Design, Synthesis, and Anticancer Activity of New Quinazoline Derivatives Containing Acetylhydrazide Moiety as EGFR Inhibitors and Apoptosis Inducers

被引：5
|
作者：
Alsantali, Reem I. [1 ]
机构：
[1] Taif Univ, Coll Pharm, Dept Pharmaceut Chem, POB 11099, Taif 21944, Saudi Arabia
来源：
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY | 2023年 / 49卷 / 03期
关键词：
quinazoline; acetohydrazide; cytotoxicity; cell cycle; apoptosis; VITRO ANTITUMOR-ACTIVITY; GROWTH-FACTOR RECEPTOR; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; KINASE; ANTICONVULSANT; THIAZOLIDINONE; CLEAVAGE;
D O I：
10.1134/S1068162023030044
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Novel fuoryl quinazoline compounds were synthesized and assessed for anti-cancer efficacy. To varying degrees, all drugs exhibited cytotoxic effect against the test strains. Compound (VIIIc) had the highest IC50 values on MCF7 and HCT116 cell lines, with 25.43 to 23.69 mu M, respectively. Compound (VIIIc) shows potent inhibitory activity towards EGFR. Flow cytometric studies revealed that compound (VIIIc) was capable of inducing G2/M arrest with a strong apoptotic effect.
引用
收藏
页码：645 / 654
页数：10
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