Alkylamino Phenol Derivative Induces Apoptosis by Inhibiting EGFR Signaling Pathway in Breast Cancer Cells.

Abstract:

BACKGROUND AND OBJECTIVE:The present study was carried out to evaluate the anticancer property of an alkylamino phenol derivative -2-((3,4-Dihydroquinolin-1(2H)-yl)(p-tolyl)methyl)phenol) (THTMP) against human breast cancer cells. The cytotoxicity of the THTMP was assessed to know its specificity towards breast cancer cells without affecting the normal cells. METHODS:The THTMP was synthesized and the cytotoxicity was assessed by MTT assay, Caspases enzyme activity, DNA fragmentation and FITC/Annexin V, AO/EtBr staining, RT-PCR and QSAR. In addition, ADME analysis was executed to understand the mode of action of THTMP. RESULTS:THTMP showed potential cytotoxic activity against the growth of MCF7 and SK-BR3 cells with the IC50 values of 87.92μM and 172.51μM, respectively. Interestingly, THTMP found to activate caspase 3 and caspase 9 enzymes in cancer cells, which are the key enzymes implicated in apoptosis. THTMP induced apoptosis in which 33% of the cells entered the late apoptotic stage after 24h of treatment. The results also revealed that the apoptotic response could be influenced by the association of THTMP with the Epidermal Growth Factor Receptor (EGFR) mediated inhibition of the Phosphatidylinositol 3-Kinase (PI3K)/S6K1 signaling pathway. In addition, docking was performed to study the binding mode of the THTMP, which shows better interaction with EGFR. The structural elucidation of THTMP by Quantitative Structure-Activity Relationship model (QSAR) and ADMET screening suggested, THTMP as an effective anticancer compound. CONCLUSION:This work strengthens the potential of a promising drug-like compound, THTMP, for the discovery of anticancer drug against breast cancer.

authors

Palanivel S,Yli-Harja O,Kandhavelu M

doi

10.2174/1871520620666200213101407

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

809-819

issue

7

eissn

1871-5206

issn

1875-5992

pii

ACAMC-EPUB-104462

journal_volume

20

pub_type

杂志文章
  • Design and Synthesis of Tetrahydroisoquinoline Derivatives as AntiAngiogenesis and Anti-Cancer Agents.

    abstract:AIM:The aim of our research work is the synthesis of tetrahydroisoquinoline derivatives as anti-Angiogenesis and anti-cancer agents. BACKGROUND:Cancer is the second leading cause of deaths in United States. The current recovery rate from the advanced treatment for the cancer is unacceptably low. Therefore, identificat...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520621666210112122913

    authors: Gangapuram M,Eyunni S,Zhang W,Redda KK

    更新日期:2021-01-12 00:00:00

  • Novel 1,3,4-Triaryl Pyrazoles: Synthesis, QSAR Studies and Cytotoxicity against Breast Cancer.

    abstract:BACKGROUND:The existence of drug-resistance and lack of selectivity encourages scientists to search for novel and more selective cytotoxic agents. OBJECTIVES:In this work, novel 1,3,4-triarylpyrazole derivatives were synthesized to study their cytotoxicity on MCF7 (human breast Cell Line). In addition, QSAR studies we...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666190207094610

    authors: Ismail MMF,Farrag AM,Harras MF

    更新日期:2019-01-01 00:00:00

  • Pharmaceutical aspects of green synthesized silver nanoparticles: A boon to cancer treatment.

    abstract:BACKGROUND:Silver nanoparticles (AgNPs) are one of the most investigated nanostructures in recent years, which gives more challenging and promising qualities in different biomedical applications. The AgNPs synthesized by the green approach provide potential healthcare benefits over chemical approaches, including improv...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200918111024

    authors: Mishra V,Nayak P,Singh M,Tambuwala MM,Aljabali AA,Chellappan DK,Dua K

    更新日期:2020-09-18 00:00:00

  • Therapeutic targeting of malignant glioma.

