Abstract:
:In this paper, a set of 3-methylquniazolinone derivatives were designed, synthesised, and studied the preliminary structure-activity relationship for antiproliferative activities. All target compounds performed significantly inhibitory effects against wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) and tumour cells (A431, A549, MCF-7, and NCI-H1975). In particular, compound 4d 3-fluoro-N-(4-((3-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)methoxy)phenyl)benzamide showed higher antiproliferative activities against all tumour cells than Gefitinib (IC50 of 3.48, 2.55, 0.87 and 6.42 μM, respectively). Furthermore, compound 4d could induce apoptosis of MCF-7 cells and arrest in G2/M phase at the tested concentration. Molecular docking and ADMET studies showed that compound 4d could closely form many hydrogen bonds with EGFRwt-TK. Therefore, compound 4d is potential to develop as novel anti-cancer drug.
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Zhang Y,Wang Q,Li L,Le Y,Liu L,Yang J,Li Y,Bao G,Yan Ldoi
10.1080/14756366.2021.1933466keywords:
["EGFR","Quinazolinone","antiproliferative","kinase inhibitor","structure-activity relationship"]subject
Has Abstractpub_date
2021-12-01 00:00:00pages
1205-1216issue
1eissn
1475-6366issn
1475-6374journal_volume
36pub_type
杂志文章abstract::Mating stimulation, particularly vaginal-cervical stimulation, causes estrous abbreviation in female rats. In most previous studies, female rats were repeatedly tested for sexual behavior until estrous termination occurred. Thus, it was not clear whether sensory stimulation (e.g., flank stimulation, olfactory cues) re...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360290018611
更新日期:2002-02-01 00:00:00
abstract::During a polyphasic taxonomic analysis performed on isolates from shallow marine hydrothermal vents of Eolian Islands (Italy), three thermophilic, halotolerant bacilli, designated as strain 1bw, strain 5-2 and strain 10-1, could not be affiliated to any described species. Physiological and biochemical characteristics,...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360290028610
更新日期:2002-04-01 00:00:00
abstract::Steroid receptor RNA activator (SRA) is an RNA transcript that functions as a eukaryotic transcriptional coactivator for steroid hormone receptors. We report here the isolation and functional characterization of distinct RNA substructures within the SRA molecule that constitute its coactivation function. We used compa...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636021000003174
更新日期:2002-06-01 00:00:00
abstract::This study investigated the functional neuroanatomy of the anterior medial prefrontal cortex (aMPFC). Previous studies have shown that the aMPFC is involved in evaluative judgment and self-referential processes. Specifically, different sections of the aMPFC are differentially influenced by attention demanding processe...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章,评审
doi:10.1080/14756360210000010923
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abstract::Emerin and MAN1 are LEM domain-containing integral membrane proteins of the vertebrate nuclear envelope. The function of MAN1 is unknown, whereas emerin is known to interact with nuclear lamins, barrier-to-autointegration factor (BAF), nesprin-1 alpha, and a transcription repressor. Mutations in emerin cause X-linked ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636021000005659
更新日期:2002-12-01 00:00:00
abstract::Emerin and MAN1 are LEM domain-containing integral membrane proteins of the vertebrate nuclear envelope. The function of MAN1 is unknown, whereas emerin is known to interact with nuclear lamins, barrier-to-autointegration factor (BAF), nesprin-1 alpha, and a transcription repressor. Mutations in emerin cause X-linked ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636021000005758
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abstract::Filarial infections are characterized by high IgE antibody responses. So far, it is not clear whether IgE antibodies are involved in protection, pathology or both. We established a bioassay to detect reactive IgE antibodies in jirds infected with the filaria Acanthocheilonema viteae. Sera of A. viteae-infected jirds w...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636031000069291
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abstract::The synthesis of benzoxathiins bearing a retroamide function is described from 8-hydroxythiochroman, the key step involving the synthesis of the benzoxathiin ring through a sulfonium salt. These new melatonin analogues were evaluated on human receptors MT1 and MT2 and have a similar affinity to that of melatonin itsel...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636031000093534
更新日期:2003-04-01 00:00:00
abstract::The synthesis of benzoxathiins bearing a retroamide function is described from 8-hydroxythiochroman, the key step involving the synthesis of the benzoxathiin ring through a sulfonium salt. These new melatonin analogues were evaluated on human receptors MT1 and MT2 and have a similar affinity to that of melatonin itsel...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636032000096855
更新日期:2003-04-01 00:00:00
abstract::Secular trends and epidemiological characteristics of 1,581 oesophageal cancers, diagnosed in South Australian residents in 1977-2000, were analysed by histological type and diagnostic period, using multivariable Poisson regression and logistic regression. The age-adjusted incidence of squamous cell carcinoma did not ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636031000080216
更新日期:2003-06-01 00:00:00
abstract::The prognosis of HIV infection has been modified by antiretroviral therapy. However, the morbidity and the mortality of HCV co-infection increase and may be a major problem of health service. Up to now co-infected patients are excluded of transplantation due to complexity, the ethical aspects, the immunodeficiency and...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636031000118428
更新日期:2003-08-01 00:00:00
abstract::The prognosis of HIV infection has been modified by antiretroviral therapy. However, the morbidity and the mortality of HCV co-infection increase and may be a major problem of health service. Up to now co-infected patients are excluded of transplantation due to complexity, the ethical aspects, the immunodeficiency and...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636031000120416
更新日期:2003-08-01 00:00:00
abstract:OBJECTIVE:The aim of this study was to determine whether open-magnet magnetic resonance (MR) defaecography could provide more useful clinical information than evacuation proctography (EP) alone in the evaluation of a cohort of patients with full-thickness rectal intussusception and could assist in decisions concerning ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/1475636031000138741
更新日期:2003-10-01 00:00:00
