title: Synthesis and antitumor evaluation of trimethoxyanilides based on 4(3H)-quinazolinone scaffolds.
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.
authors.affiliation: 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.
authors.forename: Menshawy A
authors.initials: MA
authors.lastname: Mohamed
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
authors.forename: Rezk R
authors.initials: RR
authors.lastname: Ayyad
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.
authors.forename: Taghreed Z
authors.initials: TZ
authors.lastname: Shawer
authors.affiliation: 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.
authors.forename: Alaa A-M
authors.initials: AA
authors.lastname: Abdel-Aziz
authors.affiliation: 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.
authors.forename: Adel S
authors.initials: AS
authors.lastname: El-Azab
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D052999:Quinazolinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D052999:Quinazolinones; C061339:4-hydroxyquinazoline
keywords: Anticancer; Broad spectrum; NCI; Quinazoline scaffolds; Synthesis