26,275 results match your criteria novel anticancer

Targeted Restriction of Viral Gene Expression and Replication by the ZAP Antiviral System.

Annu Rev Virol 2021 Jun 15. Epub 2021 Jun 15.

Department of Infectious Diseases, School of Immunology & Microbial Sciences, King's College London, London SE1 9RT, United Kingdom; email:

The zinc finger antiviral protein (ZAP) restricts the replication of a broad range of RNA and DNA viruses. ZAP directly binds viral RNA, targeting it for degradation and inhibiting its translation. While the full scope of RNA determinants involved in mediating selective ZAP activity are unclear, ZAP binds CpG dinucleotides, dictating at least part of its target specificity. Read More

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Discovery of novel furo[2,3-d]pyrimidin-2-one-1,3,4-oxadiazole hybrid derivatives as dual antiviral and anticancer agents that induce apoptosis.

Arch Pharm (Weinheim) 2021 Jun 15:e2100146. Epub 2021 Jun 15.

Laboratory of Biomolecular and Medicinal Chemistry, Chemistry Department, Faculty of Science Semlalia, University Cadi Ayyad, Marrakesh, Morocco.

A new series of furo[2,3-d]pyrimidine-1,3,4-oxadiazole hybrid derivatives were synthesized via an environmentally friendly, multistep synthetic tool and a one-pot Songoashira-heterocyclization protocol using, for the first time, nanostructured palladium pyrophosphate (Na PdP O ) as a heterogeneous catalyst. Compounds 9a-c exhibited broad-spectrum activity with low micromolar EC values toward wild and mutant varicella-zoster virus (VZV) strains. Compound 9b was up to threefold more potent than the reference drug acyclovir against thymidine kinase-deficient VZV strains. Read More

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Inhibition of translation initiation factor eIF4a inactivates heat shock factor 1 (HSF1) and exerts anti-leukemia activity in AML.

Leukemia 2021 Jun 14. Epub 2021 Jun 14.

Department of Leukemia, Section of Molecular Hematology and Therapy, The University of Texas MD Anderson Cancer Center, Houston, TX, USA.

Eukaryotic initiation factor 4A (eIF4A), the enzymatic core of the eIF4F complex essential for translation initiation, plays a key role in the oncogenic reprogramming of protein synthesis, and thus is a putative therapeutic target in cancer. As important component of its anticancer activity, inhibition of translation initiation can alleviate oncogenic activation of HSF1, a stress-inducible transcription factor that enables cancer cell growth and survival. Here, we show that primary acute myeloid leukemia (AML) cells exhibit the highest transcript levels of eIF4A1 compared to other cancer types. Read More

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Novel Benzyloxyphenyl Pyrimidine-5-Carbonitrile Derivatives as Potential Apoptotic Antiproliferative Agents.

Anticancer Agents Med Chem 2021 Jun 11. Epub 2021 Jun 11.

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519. Egypt.

Background: Pyrimidine-5-carbonitrile had a broad spectrum of biological activities such as antiviral, antioxidant and anticancer activity. Among similar compounds, monastrol being the most prominent due to cell-permeant inhibitor of mitosis therefore, we investigated the new Pyrimidine-5-carbonitrile as a cytotoxic agent for p53 pathway.

Objective: Several new benzyloxyphenyl pyrimidine-5-carbonitrile derivatives were designed, synthesized, characterized, and their cytotoxicity was evaluated. Read More

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From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity.

Bioorg Med Chem 2021 Jun 5;42:116266. Epub 2021 Jun 5.

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City 11884, Cairo, Egypt; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Horus University - Egypt, International Coastal Road, 34518 New Damietta, Egypt. Electronic address:

Inhibition of PCAF bromodomain has been validated as a promising strategy for the treatment of cancer. In this study, we report the bioisosteric modification of the first reported potent PCAF bromodomain inhibitor, L-45 to its triazoloquinazoline bioisosteres. Accordingly, three new series of triazoloquinazoline derivatives were designed, synthesized, and assessed for their anticancer activity against a panel of four human cancer cells. Read More

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A One-Two-Three Multifunctional System for Enhanced Imaging and Detection of Intracellular MicroRNA and Chemogene Therapy.

ACS Appl Mater Interfaces 2021 Jun 14. Epub 2021 Jun 14.

Weifang Customs, Yuqing East Street, No.15789, High tech District, Weifang 261000, Shandong Province, China.

Simultaneous imaging, diagnosis, and therapy can offer an effective strategy for cancer treatment. However, the complex probe design, poor drug release efficiency, and multidrug resistance remain tremendous challenges to cancer treatment. Here, a novel one-two-three system is built for enhanced imaging and detection of miRNA-21 (miR-21) overexpressed in cancer cell and chemogene therapy. Read More

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β-Carboline-based molecular hybrids as anticancer agents: a brief sketch.

