Abstract:
:A series of quinazoline clubbed 1,3,5-triazine derivatives (QCT) were synthesized and evaluated for their in vitro anticancer activity against HeLa (human cervical cancer), MCF-7 (human breast cancer cell), HL-60 (human promyelocytic leukemia cell), HepG2 (human Hepatocellular carcinoma cell), and one normal cell line HFF (human foreskin fibroblasts). In vitro assay result encouraged to further move towards in ovo anticancer evaluation using chick embryo. The series of QCT derivatives showed higher anticancer and antiangiogenic activity against HeLa and MCF-7 cell lines. In the series, synthetic molecule 8d, 8l, and 8m displayed significant activity. Further, these results substantiated by docking study on VGFR2. SAR study concluded that the potency of drugs depends on the nature of aliphatic substitution and the heterocyclic ring system.
journal_name
Inflammopharmacologyjournal_title
Inflammopharmacologyauthors
Pathak P,Shukla PK,Kumar V,Kumar A,Verma Adoi
10.1007/s10787-018-0471-3subject
Has Abstractpub_date
2018-12-01 00:00:00pages
1441-1453issue
6eissn
0925-4692issn
1568-5608pii
10.1007/s10787-018-0471-3journal_volume
26pub_type
杂志文章abstract::TRP channels have been discovered as a specialized group of somatosensory neurons involved in the detection of noxious stimuli. Desensitization of TRPV1 located on dorsal root and trigeminal ganglia exhibits analgesic effect and makes it potential therapeutic target for treatment of neuropathic pain. With this backgro...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-016-0285-0
更新日期:2016-12-01 00:00:00
abstract:AIM:Activation of sphingosine kinase (SK) is a key response to many inflammatory processes. The present studies test the hypothesis that an orally available SK inhibitor, ABC294640, would be effective in rodent models of Crohn's disease. METHODS:Trinitrobenzene sulfonic acid (TNBS) was administered rectally to mice an...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-010-0032-x
更新日期:2010-04-01 00:00:00
abstract::- The use of the non-steroidal anti-inflammatory drug, diclofenac, is associated with occasional serious side effects in the gastrointestinal (GI) tract. We examined the effect of altering the site of release of diclofenac sodium on GI tract side effects. Dissolution and pharmacokinetic studies were carried out to sub...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1163/156856004773121383
更新日期:2004-01-01 00:00:00
abstract::A small GTPase, Rac1, is recognized as an important modulator of the inflammatory responses to bacterial lipopolysaccharide (LPS) by affecting the processes of phospholipase C activation. The activation of Rac1 involves the exchange of GDP for GTP and is catalyzed by the guanine nucleotide exchange factors (GEFs). Her...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-015-0235-2
更新日期:2015-06-01 00:00:00
abstract::The intestinal mucosa is subject to a variety of physical forces in a complex manner during normal gut function and in disease. Intestinal mucosal atrophy during some disease states is a troubling phenomenon that is only partially explained by nutritional parameters. Increasing evidence suggests the possibility that r...
journal_title:Inflammopharmacology
pub_type: 杂志文章,评审
doi:10.1007/s10787-007-1562-8
更新日期:2007-06-01 00:00:00
abstract::Neuropathic pain triggers a cascade of events in the sensory neurons. It is the main complication of diabetes after cardiovascular disease. Nitric oxide (NO) produced from nitric oxide synthases (NOS) is an important signaling molecule which is crucial for many physiological processes such as synaptic plasticity, neur...
