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 aimed to evaluate the in vitro antitumor activity of a new series of hybrid molecules containing coumarin and quinolinone moieties 4 and 5 against four cancer cell lines. MATERIALS AND METHODS:A new series of hybrid molecules containing coumarin and quinolinone moieties, 4a-c and 5a-c, were synthesized and screened for their cytotoxicity against prostate PC-3, breast MCF-7, colon HCT- 116 and liver HepG2 cancer cell lines as well as normal breast Hs-371 T. RESULTS:All the synthesized compounds were assessed for their in vitro antiproliferative activity against four cancer cell lines and several compounds were found to be active. Further in vitro cell cycle study of compounds 4a and 5a revealed MCF-7 cells arrest at G2 /M phase of the cell cycle profile and induction apoptosis at pre-G1 phase. The apoptosis-inducing activity was evidenced by up-regulation of Bax protein together with the downregulation of the expression of Bcl-2 protein. The mechanism of cytotoxic activity of compounds 4a and 5a correlated to its topoisomerase II inhibitory activity. CONCLUSION:Hybrid molecules containing coumarin and quinolinone moieties represents a scaffold for further optimization to obtain promising anticancer agents.

authors

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

doi

10.2174/1871520619666190930143856

subject

Has Abstract

pub_date

2019-01-01 00:00:00

pages

2010-2018

issue

16

eissn

1871-5206

issn

1875-5992

pii

ACAMC-EPUB-101094

journal_volume

19

pub_type

杂志文章
  • In Vitro Anticancer Effects of Two New Potent Hydrazide Compounds on Leukemic Cells.

    abstract:BACKGROUND:Chronic myeloid leukemia (CML), also recognized as chronic myelogenous leukemia, is initiated in some types of blood-forming cells of the bone marrow. The therapeutic approach to CML is usually chemotherapy; however, severe side effects and complications are major problems in the clinical research. Thus, rec...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520616666160404112945

    authors: Tavakolfar S,Mousavi E,Almasirad A,Amanzadeh A,Atyabi SM,Yaghamii P,Samiee-Sadr S,Salimi M

    更新日期:2016-01-01 00:00:00

  • The design and characterization of a novel beta-casein nano-vehicle loaded with platinum anticancer drug for drug delivery.

    abstract::We developed a drug-delivery system comprising a novel platinum drug (Pt(II) complex) entrapped within β-Casein (β-CN) nanoparticles referred to as nano-vehicles. Fluorescence spectroscopy, UV-Vis spectrometry, dynamic light scattering (DLS), and scanning electron microscopy (SEM) were used to characterize the β-CN-Pt...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520614666140207123147

    authors: Divsalar A,Razmi M,Saboury AA,Seyedarabi A

    更新日期:2014-01-01 00:00:00

  • Cytotoxic Sesquiterpenes from Sonchus oleraceus.

    abstract:BACKGROUND:Sonchus oleraceus is a large and widespread plant in the world. It is edible to humans as a leaf vegetable and is also used as a folklore medicinal herb in the treatment of infections and inflammatory disease, but limited research on its chemical constituents has been done. OBJECTIVE:To isolate and identify...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200101152934

    authors: Zhang H,Wang Y,Wang S,Wang Q,Wang T,Zhu J,Liu B

    更新日期:2020-01-01 00:00:00

  • Analysis of Comparative Proteomic and Potent Targets of Peniciketal A in Human Acute Monocytic Leukemia.

    abstract:BACKGROUND:Peniciketal A (Pe-A), a spiroketal compound, shows potent anticancer activities in human acute monocytic leukemia. However, the detailed mechanisms and potent targets of Pe-A remain largely unexplored. Here, we investigated the differentially expressed proteins between the Pe-A-treated group and the control ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666190212124339

    authors: Gao X,Zhou Y,Sun H,Liu D,Zhang J,Zhang J,Liu W,Pan X

    更新日期:2019-01-01 00:00:00

  • 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

  • Artesunate enhances the antiproliferative effect of temozolomide on U87MG and A172 glioblastoma cell lines.

    abstract::As chemotherapy with temozolomide is far from providing satisfactory clinical outcomes for patients with glioblastoma, more efficient drugs and drug combinations are urgently needed. The anti-malarial artesunate was previously shown to exert a profound cytotoxic effect on various tumor cell lines including those deriv...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113136660340

    authors: Karpel-Massler G,Westhoff MA,Kast RE,Dwucet A,Nonnenmacher L,Wirtz CR,Debatin KM,Halatsch ME

    更新日期:2014-02-01 00:00:00

  • Novel molecular-targeted therapeutics for the treatment of cancer.

    abstract::Recently, intensive laboratory and preclinical studies have identified and validated therapeutic molecular targets in cancer, particularly the receptor tyrosine kinases, the intracellular pathways, and the genetic and epigenetic alterations, resulting in an unprecedented surge of novel, targeted therapies and therapeu...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152008784533099

    authors: Yasui H,Imai K

    更新日期:2008-06-01 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

  • 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

  • Overcoming Cancer Cell Drug Resistance by a Folic Acid Targeted Polymeric Conjugate of Buthionine Sulfoximine.