RSC Med Chem 2021 May 24;12(5):730-750. Epub 2021 Mar 24.

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER) Hyderabad 500037 India

Cancer is a huge burden on the healthcare system and is foremost cause of mortality across the globe. Among various therapeutic strategies, chemotherapy plays an enormous role in overcoming the challenges of treating cancer, especially in late stage detection. However, limitations such as extreme side/adverse effects and drug resistance associated with available drugs have impelled the development of novel chemotherapeutic agents. Read More

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Proteomic Analysis Reveals That Metformin Suppresses PSMD2, STIP1, and CAP1 for Preventing Gastric Cancer AGS Cell Proliferation and Migration.

ACS Omega 2021 Jun 26;6(22):14208-14219. Epub 2021 May 26.

Genome and Systems Biology Degree Program, Academia Sinica and National Taiwan University, Taipei 10617, Taiwan.

Metformin is one of the most widely used anti-diabetic drugs in type-II diabetes treatment. The mechanism of decreasing blood glucose is believed to suppress hepatic gluconeogenesis by increasing muscular glucose uptake and insulin sensitivity. Recent studies suggest that metformin may reduce cancer risk; however, its anticancer mechanism in gastric cancers remains unclear. Read More

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G2/M Checkpoint Abrogation With Selective Inhibitors Results in Increased Chromatid Breaks and Radiosensitization of 82-6 hTERT and RPE Human Cells.

Front Public Health 2021 28;9:675095. Epub 2021 May 28.

Institute of Medical Radiation Biology, Medical School, University of Duisburg-Essen, Essen, Germany.

While technological advances in radiation oncology have led to a more precise delivery of radiation dose and a decreased risk of side effects, there is still a need to better understand the mechanisms underlying DNA damage response (DDR) at the DNA and cytogenetic levels, and to overcome tumor resistance. To maintain genomic stability, cells have developed sophisticated signaling pathways enabling cell cycle arrest to facilitate DNA repair via the DDR-related kinases and their downstream targets, so that DNA damage or DNA replication stress induced by genotoxic therapies can be resolved. ATM, ATR, and Chk1 kinases are key mediators in DDR activation and crucial factors in treatment resistance. Read More

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QTMP, a Novel Thiourea Polymer, Causes DNA Damage to Exert Anticancer Activity and Overcome Multidrug Resistance in Colorectal Cancer Cells.

Front Oncol 2021 28;11:667689. Epub 2021 May 28.

School of Life Science and Technology, China Pharmaceutical University, Nanjing, China.

Colorectal cancer (CRC) is one of the most common malignancies, and multidrug resistance (MDR) severely restricts the effectiveness of various anticancer drugs. Therefore, the development of novel anticancer drugs for the treatment of CRC patients with MDR is necessary. Quaternized thiourea main-chain polymer (QTMP) is a self-assembled nanoparticle with good water solubility. Read More

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Metallodrugs are unique: opportunities and challenges of discovery and development.

Chem Sci 2020 Nov 12;11(48):12888-12917. Epub 2020 Nov 12.

Department of Chemistry, University of Warwick Gibbet Hill Road Coventry CV4 7AL UK

Metals play vital roles in nutrients and medicines and provide chemical functionalities that are not accessible to purely organic compounds. At least 10 metals are essential for human life and about 46 other non-essential metals (including radionuclides) are also used in drug therapies and diagnostic agents. These include platinum drugs (in 50% of cancer chemotherapies), lithium (bipolar disorders), silver (antimicrobials), and bismuth (broad-spectrum antibiotics). Read More

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November 2020

Traditional Herbal Medicines, Bioactive Metabolites, and Plant Products Against COVID-19: Update on Clinical Trials and Mechanism of Actions.

Front Pharmacol 2021 28;12:671498. Epub 2021 May 28.

Pharmacology Department, Medical Faculty, Universiti Kebangsaan Malaysia (The National University of Malaysia), Kuala Lumpur, Malaysia.

SARS-CoV-2 is the latest worldwide pandemic declared by the World Health Organization and there is no established anti-COVID-19 drug to combat this notorious situation except some recently approved vaccines. By affecting the global public health sector, this viral infection has created a disastrous situation associated with high morbidity and mortality rates along with remarkable cases of hospitalization because of its tendency to be high infective. These challenges forced researchers and leading pharmaceutical companies to find and develop cures for this novel strain of coronavirus. Read More

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Endophytic microbes from Nigerian ethnomedicinal plants: a potential source for bioactive secondary metabolites-a review.