    abstract::Glioblastoma Multiforme (GMB) is the most aggressive primary brain tumor with poor survival rates and universal recurrence despite aggressive treatments. Recent research suggested that GBM has multiple glioma cell populations, some of which are organized in a stem cell hierarchical order with different stages of diffe...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520614666140825105145

    authors: Alexandru-Abrams D,Jadus MR,Hsu FP,Stathopoulos A,Bota DA

    更新日期:2014-01-01 00:00:00

  • VDAC1 Mediated Anticancer Activity of Gallic Acid in Human Lung Adenocarcinoma A549 Cells.

    abstract:AIMS:Gallic acid (GA) is generally distributed in a variety of plants and foods, and possesses cell growth-inhibiting activities in cancer cell lines. In the present study, the impact of GA on cell viability, apoptosis induction and possible molecular mechanisms in cultured A549 lung carcinoma cells was investigated. ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520617666170912115441

    authors: Maimaiti A,Aili A,Kuerban H,Li X

    更新日期:2018-01-01 00:00:00

  • Induction of Autophagic Cell Death in Apoptosis-resistant Pancreatic Cancer Cells using Benzo[α]phenoxazines Derivatives, 10-methyl-benzo[α]phenoxazine-5-one and benzo[α]phenoxazine-5-one.

    abstract:BACKGROUND:Intrinsic resistance to apoptotic cell death due to co-occurrence of mutated KRAS and p53 is frequently reported in pancreatic cancer that renders them aggressive, highly proliferative and metastatic. In addition, these cancer types are less sensitive to apoptosis inducing drugs where promotion of autophagic...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:

    authors: Pal S,Salunke-Gawalib S,Konkimallaa VB

    更新日期:2017-01-01 00:00:00

  • The effects of cantharidin and cantharidin derivates on tumour cells.

    abstract::Natural product extracts are a rich source of small molecules that display antitumor activity. Cantharidin, in the form of the dried body of the Chinese blister beetles: Mylabris phalerata or M. cichorii, displays antitumor activity and induces apoptosis in many types of tumor cells. Cantharidin has been used as an an...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520610909040392

    authors: Liu D,Chen Z

    更新日期:2009-05-01 00:00:00

  • Reverse Screening Bioinformatics Approach to Identify Potential Anti Breast Cancer Targets Using Thymoquinone from Neutraceuticals Black Cumin Oil.

    abstract:BACKGROUND:Functional foods, neutraceuticals and natural antioxidants have established their potential roles in the protection of human health and diseases. Thymoquinone (TQ), the main bioactive component of Nigella sativa seeds (black cumin seeds), a plant derived neutraceutical was used by ancient Egyptians because o...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666190124155359

    authors: Sundaravadivelu S,Raj SK,Kumar BS,Arumugamand P,Ragunathan PP

    更新日期:2019-01-01 00:00:00

  • Lumiflavin Enhances the Effects of Ionising Radiation on Ovarian Cancer Stem-Like Cells by Inhibiting Autophagy.

    abstract:BACKGROUND:The development of cancer stem-like cells (CSCs) is one of the main causes of ovarian cancer tolerance to radiotherapy. Autophagy is an adaptive process by which cells repair damage due to radiation. As a metabolite of riboflavin, lumiflavin can enhance the chemotherapeutic effects of cisplatin on ovarian ca...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520621999210104201907

    authors: Wu M,Huang Y,Song Z,Yang R

    更新日期:2021-01-04 00:00:00

  • Killing Glioma 'Stem-like' Cells via Drug-Induced Relocation of Endosomal Urokinase Proteins.

    abstract::High grade gliomas (HGGs) are primary CNS cancers with more than 95% of patients experiencing tumor recurrence following radiation therapy, chemotherapy, and/or an anti-angiogenic therapy. Populations of glioma 'stem-like' cells (GSCs) exist in both proliferative and non-proliferative states and are capable of tumor r...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:

    authors: Gorin FA,Pasupuleti N,Mahajan D,Dugar S

    更新日期:2017-01-01 00:00:00

  • Follow the ATP: tumor energy production: a perspective.

