Synthesis and biological evaluation of 4-amino-5-cinnamoylthiazoles as chalcone-like anticancer agents
Copyright © 2018 Elsevier Masson SAS. All rights reserved..
A series of 4-amino-5-cinnamoylthiazoles 3a-p were designed and synthesized as chalcone-like anticancer agents. The synthesized derivatives 3a-p were evaluated for their in vitro antiproliferative activities against three different human cancer cell lines including MCF-7, HepG2 and SW480. Most of compounds could significantly prevent proliferation of tested cell lines. In particular, the pyrrolidine derivative 3e namely (E)-1-(4-amino-2-(pyrrolidin-1-yl)thiazol-5-yl)-3-(2,4-dichlorophenyl)prop-2-en-1-one showed promising activity, especially against HepG2 cells (IC50 = 10.6 μg/ml). Flow cytometric analyses revealed that the prototype compound 3e can prevent the proliferation of HepG2 cells by blockade of the cell cycle at the G2 phase and induction of apoptosis.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2018 |
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| Erschienen: |
2018 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:145 |
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| Enthalten in: |
European journal of medicinal chemistry - 145(2018) vom: 10. Feb., Seite 404-412 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ayati, Adileh [VerfasserIn] |
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| Links: |
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| Themen: |
Anticancer |
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| Anmerkungen: |
Date Completed 02.03.2018 Date Revised 02.03.2018 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejmech.2018.01.015 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM279974469 |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2018 Elsevier Masson SAS. All rights reserved. | ||
| 520 | |a A series of 4-amino-5-cinnamoylthiazoles 3a-p were designed and synthesized as chalcone-like anticancer agents. The synthesized derivatives 3a-p were evaluated for their in vitro antiproliferative activities against three different human cancer cell lines including MCF-7, HepG2 and SW480. Most of compounds could significantly prevent proliferation of tested cell lines. In particular, the pyrrolidine derivative 3e namely (E)-1-(4-amino-2-(pyrrolidin-1-yl)thiazol-5-yl)-3-(2,4-dichlorophenyl)prop-2-en-1-one showed promising activity, especially against HepG2 cells (IC50 = 10.6 μg/ml). Flow cytometric analyses revealed that the prototype compound 3e can prevent the proliferation of HepG2 cells by blockade of the cell cycle at the G2 phase and induction of apoptosis | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Anticancer | |
| 650 | 4 | |a Apoptosis | |
| 650 | 4 | |a Chalcone | |
| 650 | 4 | |a Cytotoxic activity | |
| 650 | 4 | |a Thiazole | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Thiazoles |2 NLM | |
| 700 | 1 | |a Esmaeili, Rezvan |e verfasserin |4 aut | |
| 700 | 1 | |a Moghimi, Setareh |e verfasserin |4 aut | |
| 700 | 1 | |a Oghabi Bakhshaiesh, Tayebeh |e verfasserin |4 aut | |
| 700 | 1 | |a Eslami-S, Zahra |e verfasserin |4 aut | |
| 700 | 1 | |a Majidzadeh-A, Keivan |e verfasserin |4 aut | |
| 700 | 1 | |a Safavi, Maliheh |e verfasserin |4 aut | |
| 700 | 1 | |a Emami, Saeed |e verfasserin |4 aut | |
| 700 | 1 | |a Foroumadi, Alireza |e verfasserin |4 aut | |
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