Bull Natl Res Cent 2021 8;45(1):103. Epub 2021 Jun 8.

Department of Pharmaceutical Microbiology and Biotechnology, Faculty of Pharmacy, University of Lagos, Lagos, Nigeria.

Background: Endophytes are highly beneficial species of microbes that live in symbiosis with plant tissues in the setting. Endophytes are difficult to isolate in their natural environment, and they are understudied despite being a rich source of bioactive molecules. There are varieties of new infectious diseases emerging across the world, necessitating a constant and expanded search for newer and more efficient bioactive molecules. Read More

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Anticancer, antioxidant, and hepatoprotective activity of , C.B. clarke (qust) on human hepatoma cell line.

J Cancer Res Ther 2021 Apr-Jun;17(2):499-503

Department of Interdisciplinary Sciences, Faculty of Natural Sciences, Jamia Millia Islamia, New Delhi, India.

Background: Liver cancer is considered as one of the most widespread malignancies across the globe. According to a recent estimate, about 782,000 people were diagnosed with liver cancer, out of which 746,000 people died. Conventional anticancer therapy cannot fulfill all the clinical needs due to accessibility, clinical efficacy, and safety issues. Read More

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Evaluation of antiangiogenic and antiproliferative potential of ethanolic extracts of using and assays.

J Cancer Res Ther 2021 Apr-Jun;17(2):484-490

Department of Pharmacology, Sri Ramachandra Medical College, Sri Ramachandra Institute of Higher Education And Research (Deemed University), Porur, Chennai, Tamil Nadu, India.

Introduction: Andrographis echioides is a prevalently used medicinal herb in South Asian countries. Scientific researches with the extracts of A. echioides revealed its antipyretic, anti-inflammatory, antimicrobial, ulceroprotective, and hepatoprotective properties. Read More

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Novel CD123 polyaptamer hydrogel edited by Cas9/sgRNA for AML-targeted therapy.

Drug Deliv 2021 Dec;28(1):1166-1178

Department of Neonatology, the First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, Shaanxi, China.

CD123 targeting molecules have been widely applied in acute myelocytic leukemia (AML) therapeutics. Although antibodies have been more widely used as targeting molecules, aptamer have unique advantages for CD123 targeting therapy. In this study, we constructed an aptamer hydrogel termed as SSFH which could be precisely cut by Cas9/sgRNA for programmed SS30 release. Read More

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December 2021

Combination prostate cancer therapy: Prostate-specific membranes antigen targeted, pH-sensitive nanoparticles loaded with doxorubicin and tanshinone.

Drug Deliv 2021 Dec;28(1):1132-1140

Department of Pharmacy, Municipal Hospital of Zaozhuang, Zaozhuang, P. R. China.

Prostate cancer is the second most frequently diagnosed cancer in the men population. Combination anticancer therapy using doxorubicin (DOX) and another extract of traditional Chinese medicine is one nano-sized drug delivery system promising to generate synergistic anticancer effects, maximize the treatment effect, and overcome multi-drug resistance. The purpose of this study is to construct a drug delivery system for the co-delivery of DOX and tanshinones (TAN). Read More

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December 2021

Synthesis, biological evaluation, and molecular docking analysis of novel linker-less benzamide based potent and selective HDAC3 inhibitors.

Bioorg Chem 2021 Jun 4;114:105050. Epub 2021 Jun 4.

Epigenetic Research Laboratory, Department of Pharmacy, BITS-Pilani, Hyderabad Campus, Shamirpet, Hyderabad 500078, India. Electronic address:

A series of novel linker-less benzamides with different aryl and heteroaryl cap groups have been designed, synthesized, and screened as potent histone deacetylase (HDAC) inhibitors with promising anticancer activity. Two lead compounds 5e and 5f were found as potent and highly selective HDAC3 inhibitors over other Class-I HDACs and HDAC6. Compound 5e bearing a 6-quinolinyl moiety as the cap group was found to be a highly potent HDAC3 inhibitor (IC = 560 nM) and displayed 46-fold selectivity for HDAC3 over HDAC2, and 33-fold selectivity for HDAC3 over HDAC1. Read More

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Tea tree oil extract causes mitochondrial superoxide production and apoptosis as an anticancer agent, promoting tumor infiltrating neutrophils cytotoxic for breast cancer to induce tumor regression.

Biomed Pharmacother 2021 Jun 11;140:111790. Epub 2021 Jun 11.