journal_title:Inflammopharmacology
pub_type: 杂志文章,评审
doi:10.1007/s10787-014-0213-0
更新日期:2014-10-01 00:00:00
abstract::Kerabala (CB) is a novel ayurvedic formulation used for treating various inflammatory diseases. This formulation was made from virgin coconut oil and it comprises extracts of Sida cordifolia, coconut milk and sesame oil. The current study was performed to evaluate the anti-inflammatory action of CB on carrageenan-indu...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-016-0298-8
更新日期:2017-02-01 00:00:00
abstract::The aim of the study was to evaluate the effect of Pterocarpus marsupium (PM) on acetic acid (AA)-induced ulcerative colitis (UC) in rats. The rats were divided into five groups, each having six rats. PM extract 100 mg and 200 mg/kg was given orally to groups four and five, respectively, and standard drug sulfasalazin...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-015-0234-3
更新日期:2015-08-01 00:00:00
abstract::Central nervous system (CNS) has a completely separate immune system that communicates with the neurons by small molecules called cytokines. Cytokines are involved in many crucial processes in neuron including cell metabolism and neurotransmitter synthesis. It has been reported that cytokine imbalance is involved in t...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-013-0181-9
更新日期:2013-12-01 00:00:00
abstract::Propolis is a resinous substance collected by honeybees from leaf buds and cracks in the bark of various plants. Propolis has been reported to have immunomodulatory activity. We hypothesized that propolis would be able to reduce the disease severity of rheumatoid arthritis. We evaluated the effect of Brazilian propoli...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-011-0088-2
更新日期:2012-02-01 00:00:00
abstract:OBJECTIVE:To evaluate the potential of Azadirachta indica leaf extracts against Salmonella typhimurium-induced inflammation in BALB/c mice. DESIGN:Qualitative tests of A. indica leaf extracts were conducted for screening of various phytochemicals. The antiinflammatory potential of A. indica leaf extracts on S. typhimu...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-008-8032-9
更新日期:2009-02-01 00:00:00
abstract::Tovophyllin A (TA) is a xanthone isolated from Garcinia mangostana L. (GM, Guttiferae) pericarps that possesses various beneficial bioactivities. However, its protective effects on acute lung injury (ALI) and lung carcinoma have not yet been explored. The current work was designed to investigate the protective potenti...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-019-00609-1
更新日期:2020-02-01 00:00:00
abstract:BACKGROUND:Osthole is a bioactive component reported in medicinal plants such as Angelica pubescens and Cnidium monnieri, known for analgesic activity. However, the toxicity, median effective dose (ED50), and dual modulation of nitric oxide and cyclooxygenase pathways along with inflammatory cytokines of osthole are ye...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-018-0486-9
更新日期:2019-10-01 00:00:00
abstract::Allanblackia gabonensis (Guttiferae) is a plant used in the African traditional medicine as remedies against pain, rheumatism, inflammations. In the present work, the analgesic effect of aqueous extract has been evaluated using acetic acid, formalin, hot-plate test, tail immersion and paw-pressure test. The anti-infla...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-011-0096-2
更新日期:2013-02-01 00:00:00
abstract::2-(4-phenylquinoline-2-yl)phenol derivatives (4a-l) with COX-2 enzyme inhibition, analgesic, anti-inflammatory and antipyretic potentials were executed and reported. From the in vitro COX-2 enzyme inhibition assay, compounds 4 h (IC50 0.026 µM) and 4j (IC50 0.102 µM) were found as most potent COX-2 inhibitors. Consequ...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-017-0342-3
更新日期:2017-12-01 00:00:00
abstract::Helicobacter pylori infection, as well as NSAIDs induce oxidative stress on gastric mucosa, thereby causing mucosal damage and retarding mucosal repair. Cells can survive against chronic oxidative stress by enhancing activities of anti-oxidant enzymes, thereby protecting cells from DNA damage. Recent studies have clea...
journal_title:Inflammopharmacology
pub_type: 杂志文章,评审
doi:10.1163/156856005774423863
更新日期:2005-01-01 00:00:00
abstract::Pain is recognized as a multifactorial sensory experience that is wholly unpleasant. It can vary in intensity from mild to severe and its duration can be anything from transient to persistent. Today we know so much more about the peripheral nociceptor as the primary detection apparatus for painful stimuli. We also und...
journal_title:Inflammopharmacology
pub_type: 杂志文章,评审
doi:10.1007/s10787-009-0006-z
更新日期:2009-06-01 00:00:00
abstract::Since their development and licensing no class of drug has received as much attention both in the scientific and lay press as the cyclo-oxygenase 2 (COX-2) inhibitors. These compounds, also known as coxibs, were developed as a safer alternative to traditional non-steroidal anti-inflammatory drugs (NSAIDs) due to their...
journal_title:Inflammopharmacology
pub_type: 杂志文章,评审
doi:10.1163/156856005774415619
更新日期:2005-01-01 00:00:00
abstract::Genistein is an isoflavone with oestrogenic activity that is present in a variety of soy products as a constituent of complex mixtures of bioactive compounds, whose matrix profiles play an important role in determining the overall oestrogenic bioactivity of genistein. We review data on how the profile of soy bioactive...
