Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives

Some new 3H-quinazolin-4-one derivatives were synthesised and screened for anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities. Compound 15d was more potent in reducing the cell viabilities of HT-29 and SW620 cells lines to 38%, 36.7%, compared to 5-FU which demonstr...

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Main Authors:	El-Sayed, Nahed Nasser Eid, Almaneai, Norah M., Ben Bacha, Abir G., Al-Obeed, Omar A., Ahmad, Rehan, Abdulla, Maha Hamadien, Alafeefy, Ahmed Mahmoud
Format:	Article
Language:	English English English
Published:	Taylor & Francis 2019
Subjects:	QD Chemistry RC0254 Neoplasms. Tumors. Oncology (including Cancer)
Online Access:	http://irep.iium.edu.my/72704/ http://irep.iium.edu.my/72704/ http://irep.iium.edu.my/72704/ http://irep.iium.edu.my/72704/19/72704_Synthesis%20and%20evaluation%20of%20anticancer_article.pdf http://irep.iium.edu.my/72704/2/72704_Synthesis%20and%20evaluation%20of%20anticancer_scopus.pdf http://irep.iium.edu.my/72704/3/72704_Synthesis%20and%20evaluation%20of%20anticancer_wos.pdf

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recordtype	eprints
spelling	iium-727042019-11-17T16:07:59Z http://irep.iium.edu.my/72704/ Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives El-Sayed, Nahed Nasser Eid Almaneai, Norah M. Ben Bacha, Abir G. Al-Obeed, Omar A. Ahmad, Rehan Abdulla, Maha Hamadien Alafeefy, Ahmed Mahmoud QD Chemistry RC0254 Neoplasms. Tumors. Oncology (including Cancer) Some new 3H-quinazolin-4-one derivatives were synthesised and screened for anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities. Compound 15d was more potent in reducing the cell viabilities of HT-29 and SW620 cells lines to 38%, 36.7%, compared to 5-FU which demonstrated cell viabilities of 65.9 and 42.7% respectively. The IC50 values of 15d were ∼20 µg/ml. Assessment of apoptotic activity revealed that 15d decreased the cell viability by down regulating Bcl2 and BclxL. Moreover, compounds, 8j, 8d/15a/15e, 5b, and 8f displayed lowered IC50 values than oleanolic acid against proinflammatory isoforms of hGV, hG-X, NmPLA2, and AmPLA2. In addition, 8d, 8h, 8j, 15a, 15b, 15e, and 15f showed better anti-α-amylase than quercetin, whereas 8g, 8h, and 8i showed higher anti-α-glucosidase activity than allopurinol. Thus, these compounds can be considered as potential antidiabetic agents. Finally, none of the compounds showed higher antiproteases or xanthine oxidase activities than the used reference drugs. Taylor & Francis 2019-01-01 Article PeerReviewed application/pdf en http://irep.iium.edu.my/72704/19/72704_Synthesis%20and%20evaluation%20of%20anticancer_article.pdf application/pdf en http://irep.iium.edu.my/72704/2/72704_Synthesis%20and%20evaluation%20of%20anticancer_scopus.pdf application/pdf en http://irep.iium.edu.my/72704/3/72704_Synthesis%20and%20evaluation%20of%20anticancer_wos.pdf El-Sayed, Nahed Nasser Eid and Almaneai, Norah M. and Ben Bacha, Abir G. and Al-Obeed, Omar A. and Ahmad, Rehan and Abdulla, Maha Hamadien and Alafeefy, Ahmed Mahmoud (2019) Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives. Journal of Enzyme Inhibition and Medicinal Chemistry, 34 (1). pp. 672-683. ISSN 1475-6366 E-ISSN 1475-6374 https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1574780 10.1080/14756366.2019.1574780
repository_type	Digital Repository
institution_category	Local University
institution	International Islamic University Malaysia
building	IIUM Repository
collection	Online Access
language	English English English
topic	QD Chemistry RC0254 Neoplasms. Tumors. Oncology (including Cancer)
spellingShingle	QD Chemistry RC0254 Neoplasms. Tumors. Oncology (including Cancer) El-Sayed, Nahed Nasser Eid Almaneai, Norah M. Ben Bacha, Abir G. Al-Obeed, Omar A. Ahmad, Rehan Abdulla, Maha Hamadien Alafeefy, Ahmed Mahmoud Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
description	Some new 3H-quinazolin-4-one derivatives were synthesised and screened for anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities. Compound 15d was more potent in reducing the cell viabilities of HT-29 and SW620 cells lines to 38%, 36.7%, compared to 5-FU which demonstrated cell viabilities of 65.9 and 42.7% respectively. The IC50 values of 15d were ∼20 µg/ml. Assessment of apoptotic activity revealed that 15d decreased the cell viability by down regulating Bcl2 and BclxL. Moreover, compounds, 8j, 8d/15a/15e, 5b, and 8f displayed lowered IC50 values than oleanolic acid against proinflammatory isoforms of hGV, hG-X, NmPLA2, and AmPLA2. In addition, 8d, 8h, 8j, 15a, 15b, 15e, and 15f showed better anti-α-amylase than quercetin, whereas 8g, 8h, and 8i showed higher anti-α-glucosidase activity than allopurinol. Thus, these compounds can be considered as potential antidiabetic agents. Finally, none of the compounds showed higher antiproteases or xanthine oxidase activities than the used reference drugs.
format	Article
author	El-Sayed, Nahed Nasser Eid Almaneai, Norah M. Ben Bacha, Abir G. Al-Obeed, Omar A. Ahmad, Rehan Abdulla, Maha Hamadien Alafeefy, Ahmed Mahmoud
author_facet	El-Sayed, Nahed Nasser Eid Almaneai, Norah M. Ben Bacha, Abir G. Al-Obeed, Omar A. Ahmad, Rehan Abdulla, Maha Hamadien Alafeefy, Ahmed Mahmoud
author_sort	El-Sayed, Nahed Nasser Eid
title	Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
title_short	Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
title_full	Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
title_fullStr	Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
title_full_unstemmed	Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives
title_sort	synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3h-quinazolin-4-one derivatives
publisher	Taylor & Francis
publishDate	2019
url	http://irep.iium.edu.my/72704/ http://irep.iium.edu.my/72704/ http://irep.iium.edu.my/72704/ http://irep.iium.edu.my/72704/19/72704_Synthesis%20and%20evaluation%20of%20anticancer_article.pdf http://irep.iium.edu.my/72704/2/72704_Synthesis%20and%20evaluation%20of%20anticancer_scopus.pdf http://irep.iium.edu.my/72704/3/72704_Synthesis%20and%20evaluation%20of%20anticancer_wos.pdf
first_indexed	2023-09-18T21:43:02Z
last_indexed	2023-09-18T21:43:02Z
_version_	1777413267398852608

Synthesis and evaluation of anticancer, antiphospholipases, antiproteases, and antimetabolic syndrome activities of some 3H-quinazolin-4-one derivatives

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