    abstract::As early as the 1920s, the eminent physician and chemist, Otto Warburg, nominated for a second Nobel Prize for his work on fermentation, observed that the core metabolic signature of cancer cells is a high glycolytic flux. Warburg averred that the prime mover of cancer is defective mitochondrial respiration, which dri...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520614666140804224637

    authors: Oronsky BT,Oronsky N,Fanger GR,Parker CW,Caroen SZ,Lybeck M,Scicinski JJ

    更新日期:2014-01-01 00:00:00

  • In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH2Ph)]Br.

    abstract::A physiologically stable thiolate gold(I) derivative [Au(Spyrimidine)(PTA-CH2Ph)]Br has shown inhibition in colon cancer proliferation of Caco-2/TC7, Caco-2/PD7 and HTC-116-luc2 cell lines via apoptotic pathway and S-phase arrest in the cell cycle. Intraperitoneal injection of [Au(Spyrimidine)(PTA-CH2Ph)]Br in athymic...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520615666150129211440

    authors: García-Moreno E,Gascón S,García de Jalón JA,Romanos E,Rodriguez-Yoldi MJ,Cerrada E,Laguna M

    更新日期:2015-01-01 00:00:00

  • Oxaliplapin and capecitabine (XELOX) based chemotherapy in the treatment of metastatic colorectal cancer: the right choice in elderly patients.

    abstract:PURPOSE:Elderly patients with metastatic colorectal cancer (mCRC) differ from the general population and are underrepresented in clinical trials. We, retrospectively, analyzed the safety and efficacy of XELOX regimen in the treatment of elderly patients affected by mCRC. PATIENTS AND METHODS:One-hundred-eleven consecu...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113136660347

    authors: Berretta M,Aprile G,Nasti G,Urbani M,Bearz A,Lutrino S,Foltran L,Ferrari L,Talamini R,Fiorica F,Lleshi A,Canzonieri V,Lestuzzi C,Borsatti E,Fisichella R,Tirelli U

    更新日期:2013-11-01 00:00:00

  • Protective Effects of Downregulating Estrogen Receptor Alpha Expression in Cervical Cancer.

    abstract:BACKGROUND:The cause of cervical cancer can be traced to Human Papilloma Virus (HPV) along with other, nonviral factors. The uterine cervix is reactive to hormones, and female hormones have been implicated in cervical cancer pathogenesis. Previous studies have indicated that malignant cervical cells tend to lose Estrog...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520618666180830162517

    authors: Yu P,Wang Y,Li C,Lv L,Wang J

    更新日期:2018-01-01 00:00:00

  • In Vitro Antitumor Evaluation of Some Hybrid Molecules Containing Coumarin and Quinolinone Moieties.

    abstract:BACKGROUND:Hybrid molecules furnished by merging two or more pharmacophores is an emerging concept in the field of medicinal chemistry and drug discovery. Currently, coumarin hybrids have attracted the keen attention of researchers to discover their therapeutic capability against cancer. OBJECTIVE:The present study ai...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666190930143856

    authors: Rizzk YW,El-Deen IM,Mohammed FZ,Abdelhamid MS,Khedr AIM

    更新日期:2019-01-01 00:00:00

  • Synthesis of New Benzimidazole and Benzothiazole Disulfide Metal Complexes as G-quadruplex Binding Ligands.

    abstract::Compounds that can bind and stabilize non-canonical DNA structures are named quadruplex and are of interest in anticancer drug design due to their selective inhibitions of telomerase and consequent effects on cell proliferation. In this study, we report novel Co/Cu [II] complex compounds as G-quadruplex DNA binding li...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520616666160204111637

    authors: Saour K,Lafta D

    更新日期:2016-01-01 00:00:00

  • lncRNAs as Potential Targets in Small Cell Lung Cancer: MYC -dependent Regulation.

