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 nude mice inoculated with HTC-116-luc2 cells prolonged their survival and greatly inhibited tumour growth, near to disappearance. Low concentration of gold in urine and blood were detected in mice after 48 h of administration of 5 mg/kg body weight (bw) of the gold complex and non-organ (kidney and liver) damage has been detected after gold treatment. The results obtained suggested that the thiolate gold(I) derivative shown here could be considered as a candidate for therapeutic treatment in colon cancer.

authors

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

doi

10.2174/1871520615666150129211440

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

773-82

issue

6

eissn

1871-5206

issn

1875-5992

pii

ACAMC-EPUB-64878

journal_volume

15

pub_type

杂志文章
  • Novel triazolyl berberine derivatives prepared via CuAAC click chemistry: synthesis, anticancer activity and structure-activity relationships.

    abstract::To search for novel anticancer agents, we designed and synthesized a series of new triazolyl berberine derivatives. The evaluation of all the synthesized compounds and their anticancer activities against a panel of four human cancer cell lines including MCF-7 (breast), MCF-7/ADR (breast), SW-1990 (pancreatic), SMMC-77...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:

    authors: Jin X,Yan L,Li HJ,Wang RL,Hu ZL,Jiang YY,Cao YB,Yan TH,Sun QY

    更新日期:2015-01-01 00:00:00

  • Management of elderly patients with diffuse large B-cell lymphomas.

    abstract::Life expectancy has impressively increased over the past century and the US population over 65 years is rapidly growing, especially those over 80 years. In fact, persons older than 80 years have increased by more than 250% between the years 1960 and 2000, and it is expected that the population aged >75 years will trip...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/18715206113136660363

    authors: Ciancia R,Tirelli U,Ribera J,Spina M

    更新日期:2013-11-01 00:00:00

  • Novel Pyrazolo[3,4-d]pyrimidines as Potential Cytotoxic Agents: Design, Synthesis, Molecular Docking and CDK2 Inhibition.

    abstract:BACKGROUND:Pyrazolo[3,4-d]pyrimidine scaffold was reported to possess potent cytotoxic and CDK2 inhibitory activity as analogue of roscovitine. OBJECTIVE:To design and synthesize novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidine derivatives as bioisosters of roscovitine with potential cytotoxic and CDK2 inhibitory act...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666190417153350

    authors: Maher M,Kassab AE,Zaher AF,Mahmoud Z

    更新日期:2019-01-01 00:00:00

  • Vitamin D, sunlight, and the epidemiology of prostate cancer.

    abstract::The hypothesis that vitamin D deficiency increases the risk of clinical prostate cancer has stimulated an extensive body of research. Ecologic studies have shown that mortality rates from prostate cancer are inversely correlated with levels of ultraviolet radiation, the principal source of vitamin D. Human prostate ce...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:

    authors: Schwartz GG

    更新日期:2013-01-01 00:00:00

  • Bovine serum albumin significantly improves the DPPH free radical scavenging potential of dietary polyphenols and gallic acids.

    abstract::Polyphenol-protein interaction (PPI) is reversible in that polyphenol-protein complex can be dissociated and release the free polyphenols. The aim of this study is to evaluate the contribution of polyphenol-protein interaction on improving the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging capacity of polyphe...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/187152012802650101

    authors: Cao H,Chen X,Yamamoto K

    更新日期:2012-10-01 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

  • 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

  • Platinum compounds: a hope for future cancer chemotherapy.

    abstract::The discovery of cis-platin and its second and third generation analogues created a hope in cancer chemotherapy. Cis-platin and its second generation analogue carboplatin have been used for the treatment of some cancers from a long time. The third generation analogues have superior anti-cancer profiles for curing a fe...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520611313020016

    authors: Ali I,Wani WA,Saleem K,Haque A

    更新日期:2013-02-01 00:00:00

  • Therapeutic Potentials and Mechanisms of Artemisinin and its Derivatives for Tumorigenesis and Metastasis.

    abstract:BACKGROUND:Tumor recurrence and metastasis are still leading causes of cancer mortality worldwide. The influence of traditional treatment strategies against metastatic tumors may still be limited. To search for novel and powerful agents against tumors has become a major research focus. In this study, Artemisinin (ARM),...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200120100252

    authors: Li Y,Zhou X,Liu J,Yuan X,He Q

    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

  • Oncogenic MicroRNA-27a is a target for genistein in ovarian cancer cells.

