Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety 2016 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC50: 2.357–3.012 μM) was found more potent than Sunitinib (IC50: 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively. 5-bromo-7-azaindolin-2-ones synthesis antitumor activity Organic chemistry Weiyi Shen verfasserin aut Xiaoning Li verfasserin aut Yun Chai verfasserin aut Senjun Li verfasserin aut Kai Lv verfasserin aut Huiyuan Guo verfasserin aut Mingliang Liu verfasserin aut In Molecules MDPI AG, 2003 21(2016), 12, p 1674 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:21 year:2016 number:12, p 1674 https://doi.org/10.3390/molecules21121674 kostenfrei https://doaj.org/article/a25ad3bf80f64e1fb87be593cb8a6848 kostenfrei http://www.mdpi.com/1420-3049/21/12/1674 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 21 2016 12, p 1674
allfields_unstemmed	10.3390/molecules21121674 doi (DE-627)DOAJ002654369 (DE-599)DOAJa25ad3bf80f64e1fb87be593cb8a6848 DE-627 ger DE-627 rakwb eng QD241-441 Jun Zhang verfasserin aut Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety 2016 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC50: 2.357–3.012 μM) was found more potent than Sunitinib (IC50: 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively. 5-bromo-7-azaindolin-2-ones synthesis antitumor activity Organic chemistry Weiyi Shen verfasserin aut Xiaoning Li verfasserin aut Yun Chai verfasserin aut Senjun Li verfasserin aut Kai Lv verfasserin aut Huiyuan Guo verfasserin aut Mingliang Liu verfasserin aut In Molecules MDPI AG, 2003 21(2016), 12, p 1674 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:21 year:2016 number:12, p 1674 https://doi.org/10.3390/molecules21121674 kostenfrei https://doaj.org/article/a25ad3bf80f64e1fb87be593cb8a6848 kostenfrei http://www.mdpi.com/1420-3049/21/12/1674 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 21 2016 12, p 1674
allfieldsGer	10.3390/molecules21121674 doi (DE-627)DOAJ002654369 (DE-599)DOAJa25ad3bf80f64e1fb87be593cb8a6848 DE-627 ger DE-627 rakwb eng QD241-441 Jun Zhang verfasserin aut Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety 2016 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC50: 2.357–3.012 μM) was found more potent than Sunitinib (IC50: 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively. 5-bromo-7-azaindolin-2-ones synthesis antitumor activity Organic chemistry Weiyi Shen verfasserin aut Xiaoning Li verfasserin aut Yun Chai verfasserin aut Senjun Li verfasserin aut Kai Lv verfasserin aut Huiyuan Guo verfasserin aut Mingliang Liu verfasserin aut In Molecules MDPI AG, 2003 21(2016), 12, p 1674 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:21 year:2016 number:12, p 1674 https://doi.org/10.3390/molecules21121674 kostenfrei https://doaj.org/article/a25ad3bf80f64e1fb87be593cb8a6848 kostenfrei http://www.mdpi.com/1420-3049/21/12/1674 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 21 2016 12, p 1674
allfieldsSound	10.3390/molecules21121674 doi (DE-627)DOAJ002654369 (DE-599)DOAJa25ad3bf80f64e1fb87be593cb8a6848 DE-627 ger DE-627 rakwb eng QD241-441 Jun Zhang verfasserin aut Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety 2016 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC50: 2.357–3.012 μM) was found more potent than Sunitinib (IC50: 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively. 5-bromo-7-azaindolin-2-ones synthesis antitumor activity Organic chemistry Weiyi Shen verfasserin aut Xiaoning Li verfasserin aut Yun Chai verfasserin aut Senjun Li verfasserin aut Kai Lv verfasserin aut Huiyuan Guo verfasserin aut Mingliang Liu verfasserin aut In Molecules MDPI AG, 2003 21(2016), 12, p 1674 (DE-627)311313132 (DE-600)2008644-1 14203049 nnns volume:21 year:2016 number:12, p 1674 https://doi.org/10.3390/molecules21121674 kostenfrei https://doaj.org/article/a25ad3bf80f64e1fb87be593cb8a6848 kostenfrei http://www.mdpi.com/1420-3049/21/12/1674 kostenfrei https://doaj.org/toc/1420-3049 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_70 GBV_ILN_73 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_2005 GBV_ILN_2009 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2055 GBV_ILN_2111 GBV_ILN_4012 GBV_ILN_4037 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4249 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 21 2016 12, p 1674
language	English
source	In Molecules 21(2016), 12, p 1674 volume:21 year:2016 number:12, p 1674
sourceStr	In Molecules 21(2016), 12, p 1674 volume:21 year:2016 number:12, p 1674
format_phy_str_mv	Article
institution	findex.gbv.de
topic_facet	5-bromo-7-azaindolin-2-ones synthesis antitumor activity Organic chemistry
isfreeaccess_bool	true
container_title	Molecules
authorswithroles_txt_mv	Jun Zhang @@aut@@ Weiyi Shen @@aut@@ Xiaoning Li @@aut@@ Yun Chai @@aut@@ Senjun Li @@aut@@ Kai Lv @@aut@@ Huiyuan Guo @@aut@@ Mingliang Liu @@aut@@
publishDateDaySort_date	2016-01-01T00:00:00Z
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callnumber-first	Q - Science
author	Jun Zhang
spellingShingle	Jun Zhang misc QD241-441 misc 5-bromo-7-azaindolin-2-ones misc synthesis misc antitumor activity misc Organic chemistry Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
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topic_title	QD241-441 Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety 5-bromo-7-azaindolin-2-ones synthesis antitumor activity
topic	misc QD241-441 misc 5-bromo-7-azaindolin-2-ones misc synthesis misc antitumor activity misc Organic chemistry
topic_unstemmed	misc QD241-441 misc 5-bromo-7-azaindolin-2-ones misc synthesis misc antitumor activity misc Organic chemistry
topic_browse	misc QD241-441 misc 5-bromo-7-azaindolin-2-ones misc synthesis misc antitumor activity misc Organic chemistry
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title	Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
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title_full	Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
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author_browse	Jun Zhang Weiyi Shen Xiaoning Li Yun Chai Senjun Li Kai Lv Huiyuan Guo Mingliang Liu
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title_sort	synthesis and antitumor activity of 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1h-pyrrole-3-carboxamide moiety
callnumber	QD241-441
title_auth	Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
abstract	We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC50: 2.357–3.012 μM) was found more potent than Sunitinib (IC50: 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively.
abstractGer	We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC50: 2.357–3.012 μM) was found more potent than Sunitinib (IC50: 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively.
abstract_unstemmed	We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC50: 2.357–3.012 μM) was found more potent than Sunitinib (IC50: 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively.
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container_issue	12, p 1674
title_short	Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
url	https://doi.org/10.3390/molecules21121674 https://doaj.org/article/a25ad3bf80f64e1fb87be593cb8a6848 http://www.mdpi.com/1420-3049/21/12/1674 https://doaj.org/toc/1420-3049
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Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety

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