Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies

The present study describes several novel 2,5-biaryl-3-hexylthiophene derivatives (3a-i) synthesized via a Pd(0)-catalyzed Suzuki cross-coupling reaction in moderate to good yields. The novel compounds were also analyzed for their anti-thrombolytic, haemolytic, and biofilm inhibition activities. In...

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Main Authors:	Ikram , Hafiz Mansoor, Rasool, Nasir, Zubair, Muhammad, Khan, Khalid Mohammed, Chotana, Ghayoor Abbas, Akhtar, Muhammad Nadeem, Nadiah, Abu, Noorjahan Banu, Alitheen, Elgorban, Abdallah Mohamed, Rana, Usman Ali
Format:	Article
Language:	English
Published:	MDPI - Open Access Publishing 2016
Subjects:	QR Microbiology
Online Access:	http://umpir.ump.edu.my/id/eprint/16833/ http://umpir.ump.edu.my/id/eprint/16833/ http://umpir.ump.edu.my/id/eprint/16833/ http://umpir.ump.edu.my/id/eprint/16833/1/fist-2016-nadeem-Efficient%20Double%20Suzuki%20Cross-Coupling.pdf

id	ump-16833
recordtype	eprints
spelling	ump-168332017-11-02T07:21:34Z http://umpir.ump.edu.my/id/eprint/16833/ Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies Ikram , Hafiz Mansoor Rasool, Nasir Zubair, Muhammad Khan, Khalid Mohammed Chotana, Ghayoor Abbas Akhtar, Muhammad Nadeem Nadiah, Abu Noorjahan Banu, Alitheen Elgorban, Abdallah Mohamed Rana, Usman Ali QR Microbiology The present study describes several novel 2,5-biaryl-3-hexylthiophene derivatives (3a-i) synthesized via a Pd(0)-catalyzed Suzuki cross-coupling reaction in moderate to good yields. The novel compounds were also analyzed for their anti-thrombolytic, haemolytic, and biofilm inhibition activities. In addition, the anti-tumor activity was also evaluated in vitro for newly-synthesized compounds, where 3-hexyl-2,5-bis(4-(methylthio)phenyl)thiophene exhibited the best anti-tumor activity against 4T1 cells with IC50 value of 16 μM. Moreover, 2,5-bis(4-methylphenyl)-3-hexylthiophene showed the highest activity against MCF-7 cells with an IC50 value of 26.2 μM. On the other hand, the compound 2,5-bis(4-chloropheny)-3-hexylthiophene exhibited excellent biofilm inhibition activity. Furthermore, the compound 2,5-bis(3-chloro-4-fluorophenyl)-3-hexylthiophene also exhibited better anti-thrombolytic and hemolytic activity results as compared to the other newly-synthesized compounds. MDPI - Open Access Publishing 2016 Article PeerReviewed application/pdf en cc_by http://umpir.ump.edu.my/id/eprint/16833/1/fist-2016-nadeem-Efficient%20Double%20Suzuki%20Cross-Coupling.pdf Ikram , Hafiz Mansoor and Rasool, Nasir and Zubair, Muhammad and Khan, Khalid Mohammed and Chotana, Ghayoor Abbas and Akhtar, Muhammad Nadeem and Nadiah, Abu and Noorjahan Banu, Alitheen and Elgorban, Abdallah Mohamed and Rana, Usman Ali (2016) Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies. Molecules, 21 (977). pp. 1-11. ISSN 1420-3049 (print); 1420-3049 (online) http://dx.doi.org/10.3390/molecules21080977 doi: 10.3390/molecules21080977
repository_type	Digital Repository
institution_category	Local University
institution	Universiti Malaysia Pahang
building	UMP Institutional Repository
collection	Online Access
language	English
topic	QR Microbiology
spellingShingle	QR Microbiology Ikram , Hafiz Mansoor Rasool, Nasir Zubair, Muhammad Khan, Khalid Mohammed Chotana, Ghayoor Abbas Akhtar, Muhammad Nadeem Nadiah, Abu Noorjahan Banu, Alitheen Elgorban, Abdallah Mohamed Rana, Usman Ali Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies
description	The present study describes several novel 2,5-biaryl-3-hexylthiophene derivatives (3a-i) synthesized via a Pd(0)-catalyzed Suzuki cross-coupling reaction in moderate to good yields. The novel compounds were also analyzed for their anti-thrombolytic, haemolytic, and biofilm inhibition activities. In addition, the anti-tumor activity was also evaluated in vitro for newly-synthesized compounds, where 3-hexyl-2,5-bis(4-(methylthio)phenyl)thiophene exhibited the best anti-tumor activity against 4T1 cells with IC50 value of 16 μM. Moreover, 2,5-bis(4-methylphenyl)-3-hexylthiophene showed the highest activity against MCF-7 cells with an IC50 value of 26.2 μM. On the other hand, the compound 2,5-bis(4-chloropheny)-3-hexylthiophene exhibited excellent biofilm inhibition activity. Furthermore, the compound 2,5-bis(3-chloro-4-fluorophenyl)-3-hexylthiophene also exhibited better anti-thrombolytic and hemolytic activity results as compared to the other newly-synthesized compounds.
format	Article
author	Ikram , Hafiz Mansoor Rasool, Nasir Zubair, Muhammad Khan, Khalid Mohammed Chotana, Ghayoor Abbas Akhtar, Muhammad Nadeem Nadiah, Abu Noorjahan Banu, Alitheen Elgorban, Abdallah Mohamed Rana, Usman Ali
author_facet	Ikram , Hafiz Mansoor Rasool, Nasir Zubair, Muhammad Khan, Khalid Mohammed Chotana, Ghayoor Abbas Akhtar, Muhammad Nadeem Nadiah, Abu Noorjahan Banu, Alitheen Elgorban, Abdallah Mohamed Rana, Usman Ali
author_sort	Ikram , Hafiz Mansoor
title	Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies
title_short	Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies
title_full	Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies
title_fullStr	Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies
title_full_unstemmed	Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies
title_sort	efficient double suzuki cross-coupling reactions of 2,5-dibromo-3-hexylthiophene: anti-tumor, haemolytic, anti-thrombolytic and biofilm inhibition studies
publisher	MDPI - Open Access Publishing
publishDate	2016
url	http://umpir.ump.edu.my/id/eprint/16833/ http://umpir.ump.edu.my/id/eprint/16833/ http://umpir.ump.edu.my/id/eprint/16833/ http://umpir.ump.edu.my/id/eprint/16833/1/fist-2016-nadeem-Efficient%20Double%20Suzuki%20Cross-Coupling.pdf
first_indexed	2023-09-18T22:22:51Z
last_indexed	2023-09-18T22:22:51Z
_version_	1777415772112420864

Efficient Double Suzuki Cross-Coupling Reactions of 2,5-Dibromo-3-hexylthiophene: Anti-Tumor, Haemolytic, Anti-Thrombolytic and Biofilm Inhibition Studies

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