School of Pharmacy and Medical Science, Menzies Health Institute of Queensland, Griffith University, Gold Coast Campus, Southport, Queensland 4222, Australia. Electronic address:

The antitumor activity of the tea tree oil (TTO) derived product, Melaleuca Alternifolia Concentrate (MAC) was characterized mechanistically at the molecular and cellular level. MAC was analyzed for its anticancer activity against human prostate (LNCaP) and breast (MCF-7) cancer cell lines growing in vitro. MAC (0. Read More

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Urinary exosomes-based Engineered Nanovectors for Homologously Targeted Chemo-Chemodynamic Prostate Cancer Therapy via abrogating IGFR/AKT/NF-kB/IkB signaling.

Biomaterials 2021 Jun 4;275:120946. Epub 2021 Jun 4.

School of Biomedical Engineering, Shanghai Jiao Tong University, Shanghai, 200240, PR China; Institute of Nano Biomedicine and Engineering, Shanghai Engineering Research Centre for Intelligent Diagnosis and Treatment Instrument, Department of Instrument Science and Engineering, School of Electronic Information and Electrical Engineering, Shanghai Jiao Tong University, 800 Dongchuan RD, Shanghai, 200240, PR China. Electronic address:

Multi-functional nanovectors based on exosomes from cancer cell culture supernatants in vitro has been successfully utilized for tumor-specific targeting and immune escape. However, the labor-intensive purification procedures for rich-dose and high-purity homogeneous exosomes without using targeting ligands are still a challenging task. Herein, we developed a nanovector Exo-PMA/[email protected] through cloaked by urinary exosome membrane as a chemo/chemodynamic theranostic nano-platform for targeted homologous prostate cancer therapy which pertain to the abrogation of Epidermal Growth Factor Receptor (EGFR) and its downstream AKT/NF-kB/IkB signaling instead of ERK signaling cascades. Read More

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A multiple environment-sensitive prodrug nanomicelle strategy based on chitosan graftomer for enhanced tumor therapy of gambogic acid.

Carbohydr Polym 2021 Sep 20;267:118229. Epub 2021 May 20.

School of Pharmacy, Xuzhou Medical University, Xuzhou 221004, China.

A novel multiple environment-sensitive polymeric prodrug of gambogic acid (GA) based on chitosan graftomer was fabricated for cancer treatment. Folic acid-chitosan conjugates was complexed with thermosensitive amine terminated poly-N-isopropylacrylamide (NH-PNIPAM) to develop FA-CSPN. Gambogic acid was conjugated with the graftomer via esterification to achieve high drug-loading capacity and controlled drug release. Read More

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September 2021

Liposomal Delivery of Cyclocreatine Impairs Cancer Cell Bioenergetics Mediating Apoptosis.

Methods Mol Biol 2021 ;2275:173-186

Department of Pharmaceutical Sciences, College of Pharmacy-Glendale Campus, Midwestern University, Glendale, AZ, USA.

Creatine kinase (CK) enzyme overexpression has been suggested to play a role in the process of tumorigenesis and metastasis. Cyclocreatine (CCR) is a substrate analog of creatine kinase (CK), where its phosphorylated form is a poor phosphate donor in comparison with native bioenergetic molecule, creatine phosphate (Cr-P). The compound CCR has been shown to markedly inhibit the growth of a broad spectrum of cancers, both in vitro and in vivo. Read More

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January 2021

Monitoring the mechanism of anti-cancer agents to inhibit colorectal cancer cell proliferation: Enzymatic biosensing of glucose combined with molecular docking.

Enzyme Microb Technol 2021 Aug 21;148:109804. Epub 2021 Apr 21.

Department of Biology, Faculty of Science, Yazd University, Yazd, Iran.

Glucose, a major energy source in cellular metabolism, has a significant role in cell growth. The increase in glucose uptake is a distinguishing hallmark in cancer cells. A key step in glucose utilization is the transport of glucose to the cancer cells for supplying their additional energy. Read More

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Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.

Bioorg Med Chem 2021 Jun 8;42:116251. Epub 2021 Jun 8.

Sharjah Institute for Medical Research, University of Sharjah, Sharjah 27272, United Arab Emirates; College of Pharmacy, University of Sharjah, Sharjah 27272, United Arab Emirates. Electronic address:

Selective inhibition of histone deacetylases (HDACs) is an important strategy in the field of anticancer drug discovery. However, lack of inhibitors that possess high selectivity toward certain HDACs isozymes is associated with adverse side effects that limits their clinical applications. We have initiated a collaborative initiatives between multi-institutions aimed at the discovery of novel and selective HDACs inhibitors. Read More

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Synthesis and biological evaluation of chalcone-polyamine conjugates as novel vectorized agents in colorectal and prostate cancer chemotherapy.