    abstract:BACKGROUND:Small Cell Lung Cancer (SCLC) is a highly aggressive malignancy. MYC family oncogenes are amplified and overexpressed in 20% of SCLCs, showing that MYC oncogenes and MYC regulated genes are strong candidates as therapeutic targets for SCLC. c-MYC plays a fundamental role in cancer stem cell properties and ma...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200721130700

    authors: Tokgun O,Tokgun PE,Inci K,Akca H

    更新日期:2020-01-01 00:00:00

  • Novel Inhibitors of DNA Repair Enzyme TDP1 Combining Monoterpenoid and Adamantane Fragments.

    abstract:BACKGROUND AND OBJECTIVE:The DNA repair enzyme tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a current inhibition target to improve the efficacy of cancer chemotherapy. Previous studies showed that compounds combining adamantane and monoterpenoid fragments are active against TDP1 enzyme. This investigation is focused on th...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666181207094243

    authors: Mozhaitsev ES,Zakharenko AL,Suslov EV,Korchagina DV,Zakharova OD,Vasil'eva IA,Chepanova AA,Black E,Patel J,Chand R,Reynisson J,Leung IKH,Volcho KP,Salakhutdinov NF,Lavrik OI

    更新日期:2019-01-01 00:00:00

  • Chemical properties and mechanisms determining the anti-cancer action of garlic-derived organic sulfur compounds.

    abstract::Organic sulfur compounds (OSCs) derived from plants, fungi or bacteria can serve as chemopreventive and/or chemotherapeutic agents and have been attracting medical and research interest as a promising source for novel anti-cancer agents. Garlic, which has long been used as a medicinal plant in different cultures due t...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152011795347522

    authors: Cerella C,Dicato M,Jacob C,Diederich M

    更新日期:2011-03-01 00:00:00

  • Anti-resorptive Drugs and their Impact on Maxillofacial Bone among Cancer Patients.

    abstract::This article aims to give an overview on etiology, diagnosis and treatment options of osteonecrosis of the jaw bone among cancer patients receiving anti-resorptive drugs (ARDs). The physiologic bone function of continuous resorption and buildup is modified by the use of ARDs. Although ARDs proved to reduce pain and to...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520615666150325232857

    authors: Borumandi F,Aghaloo T,Cascarini L,Gaggl A,Fasanmade K

    更新日期:2015-01-01 00:00:00

  • Plant polyphenolics as anti-invasive cancer agents.

    abstract::Because invasion is, either directly or via metastasis formation, the main cause of death in cancer patients, development of efficient anti-invasive agents is an important research challenge. We have established a screening program for potentially anti-invasive compounds. The assay is based on organotypic confronting ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152008783497037

    authors: Bracke ME,Vanhoecke BW,Derycke L,Bolca S,Possemiers S,Heyerick A,Stevens CV,De Keukeleire D,Depypere HT,Verstraete W,Williams CA,McKenna ST,Tomar S,Sharma D,Prasad AK,DePass AL,Parmar VS

    更新日期:2008-02-01 00:00:00

  • Natural products targeting autophagy via the PI3K/Akt/mTOR pathway as anticancer agents.

    abstract::The phosphatidylinositol 3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) pathway is a key regulator of authophagy. Natural products show anticancer activity and often induce apoptosis or autophagy. The crosstalk between these two types of cell death makes autophagy an interesting target since drugs targetin...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/18715206113139990130

    authors: Sun H,Wang Z,Yakisich JS

    更新日期:2013-09-01 00:00:00

  • Current Progresses in Metal-based Anticancer Complexes as Mammalian TrxR Inhibitors.

