2. Academic Validation
  3. Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds

Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds

  • Eur J Med Chem. 2016 Apr 13:112:106-113. doi: 10.1016/j.ejmech.2016.02.002.
Menshawy A Mohamed 1,  Rezk R Ayyad 2,  Taghreed Z Shawer 2,  Alaa A-M Abdel-Aziz 3,  Adel S El-Azab 4
Affiliations

Affiliations

  • 1 Department of Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt; Department of Pharmaceutical Chemistry, College of Pharmacy, Salman Bin Abdulaziz University, AlKharj, Saudi Arabia.
  • 2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
  • 3 Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura, Egypt.
  • 4 Department of Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt; Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. Electronic address: adelazaba@yahoo.com.
PMID: 26890117 DOI: 10.1016/j.ejmech.2016.02.002
Abstract

A novel series of 2-[(3-substituted-4(3H)-quinazolin-2-yl)thio]-N-(3,4,5-trimethoxyphenyl)acetamide (15-21) and 3-[(3-substituted-4(3H)-quinazolin-2-yl)thio])-N-(3,4,5-trimethoxyphenyl)propanamide (23-29) were designed, prepared and estimated for their Anticancer activity in a solo dose 10 μM of the test compounds in the NCI 57 cell lines panel assay. Compounds 20, 23, 26, 27 and 28 revealed extensive-spectrum antitumor efficiency to numerous cell lines that belong to various tumor subpanels, while compounds 15, 16 and 19 possessed perceptive activity toward A498 and UO-31 renal Cancer cell lines, and compound 17 showed selective effectiveness against NSC lung Cancer NCI-H522 cell line. Additionally, compound 18 showed advanced activity against SR leukemia cell line, NSC lung Cancer HOP-92 and renal Cancer UO-31 cell lines.

Keywords

Anticancer; Broad spectrum; NCI; Quinazoline scaffolds; Synthesis.

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