abstract::Understanding biological processes in the context of intact organ systems with fine temporal resolution has required the development of imaging strategies that reveal cellular and molecular changes in the living body. Reporter genes that confer optical signatures on a given biological process have been used widely in ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360310001613094
更新日期:2003-12-01 00:00:00
abstract::Recently, we have shown that transferrin (Tf) is actively endocytosed by the Tf R on primary cultured bovine brain capillary endothelial cells (BCEC). The objective of this investigation is to determine whether the Tf R can facilitate endocytosis of a (protein) model drug, using Tf as a targeting vector. Secondly, the...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360310001623318
更新日期:2004-02-01 00:00:00
abstract::Parathyroid hormone-related protein (PTHrP) is expressed in normal and malignant lung and has roles in development, homeostasis, and pathophysiology of injury and cancer. Its effects in developing lung include regulation of branching morphogenesis and type II cell maturation. In adult lung, PTHrP stimulates disaturate...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360310001650246
更新日期:2004-04-01 00:00:00
abstract::Parathyroid hormone-related protein (PTHrP) is expressed in normal and malignant lung and has roles in development, homeostasis, and pathophysiology of injury and cancer. Its effects in developing lung include regulation of branching morphogenesis and type II cell maturation. In adult lung, PTHrP stimulates disaturate...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360310001640472
更新日期:2004-04-01 00:00:00
abstract::We describe an automated 3-D segmentation system for in vivo brain magnetic resonance images (MRI). Our segmentation method combines a variety of filtering, segmentation, and registration techniques and makes maximum use of the available a priori biomedical expertise, both in an implicit and an explicit form. We appro...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章,评审
doi:10.1080/14756360410001689540
更新日期:2004-06-01 00:00:00
abstract::We describe an automated 3-D segmentation system for in vivo brain magnetic resonance images (MRI). Our segmentation method combines a variety of filtering, segmentation, and registration techniques and makes maximum use of the available a priori biomedical expertise, both in an implicit and an explicit form. We appro...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360410001689531
更新日期:2004-06-01 00:00:00
abstract:OBJECTIVE:To review the prevalence of sexual concerns and the relevance of this area to psychiatrists and to present evidence supporting the need for psychiatrists to routinely include a sex-function inquiry in the assessment of their patients. METHOD:A review of the recent literature was undertaken. CONCLUSIONS:Sex ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360409162450
更新日期:2004-08-01 00:00:00
abstract::By using a single compartment biophysical model of a fast spiking interneuron the synchronization properties of a pair of cells, coupled by electrical and inhibitory synapses, are investigated. The inhibitory and excitatory synaptic couplings are modeled in order to reproduce the experimental time course of the corres...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360410001733694
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abstract:OBJECTIVE:To compare pre-induction ultrasonographic cervical length and Bishop score in predicting time to delivery after labour induction with prostaglandins. DESIGN:Prognostic cohort study. SETTING:Tertiary referral maternity unit in a teaching hospital. POPULATION:Two hundred and sixty-six women with singleton pr...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360412331280464
更新日期:2004-12-01 00:00:00
abstract::For group-living animals, the maintenance of a position in the social hierarchy may be associated with physiological costs such as increased stress and energy expenditure or suppressed immune functions. In this study, we experimentally manipulated the social status of house sparrows so that each bird experienced two s...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360400015231
更新日期:2005-02-01 00:00:00
abstract::Inflammation is implicated in the pathogenesis of erythropoietin (EPO) resistance in patients with end-stage renal disease. Interleukin (IL)-6 and tumor necrosis factor (TNF)-alpha are suggested to suppress erythropoiesis in uremia. Insulin like growth factor (IGF)-1 has been proposed to stimulate erythropoiesis. Noct...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360500043257
更新日期:2005-04-01 00:00:00
abstract:BACKGROUND:Women with gestational diabetes (GDM) need to assimilate information and management skills rapidly for their diabetes to prevent adverse pregnancy outcomes. Strict glycaemic control is necessary and is improved by regular self-monitoring of blood glucose. The Softsense meter (MediSense Products, Witney, UK) ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360400021858
更新日期:2005-06-01 00:00:00
abstract:BACKGROUND:Women with gestational diabetes (GDM) need to assimilate information and management skills rapidly for their diabetes to prevent adverse pregnancy outcomes. Strict glycaemic control is necessary and is improved by regular self-monitoring of blood glucose. The Softsense meter (MediSense Products, Witney, UK) ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360310001624948
更新日期:2005-06-01 00:00:00
abstract::To date, several susceptibility loci for systemic lupus erythematosus (SLE) have been identified by individual genome-wide scans, but many of these loci have shown inconsistent results across studies. Additionally, many individual studies are at the lower limit of acceptable power recommended for declaring significant...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360500112409
更新日期:2005-08-01 00:00:00
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journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360500277251
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abstract:AIM:To evaluate the efficacy of 0.5%, 2.5% and 5.25% sodium hypochlorite (NaOCl) as intracanal irrigants associated with hand and rotary instrumentation techniques against Enterococcus faecalis within root canals and dentinal tubules. METHODOLOGY:A total of 180 extracted human premolar teeth were infected for 21 days ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360500213231
更新日期:2005-12-01 00:00:00
abstract::Rab small GTPases are involved in the transport of vesicles between different membranous organelles. RAB-3 is an exocytic Rab that plays a modulatory role in synaptic transmission. Unexpectedly, mutations in the Caenorhabditis elegans RAB-3 exchange factor homologue, aex-3, cause a more severe synaptic transmission de...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
doi:10.1080/14756360500277459
更新日期:2006-02-01 00:00:00