    abstract:BACKGROUND:Glutathione (GSH), which is the predominant low molecular weight intracellular thiol in mammals, has multiple functions, such as those of protecting against oxidative stress and detoxifying endogenous and exogenous electrophiles. High GSH levels, which have been observed in various types of tumors, have been...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666190626114641

    authors: Cilurzo F,Cristiano MC,Da Pian M,Cianflone E,Quintieri L,Paolino D,Pasut G

    更新日期:2019-01-01 00:00:00

  • Congenital Malformations Attributed to Prenatal Exposure to Cyclophosphamide.

    abstract::Cyclophosphamide (CPA) remains one of the most widely prescribed anticancer drugs. It is also used in the treatment of rheumatoid arthritis, childhood nephrotic syndrome and systemic lupus erythematosus. It is a potent immunosuppressive agent. It is commonly used in blood and bone marrow transplantation. With the grow...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520616666161206150421

    authors: Rengasamy P

    更新日期:2017-01-01 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

  • Rotundic Acid Regulates the Effects of Let-7f-5p on Caco2 Cell Proliferation.

    abstract:BACKGROUND & OBJECTIVE:Nowadays, the interaction between natural products and microRNAs provides a promising field for exploring the chemo preventive agents for various cancers.As a member of microRNAs, the expression of let-7f-5p is universally down regulated in colorectal cancer (CRC). The present study aimed to unco...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620999200730165829

    authors: Feng Y,Liu X,Han Y,Chen M,Zhang L,Hu Y,Chen L,Chen G,Li N

    更新日期:2020-07-30 00:00:00

  • Radioprotective Effects of Plants from the Lamiaceae Family.

    abstract:BACKGROUND:Edible and medicinal plants are still an interesting source of promising biologically active substances to drug discovery and development. At a time of increasing cancer incidence in the world, alleviating the bothersome side effects of radiotherapy in debilitated cancer patients is becoming an important cha...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666201029120147

    authors: Karpiński TM,Adamczak A,Ożarowski M

    更新日期:2020-10-29 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

  • Targeting sphingosine-1-phosphate receptors in cancer.

    abstract::Sphingosine 1-phosphate (S1P) is a bioactive lipid with diverse biological functions, including cell proliferation, differentiation, angiogenesis, chemotaxis, and migration. Many of the activities of S1P are mediated through five closely related G-protein-coupled receptors of the sphingosine-1-phosphate receptor famil...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152011797655041

    authors: Watters RJ,Wang HG,Sung SS,Loughran TP,Liu X

    更新日期:2011-11-01 00:00:00

  • Therapeutic Potential of Targeting PAK Signaling.

    abstract::The therapeutic potential of targeting p21-Activated Kinases (PAK1 - 6) for the treatment of cancer has recently gained traction in the biotech industry. Many pharmaceutically-viable ATP competitive inhibitors have been through different stages of pre-clinical development with only a single compound evaluated in human...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520615666150617111414

    authors: Senapedis W,Crochiere M,Baloglu E,Landesman Y

    更新日期:2016-01-01 00:00:00

  • The Use of Anthracyclines for Therapy of CNS Tumors.

    abstract::Despite being long lived, anthracyclines remain the "evergreen" drugs in clinical practice of oncology, showing a potent effect in inhibiting cell growth in many types of tumors, including brain neoplasms. Unfortunately, they suffer from a poor penetration into the brain when intravenously administered due to multidru...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520615666150407155319

    authors: da Ros M,Iorio AL,Lucchesi M,Stival A,de Martino M,Sardi I

    更新日期:2015-01-01 00:00:00

  • The cytotoxic effect of emetine and CGP-74514A studied with the hollow fiber model and ArrayScan assay in neuroendocrine tumors in vitro.

    abstract::Emetine and CGP-74514A have previously shown antitumor activity in neuroendocrine tumor cell lines. The aim of this study was to investigate the cytotoxic activity of the drugs in a three-dimensional model and to study if the mechanism of the cytotoxic activity was induction of apoptosis. An in vitro hollow fiber mode...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/187152012802650147

    authors: Larsson DE,Hassan SB,Oberg K,Granberg D

    更新日期:2012-09-01 00:00:00

  • Physiological modulation approaches to improve cancer chemotherapy : a review.

    abstract::The success of anticancer therapy is limited due to the resistance caused by tumor cells to cytotoxic agents, which interfere with the effectiveness of various chemotherapeutic agents. Several mechanisms for decreased effectiveness of anti-cancer drugs have been examined however the most widely studied mechanism is th...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/18715206113136660364

    authors: Kumar R,Kaur M,Silakari O

    更新日期:2014-06-01 00:00:00

  • Synthesis of 9-O-3-(1-piperazinyl/morpholinyl/piperidinyl)pentyl-berberines as Potential Antioxidant and Cytotoxic Agents.