journal_title:Inflammopharmacology
pub_type: 杂志文章,评审
doi:10.1007/s10787-008-8020-0
更新日期:2008-10-01 00:00:00
abstract:INTRODUCTION:Retinoic Acid Related Orphan Nuclear Receptor gamma T (RORγT) is a lineage specifying transcription factor for IL-17 expressing cells, which may contribute to the pathogenesis of Inflammatory Bowel Disease (IBD). VPR-254 is a selective in vitro inhibitor of RORγT. AIMS:The main goals of our study were two...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-019-00643-z
更新日期:2020-04-01 00:00:00
abstract::The aim of this study was to determine whether ethanol extracts of Etlingera pavieana rhizomes (EPE) can inhibit the expression of ICAM-1 and VCAM-1 in TNF-α-stimulated human vascular endothelial cells. EPE significantly reduced ICAM-1 and VCAM-1 expression in a concentration-dependent manner. EPE also suppressed phos...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-019-00676-4
更新日期:2020-12-01 00:00:00
abstract:AIM AND OBJECTIVE:6-hydroxy dopamine (6-OHDA) is a neurotoxin which on intranigral administration produces severe nigrostriatal damage with motor and cognitive deficit in animals. Curcumin (CMN) in combination with bioenhancer piperine (PP) in 6-hydroxydopamine-induced Parkinsonian rats was used to investigate the anti...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-016-0297-9
更新日期:2017-02-01 00:00:00
abstract::There is a growing body of evidence that plant polyphenols such as resveratrol, anthocyanins, catechins, and terpenes like taxol are effectively used in the treatment of chronic conditions including cancer, Alzheimer, Parkinsonism, diabetes, aging, etc. The link between oxidative stress and inflammation is well accept...
journal_title:Inflammopharmacology
pub_type: 杂志文章,评审
doi:10.1007/s10787-015-0236-1
更新日期:2015-08-01 00:00:00
abstract::The inflamed mucosa in ulcerative colitis produces high amount of prostaglandin (PG) and nitric oxide (NO) through inducible enzymes: cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS), respectively, implicating them as potential anti-inflammatory drug targets. COX-2 or iNOS-related treatments in diff...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-007-1603-3
更新日期:2007-10-01 00:00:00
abstract::Colorectal cancer (CRC) remains the most cancer type related to chronic inflammation; however, the mechanisms that link inflammation to CRC development and progression are still poorly understood. Our study aimed to investigate one of the prominent inflammatory response in cancers, iNOS/NO system. In this regard, we e...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-019-00566-9
更新日期:2019-08-01 00:00:00
abstract::The aim of this study was to investigate the effect of the nitric oxide donor isosorbide-5-mononitrate (5-ISMN) alone or in combination with the natural hepatoprotectant with anti-oxidant activity silymarin on the carbon tetrachloride (CCl(4))-induced hepatic injury in rats. 5-ISMN (1.8, 3.6 or 7.2 mg/kg), silymarin (...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-009-0027-7
更新日期:2010-04-01 00:00:00
abstract::P38 mitogen-activated protein kinase (p38 MAPK), a tissue inflammatory factor can be activated under oxidative stress and in conditions associated with hyperglycemia. Gingerol containing various natural herbs has been extensively studied for its pharmacological actions both in reducing the inflammation and as immunity...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-019-00569-6
更新日期:2019-12-01 00:00:00
abstract::R-phenylpiracetam (R-PhP, (4R)-2-(4-phenyl-2-oxopyrrolidin-1-yl)acetamide) is an optical isomer of phenotropil, a clinically-used nootropic drug that improves physical condition and cognition. Recently, R-PhP was shown to bind to the dopamine transporter (DAT). Since growing evidence suggests that dysfunction of the d...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-020-00705-7
更新日期:2020-10-01 00:00:00
abstract::The Maytenus genus is a member of the Celastraceae family. Numerous medicinal uses were assigned to species of this genus, with the use of roots, bark, and leaves for the treatment of gastric ulcers, as anti-inflammatory, analgesic, antiallergic, antitumor, among others. Several studies have demonstrated that natural ...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-018-0496-7
更新日期:2019-06-01 00:00:00
abstract::Most of the gastroprotective drugs which had been marketed in Japan were considered to have insufficient rationale for use as ulcer treatments. Such drugs may have a crucial role in maintaining mucosal integrity by the mechanisms other than inhibition of acid secretion. We re-evaluated the effect of gastroprotective d...
journal_title:Inflammopharmacology
pub_type: 杂志文章
doi:10.1007/s10787-006-0300-y
更新日期:2007-02-01 00:00:00