    abstract::Reactive oxygen species (ROS) are produced as normal products of cellular metabolism, which are essential for numerous cell biological functions. Due to aberrant metabolism, oncogenic signaling activation and mitochondrial dysfunction, cancer cells generate excessive ROS that cause severe oxidative damage, finally lea...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520617666170213150217

    authors: Cheng Y,Qi Y

    更新日期:2017-01-01 00:00:00

  • The Effect of p53-R249S on the Suppression of Hepatocellular Carcinoma Cells Survival Induced by Podophyllum Derivatives.

    abstract:BACKGROUND:Hepatocellular Carcinoma (HCC), the second leading cause of cancer-related mortality with over half a million new cases diagnosed annually in the world, accounts for nearly 70% of cancer deaths in parts of Asia and Africa. Podophyllum, one of the important members of the lignane class of natural products der...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200218110047

    authors: Chen H,Zhang M,Wang Z,Li L,Li Q,Wang H

    更新日期:2020-01-01 00:00:00

  • Targeted small-molecule inhibitors of protein kinase B as anticancer agents.

    abstract::Protein kinase B (PKB or Akt) is a central component of the PI3K - PKB - mTOR signalling cascade and is firmly established as an attractive target for pharmacological intervention in cancer. A number of small molecule inhibitors with well-defined, direct molecular interactions with PKB are now known, covering a range ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152009787047734

    authors: Collins I

    更新日期:2009-01-01 00:00:00

  • Synthesis and biological evaluation of novel antifolate analogs as potential anticancer treatment.

    abstract::A novel process for the preparation of two ketomethylenic antifolates, 2-(2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-amino]- phenyl}-2-oxo-ethyl) pentanedioic acid and 2-(2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-methyl-amino]-phenyl}-2-oxo-ethyl) pentanedioic acid is described herein. Both compounds were compared with met...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520611313020022

    authors: Stoicescu DF,Rotaru M

    更新日期:2013-02-01 00:00:00

  • Glycosidated phospholipids - a promising group of anti-tumour lipids.

    abstract::Synthetic alkylphospholipids (APLs), exhibit similarity to the platelet-activating factor (PAF). These compounds have antiproliferative effects on tumour cells and can therefore be regarded as a new class of drugs. Unlike classic cytostatic agents, synthetic alkylphospholipids do not interfere with the DNA or the mito...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520614666140309222845

    authors: Semini G,Hildmann A,von Haefen C,Danker K

    更新日期:2014-05-01 00:00:00

  • Different Methods for Cell Viability and Proliferation Assay: Essential Tools in Pharmaceutical Studies.

    abstract:BACKGROUND AND OBJECTIVE:The ratio of live cells to total cells in a sample is a definition for cell viability or cell toxicity. The assessment of the viable cells plays a critical role in all processes of the cell culture workflows. Overall, they are used to evaluate the survival of cells and also to optimize culture ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520621999201230202614

    authors: Nozhat Z,Khalaji MS,Hedayati M,Kia SK

    更新日期:2020-12-30 00:00:00

  • Statins and protein prenylation in cancer cell biology and therapy.

    abstract::The use of statins has scaled up to become one of the most prescribed medicines in the world and have been very useful in the manegement of cardiovascular diseases and related mortality. The disclosure of their chemical structure similar to that of hydroxy methyl glutaryl-CoA (HMG-CoA) revealed their ability to compet...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152012800228715

    authors: Garcia-Ruiz C,Morales A,Fernandez-Checa JC

    更新日期:2012-05-01 00:00:00

  • A Novel Triazole Nucleoside Suppresses Prostate Cancer Cell Growth by Inhibiting Heat Shock Factor 1 and Androgen Receptor.

    abstract::A novel triazole nucleoside analogue was discovered to exhibit potent anticancer activity in prostate cancer cells via down-regulating heat shock factor 1 (HSF1) and related heat shock proteins, along with the consequential inhibition of androgen receptor (AR) expression and transactivation, arresting the cell cycle i...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520615666150617110943

    authors: Xia Y,Wang M,Beraldi E,Cong M,Zoubeidi A,Gleave M,Peng L

    更新日期:2015-01-01 00:00:00