Eur J Med Chem 2021 May 28;222:113586. Epub 2021 May 28.

Université de Limoges, Laboratoire PEIRENE EA 7500, Faculté de Pharmacie, 2 Rue Du Dr Marcland, 87025, Limoges Cedex, France. Electronic address:

The aim of this study was to synthesize chalcone-polyamine conjugates in order to enhance bioavailability and selectivity of chalcone core towards cancer cells, using polyamine-based vectors. Indeed, it is well-known that polyamine transport system is upregulated in tumor cells. 3',4,4',5'-tetramethoxychalcone was selected as parent chalcone since it was found to be an efficient anti-proliferative agent on various cancer cells. Read More

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Halting colorectal cancer metastasis via novel dual nanomolar MMP-9/MAO-A quinoxaline-based inhibitors; design, synthesis, and evaluation.

Eur J Med Chem 2021 May 29;222:113558. Epub 2021 May 29.

Chemistry Department, Faculty of Science, Alexandria University, P.O. Box 426, Alexandria, 21321, Egypt; Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia. Electronic address:

Matrix metalloproteinase-9 (MMP-9) and monoamine oxidase-A (MAO-A) are central signaling nodes in CRC and promotors of distant metastasis associated with high mortality rates. Novel series of quinoxaline-based dual MMP-9/MAO-A inhibitors were synthesized to suppress CRC progression. The design rationale combines the thematic pharmacophoric features of MMP-9 and MAO-A inhibitors in hybrid scaffolds. Read More

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Ethnomedicinal uses, phytochemistry, pharmacological activities and toxicological profile of Glycosmis pentaphylla (Retz.) DC.: A review.

J Ethnopharmacol 2021 Jun 8;278:114313. Epub 2021 Jun 8.

Department of Pharmacy, International Islamic University Chittagong, Chittagong, 4318, Bangladesh; Faculty of Pharmacy, Universiti Kebangsaan Malaysia, 50300, Kuala Lumpur, Malaysia. Electronic address:

Ethnopharmacological Relevance: Glycosmis pentaphylla (Retz.) DC. is a perennial shrub indigenous to the tropical and subtropical regions of India, China, Sri Lanka, Myanmar, Bangladesh, Indonesia, Malaysia, Thailand, Vietnam, Philippine, Java, Sumatra, Borneo and Australia. Read More

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Lipid, Polymeric, Inorganic-based Drug Delivery Applications for Platinum-based Anticancer Drugs.

Int J Pharm 2021 Jun 8:120788. Epub 2021 Jun 8.

Centro de Química Inorgánica, CEQUINOR (CONICET-UNLP), Bv. 120 1465, La Plata, Argentina. Electronic address:

The three main FDA-approved platinum drugs in chemotherapy such as carboplatin, cisplatin, and oxaliplatin are extensively applied in cancer treatments. Although the clinical applications of platinum-based drugs are extremely effective, their toxicity profile restricts their extensive application. Therefore, recent studies focus on developing new platinum drug formulations, expanding the therapeutic aspect. Read More

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Synthesis and antiproliferative screening of novel doubly modified colchicines containing urea, thiourea and guanidine moieties.

Bioorg Med Chem Lett 2021 Jun 8;47:128197. Epub 2021 Jun 8.

Department of Medical Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland. Electronic address:

A new series of 10-demethoxy-10-methylaminocolchicines bearing urea, thiourea or aguanidine moieties at position C7 has been designed, synthesized and evaluated for in vitro anticancer activity against different cancer cell lines (A549, MCF-7, LoVo, LoVo/DX). The majority of the new derivatives were active in the nanomolar range and were characterized by lower IC values than cisplatin or doxorubicin. Two ureas (4 and 8) and thioureas (19 and 25) were found to be good antiproliferative agents (low IC values and high SI) and could prove to be promising candidates for further research in the field of anticancer drugs based on the colchicine skeleton. Read More

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Spiraeoside extracted from red onion skin ameliorates apoptosis and exerts potent antitumor, antioxidant and enzyme inhibitory effects.

Food Chem Toxicol 2021 Jun 8;154:112327. Epub 2021 Jun 8.

Department of Stem Cell and Regenerative Biotechnology, Konkuk University, Seoul 05029, Republic of Korea. Electronic address:

Red onion skin waste (ROSW) was analyzed for extraction of naturally occurring 4'-O-glucoside of quercetin, spiraeoside (SPI) with promising biological activities. Reversed-phase high-performance liquid chromatography was used to determine the SPI content in three different solvent extracts of ROSW: water (12.2 mg/g), methanol (27. Read More

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