Next Article in Journal
Erythroxylum in Focus: An Interdisciplinary Review of an Overlooked Genus
Next Article in Special Issue
Potent Cytotoxicity of Novel L-Shaped Ortho-Quinone Analogs through Inducing Apoptosis
Previous Article in Journal
A Glimepiride-Metformin Multidrug Crystal: Synthesis, Crystal Structure Analysis, and Physicochemical Properties
Previous Article in Special Issue
Design, Synthesis, and Biological Evaluation of Novel Thienopyrimidine Derivatives as PI3Kα Inhibitors
Open AccessArticle

Synthesis, Antiproliferative, and Antioxidant Evaluation of 2-Pentylquinazolin-4(3H)-one(thione) Derivatives with DFT Study

1
Department of Chemistry, Faculty of Science, Ain Shams University, 11566 Abbassia, Cairo 11566, Egypt
2
Pharmaceutical Chemistry Department, Drug Exploration & Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
3
Applied Organic Chemistry Department, National Research Center, Cairo, Dokki 12622, Egypt
4
Peptide Chemistry Department, Chemical Industries Research Division, National Research Centre, Dokki, Cairo 12622, Egypt
*
Author to whom correspondence should be addressed.
Academic Editor: Qiao-Hong Chen
Molecules 2019, 24(20), 3787; https://doi.org/10.3390/molecules24203787
Received: 5 October 2019 / Revised: 19 October 2019 / Accepted: 20 October 2019 / Published: 21 October 2019
(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation)
The current study was chiefly designed to examine the antiproliferative and antioxidant activities of some novel quinazolinone(thione) derivatives 614. The present work focused on two main points; firstly, comparing between quinazolinone and quinazolinthione derivatives. Whereas, antiproliferative (against two cell lines namely, HepG2 and MCF-7) and antioxidant (by two methods; ABTS and DPPH) activities of the investigated compounds, the best quinazolinthione derivatives were 6 and 14, which exhibited excellent potencies comparable to quinazolinone derivatives 5 and 9, respectively. Secondly, we compared the activity of four series of Schiff bases which included the quinazolinone moiety (11ad). In addition, the antiproliferative and antioxidant activities of the compounds with various aryl aldehyde hydrazone derivatives (11ad) analogs were studied. The compounds exhibited potency that increased with increasing electron donating group in p-position (OH > OMe > Cl) due to extended conjugated systems. Noteworthy, most of antiproliferative and antioxidant activities results for the tested compounds are consistent with the DFT calculations. View Full-Text
Keywords: quinazolin-4(3H)-one; quinazolin-4(3H)-thione; Schiff base; antiproliferative activity; antioxidant activity; DFT study quinazolin-4(3H)-one; quinazolin-4(3H)-thione; Schiff base; antiproliferative activity; antioxidant activity; DFT study
Show Figures

Figure 1

MDPI and ACS Style

El-Sayed, A.A.; Ismail, M.F.; Amr, A.E.-G.E.; Naglah, A.M. Synthesis, Antiproliferative, and Antioxidant Evaluation of 2-Pentylquinazolin-4(3H)-one(thione) Derivatives with DFT Study. Molecules 2019, 24, 3787.

AMA Style

El-Sayed AA, Ismail MF, Amr AE-GE, Naglah AM. Synthesis, Antiproliferative, and Antioxidant Evaluation of 2-Pentylquinazolin-4(3H)-one(thione) Derivatives with DFT Study. Molecules. 2019; 24(20):3787.

Chicago/Turabian Style

El-Sayed, Amira A.; Ismail, Mahmoud F.; Amr, Abd E.-G.E.; Naglah, Ahmed M. 2019. "Synthesis, Antiproliferative, and Antioxidant Evaluation of 2-Pentylquinazolin-4(3H)-one(thione) Derivatives with DFT Study" Molecules 24, no. 20: 3787.

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Search more from Scilit
 
Search
Back to TopTop