Design, synthesis and biological evaluation of some novel substituted quinazolines as antitumor agents

A novel series of 6-chloro-2-p-tolylquinazolinone and substituted-(4-methylbenzamido)benzamide (1–20) were designed, synthesized and evaluated for their in-vitro antitumor activity. Compounds 3, 14 and 16 possessed remarkable broad-spectrum antitumor activity. Compound 16 was found to be a particula...

Full description

Saved in:
Bibliographic Details
Published in:European journal of medicinal chemistry 2014-05, Vol.79, p.446-454
Main Authors: Alanazi, Amer M., Abdel-Aziz, Alaa A.-M., Al-Suwaidan, Ibrahim A., Abdel-Hamide, Sami G., Shawer, Taghreed Z., El-Azab, Adel S.
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cell Line, Tumor
Cell Proliferation - drug effects
Cyclization
Dose-Response Relationship, Drug
Drug Design
Drug Screening Assays, Antitumor
Humans
In-vitro antitumor evaluation
Molecular Structure
NCI
Quinazoline
Quinazolines - chemical synthesis
Quinazolines - chemistry
Quinazolines - pharmacology
Selective activity
Structure-Activity Relationship
Synthesis
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A novel series of 6-chloro-2-p-tolylquinazolinone and substituted-(4-methylbenzamido)benzamide (1–20) were designed, synthesized and evaluated for their in-vitro antitumor activity. Compounds 3, 14 and 16 possessed remarkable broad-spectrum antitumor activity. Compound 16 was found to be a particularly active growth inhibitor of the renal cancer (GI50 = 4.07 μM), CNS cancer (GI50 = 7.41 μM), ovarian cancer (GI50 = 7.41 μM) and non-small cell lung cancer (GI50 = 7.94 μM). Compound 16 ranks as nearly 1.5-fold more potent (mean GI50 = 15.8 μM) compared to 5-FU (mean GI50 = 22.6 μM). Compound 16 possessed broad-spectrum antitumor activities with 1.5-fold potency (mean GI50 = 15.8 μM), compared to 5-FU (mean GI50 = 22.6 μM). [Display omitted] •A novel series of 6-chloro-2-p-tolylquinazolinone were designed and synthesized.•The synthesized compounds were evaluated for their in-vitro antitumor activity.•Compound 16 possessed broad-spectrum antitumor activities.•Compound 16 has 1.5-fold potency compared to 5-FU.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2014.04.029