    abstract::MicroRNAs (miRNAs) are emerging as important regulators in various pathobiological processes in cancer. Genistein, as a major isoflavonoid isolated from dietary soybean, possesses a wide variety of biological activities particularly in cancer prevention. However, the molecular mechanisms by which genistein elicits its...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113139990006

    authors: Xu L,Xiang J,Shen J,Zou X,Zhai S,Yin Y,Li P,Wang X,Sun Q

    更新日期:2013-09-01 00:00:00

  • Glucosamine Protects Rat Bone Marrow Cells Against Cisplatin-induced Genotoxicity and Cytotoxicity.

    abstract:BACKGROUND AND OBJECTIVE:Glucosamine is a widely prescribed dietary supplement used in the treatment of osteoarthritis. In the present study, the chemoprotectant ability of glucosamine was evaluated against cisplatin-induced genotoxicity and cytotoxicity in rat bone marrow cells. METHODS:Glucosamine was orally adminis...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666190704164126

    authors: Cheki M,Jafari S,Najafi M,Mahmoudzadeh A

    更新日期:2019-01-01 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

  • Hydroxyl Group Difference between Anthraquinone Derivatives Regulate Different Cell Death Pathways via Nucleo-Cytoplasmic Shuttling of p53.

    abstract:BACKGROUND:Despite a number of measures having been taken for cancer management, it is still the second leading cause of death worldwide. p53 is the protein principally being targeted for cancer treatment. Targeting p53 localization may be an effective strategy in chemotherapy as it controls major cell death pathways b...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520618666181029133041

    authors: Kamil M,Haque E,Mir SS,Irfan S,Hasan A,Sheikh S,Alam S,Ansari KM,Nazir A

    更新日期:2019-01-01 00:00:00

  • The Emerging Roles of RASSF5 in Human Malignancy.

    abstract::Ras association domain family member 5 (RASSF5, also named NORE1) is an identified member of the RASSF gene family which could bind selectively to activate Ras and function as an antineoplastic effector in multiple cellular regulations. While highly expressed in majority of normal tissues, RASSF5 is epigenetically ina...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520617666170327120747

    authors: Li S,Teng J,Li H,Chen F,Zheng J

    更新日期:2018-01-01 00:00:00

  • 3-(4'-geranyloxy-3'-methoxyphenyl)-2-trans propenoic acid: a novel promising cancer chemopreventive agent.

    abstract::3-(4'-geranyloxy-3'-methoxyphenyl)-2-trans propenoic acid is a secondary metabolite biosynthetically related to ferulic acid in which a geranyl chain is attached to the phenolic group, extracted from Acronychia baueri Schott (Fam. Rutaceae). In the last five years some of the pharmacological properties of 3-(4'-gerany...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152006778699149

    authors: Curini M,Epifano F,Genovese S,Marcotullio MC,Menghini L

    更新日期:2006-11-01 00:00:00

  • Novel molecular anti-colorectalcancer conjugate:chlorambucil-adipic acid dihydrizide-glutamine.

    abstract::Cancer is one of the most fatal diseases in the world and it has been years that finding new drugs and chemotherapeutic techniques with lowest side effects become one of the most important challenging matters needs really hard efforts. Chlorambucil (CBL), an ancient direct-acting alkylating anticancer agent, is common...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113139990132

    authors: Tabasi MA,Amanlou M,Siadat SD,Nourmohammadi Z,Omoomi FD,Ebrahimi SE,Aghasadeghi MR,Rahimi P,Pourhosseini S,Mehravi B,Ardestani MS

    更新日期:2013-11-01 00:00:00

  • Updates of mTOR inhibitors.

    abstract::Mammalian target of rapamycin (mTOR) is a central controller of cell growth, proliferation, metabolism and angiogenesis. mTOR signaling is often dysregulated in various human diseases and thus attracts great interest in developing drugs that target mTOR. Currently it is known that mTOR functions as two complexes, mTOR...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152010793498663

    authors: Zhou H,Luo Y,Huang S

    更新日期:2010-09-01 00:00:00

  • In Vivo Performance of a Ruthenium-cyclopentadienyl Compound in an Orthotopic Triple Negative Breast Cancer Model.