    abstract::A new series of 9-O-3-(1-piperazinyl/morpholinyl/piperidinyl)pentyl-berberines has been efficiently formulated via coupling 1,5-dibromopentane with berberrubine which was obtained by treating berberine in a vacuum oven at optimum temperature and pressure. Nucleophilic substitution of a variety of substituted piperazin...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520615666151009114759

    authors: Mistry BM,Patel RV,Keum YS,Kim DH

    更新日期:2016-01-01 00:00:00

  • Garlic-derived allyl sulfides in cancer therapy.

    abstract::Garlic (Allium sativam L.) is widely used in traditional herbal remedies and alternative medicine. The potential health benefits of garlic are largely attributed to its metabolic byproducts. Extensive in vivo and in vitro studies has demonstrated that the garlic derivatives possess anti-cancer effects, but the underly...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520614666140521120811

    authors: Cao HX,Zhu KX,Fan JG,Qiao L

    更新日期:2014-01-01 00:00:00

  • First ayurvedic approach towards green drugs: anti cervical cancer-cell properties of Clerodendrum viscosum root extract.

    abstract::The concept of Ayurvedic expert guided drug discovery and development is defined and put to test systematically for the first time in literature. Western Science has explored only ~5% of the approximately 25,000 species of higher plants for drug leads. The ancient medical science of Ayurveda has however employed a muc...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113139990138

    authors: Sun C,Nirmalananda S,Jenkins CE,Debnath S,Balambika R,Fata JE,Raja KS

    更新日期:2013-12-01 00:00:00

  • Castration resistant prostate cancer (CRPC): state of the art, perspectives and new challenges.

    abstract::The rapid approval of several novel agents has given prostate cancer patients and their treating physicians many new and effective therapeutic options. Four new medical therapies were recently approved on the basis of prolonged overall survival in castration-resistant prostate cancer (CRPC) patients: sipuleucel-T, cab...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/18715206113139990077

    authors: Massari F,Maines F,Modena A,Brunelli M,Bria E,Artibani W,Martignoni G,Tortora G

    更新日期:2013-07-01 00:00:00

  • Tannic Acid Inhibits Proliferation, Migration, Invasion of Prostate Cancer and Modulates Drug Metabolizing and Antioxidant Enzymes.

    abstract::The aim of this study was to investigate the effects of plant phenolic compound tannic acid (TA) on proliferative, metastatic, invasive properties of prostate cancer (PCa) cells; PC-3 and LNCaP, as well as drug metabolizing and antioxidant enzymes. Characterization of TA was done by using FT-IR and NMR. TA dose depend...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520616666151111115809

    authors: Karakurt S,Adali O

    更新日期:2016-01-01 00:00:00

  • Design, Synthesis and Evaluation of 5-pyridin-4-yl-2-thioxo-[1,3,4]oxadiazol-3-yl Derivatives as Anti-angiogenic Agents Targeting VEGFR-2.

    abstract:BACKGROUND:Angiogenesis is physiological process in embryogenesis, organ development, endometrial vasculature in menstrual cycle and wound healing. Angiogenesis has also been associated with several pathological conditions such as cancer, arthritis, atherosclerosis, etc. Out of the many growth factor responsible for an...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:

    authors: Bhanushali U,Kalekar-Joshi S,Kulkarni-Munshi R,Yellanki S,Medishetty R,Kulkarni P,Chelakara RS

    更新日期:2017-01-01 00:00:00

  • Induction of Apoptosis by Pierisin-6 in HPV Positive HeLa and HepG2 Cancer Cells is Mediated by the Caspase-3 Dependent Mitochondrial Pathway.

    abstract:BACKGROUND:To explore the cytotoxic and apoptotic activity of the pierisin-6 protein in HPV HeLa and HepG2 cell lines. METHODS:In this study, isolation, and purification of cytotoxic Prierisin-6 from the larvae of Pieris napi by affinity column chromatography techniques. Characterization of full-length mRNA of pierisi...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666181127113848

    authors: Sarathbabu S,Marimuthu SK,Ghatak S,Vidyalakshmi S,Gurusubramanian G,Ghosh SK,Subramanian S,Zhang W,Kumar NS

    更新日期:2019-01-01 00:00:00

  • Combination of DC Vaccine and Conventional Chemotherapeutics.

    abstract::Recently mutual interactions of chemotherapy and immunotherapy have been widely accepted, and several synergistic mechanisms have been elucidated as well. Although much attention has focused on the combination of DC vaccine and chemotherapy, there are still many problems remaining to be resolved, including the optimal...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520615666150907094139

    authors: Dong W,Wei R,Shen H,Ni Y,Meng L,Du J

    更新日期:2016-01-01 00:00:00

  • 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 ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200213101407

    authors: Palanivel S,Yli-Harja O,Kandhavelu M

    更新日期:2020-01-01 00:00:00

  • Targeting base excision repair for chemosensitization.

    abstract::In both bacteria and eukaryotes the alkylated, oxidized, and deaminated bases and depurinated lesions are primarily repaired via an endogenous preventive pathway, i.e. base excision repair (BER). Radiation therapy and chemotherapy are two important modes of cancer treatment. Many of those therapeutic agents used in th...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152008784220366

    authors: Adhikari S,Choudhury S,Mitra PS,Dubash JJ,Sajankila SP,Roy R

    更新日期:2008-05-01 00:00:00