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

The current study was chiefly designed to examine the antiproliferative and antioxidant activities of some novel quinazolinone(thione) derivatives <b>6</b>&#8722;<b>14</b>. The present work focused on two main points; firstly, comparing between quinazolinone and quinazoli...

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Bibliographic Details
Main Authors: Amira A. El-Sayed, Mahmoud F. Ismail, Abd El-Galil E. Amr, Ahmed M. Naglah
Format: Article
Language:English
Published: MDPI AG 2019-10-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/24/20/3787
Description
Summary:The current study was chiefly designed to examine the antiproliferative and antioxidant activities of some novel quinazolinone(thione) derivatives <b>6</b>&#8722;<b>14</b>. 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 <b>6</b> and <b>14,</b> which exhibited excellent potencies comparable to quinazolinone derivatives <b>5</b> and <b>9</b>, respectively. Secondly, we compared the activity of four series of Schiff bases which included the quinazolinone moiety (<b>11a</b>&#8722;<b>d</b>). In addition, the antiproliferative and antioxidant activities of the compounds with various aryl aldehyde hydrazone derivatives (<b>11a</b>&#8722;<b>d</b>) analogs were studied. The compounds exhibited potency that increased with increasing electron donating group in <i>p</i>-position (OH &gt; OMe &gt; Cl) due to extended conjugated systems. Noteworthy, most of antiproliferative and antioxidant activities results for the tested compounds are consistent with the DFT calculations.
ISSN:1420-3049