    abstract:BACKGROUND:Ruthenium-based anti-cancer compounds are proposed as viable alternatives that might circumvent the disadvantages of platinum-based drugs, the only metallodrugs in clinical use for chemotherapy. Organometallic complexes in particular hold great potential as alternative therapeutic agents since their cytotoxi...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:

    authors: Mendes N,Tortosa F,Valente A,Marques F,Matos A,Morais TS,Tomaz AI,Gärtner F,Garcia MH

    更新日期:2017-01-01 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

  • Treatment approaches in elderly patients with head and neck cancer.

    abstract::Integration of geriatric assessment into cancer clinical practice is strongly needed in squamous cell carcinoma of the head and neck (SCCHN) due to the frequent discrepancy between chronologic and biologic age. Comprehensive Geriatric Assessment (CGA) is a multidimensional assessment tool that examines age-related dom...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/18715206113136660355

    authors: Perri F,Ionna F,Pavone E,Longo F,Caponigro F

    更新日期:2013-11-01 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

  • Natural Compounds A Weapon to Ameliorate Breast Cancer Cells: A Review.

    abstract::Breast cancer is the heterogeneous disease and leading cause of death in women, worldwide. It is generally caused by the perturbation of various signaling pathways responsible for cell apoptosis. Due to genetic variability, different signaling pathways are disrupted in different breast cancer patients; so, to overcome...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520616666160826150659

    authors: Thakur RS,Ahirwar B

    更新日期:2017-01-01 00:00:00

  • Effect of selenium-saturated bovine lactoferrin (Se-bLF) on antioxidant enzyme activities in human gut epithelial cells under oxidative stress.

    abstract::Cancer and many chronic inflammatory diseases are associated with increased amounts of reactive oxygen species (ROS). The potential cellular and tissue damage created by ROS has significant impact on many disease and cancer states and natural therapeutics are becoming essential in regulating altered redox states. We h...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/187152011797378616

    authors: Burrow H,Kanwar RK,Mahidhara G,Kanwar JR

    更新日期:2011-10-01 00:00:00

  • Exploring the Molecular Mechanism of Cinnamic Acid-Mediated Cytotoxicity in Triple Negative MDA-MB-231 Breast Cancer Cells.

    abstract:BACKGROUND:Cinnamic acid (CA), also known as 3-phenyl-2-propenoic acid, is a naturally occurring aromatic fatty acid found commonly in cinnamon, grapes, tea, cocoa, spinach and celery. Various studies have identified CA to have anti-proliferative action on glioblastoma, melanoma, prostate and lung carcinoma cells. OBJ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200807222248

    authors: Pal A,Tapadar P,Pal R

    更新日期:2020-08-07 00:00:00

  • Episensitization: therapeutic tumor resensitization by epigenetic agents: a review and reassessment.

    abstract::Resistance to chemotherapy, biological and targeted therapies is an important clinical problem. Resistance can arise and/or be selected for multiple mechanisms of action. Unfortunately, acquired resistance to antitumor agents or regimens is nearly inevitable in all patients with metastatic disease. Until recently, it ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520614666140418144610

    authors: Oronsky B,Oronsky N,Knox S,Fanger G,Scicinski J

    更新日期:2014-01-01 00:00:00

  • Preparation, Characterization and In-vitro Biological Evaluation of Novel Curcumin Derivatives as Cytotoxic and Apoptosis-Inducing Agents.

    abstract:BACKGROUND:Curcumin is a natural polyphenol and lead compound of the rhizomes of curcuma longa that it has been widely used for pharmacological activities. OBJECTIVE:In this study, series of novel derivatives of curcumin, which this group was linked to a 2-amino-4-phenylpyran-3-carbonitrile system, have been synthesiz...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666201002111205

    authors: Arjomandi OK,Almasi S,Hosseinzadeh L,Kavoosi M,Adibi H

    更新日期:2020-10-02 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

  • 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

  • Synthesis, in vitro Antiproliferative and Antiinflammatory Activities, and Kinase Inhibitory effects of New 1,3,4-triarylpyrazole Derivatives.

    abstract:BACKGROUND:Pyrazole derivatives have been reported as both anticancer and antiinflammatory agents. OBJECTIVE:This study was conducted to develop new pyrazole derivatives as potential anticancer and/or antiinflammatory agents. Their molecular mechanisms of action have been investigated. METHOD:a series of new triarylp...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:

    authors: El-Gamal MI,Abdel-Maksoud MS,Gamal El-Din MM,Shin JS,Lee KT,Yoo KH,Oh CH

    更新日期:2017-01-01 00:00:00