3,861 results match your criteria antiproliferative agent


Geraniol exerts its antiproliferative action by modulating molecular targets in lung and skin carcinoma cells.

Phytother Res 2021 Apr 7. Epub 2021 Apr 7.

Bioprospection and Product Development Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, India.

Geraniol, an acyclic monoterpene present in several plant species' essential oils, is utilized as a food additive. It possesses potent antiproliferative and antitumor effects ascribed to its antiinflammatory, and antioxidant properties. The study aimed to understand geraniol's mechanism in human lung and skin cancer cells by employing molecular and cell target-based assays. Read More

View Article and Full-Text PDF

A comprehensive review on α-D-Glucans: Structural and functional diversity, derivatization and bioapplications.

Carbohydr Res 2021 May 27;503:108297. Epub 2021 Mar 27.

Nuclear Agriculture and Biotechnology Division, Bhabha Atomic Research Centre (BARC), Mumbai, 400085, Maharashtra, India. Electronic address:

Glucans are the most abundant natural polysaccharides across the living kingdom with tremendous biological activities. Now a days, α-D-glucans are gaining importance as a prebiotics, nutraceuticals, immunostimulants, antiproliferative agents and biodegradable polymers in pharmaceutical and cosmetic sectors. A wide variety of bioresources including bacteria, fungi, lichens, algae, plants and animals produce α-D-glucans either as an exopolysaccharide (EPS) or a cell wall component or an energy storage polymer. Read More

View Article and Full-Text PDF

Bioinspired imidazo[1,2-a:4,5-c']dipyridines with dual antiproliferative and anti-migrative properties in human cancer cells: The SAR investigation.

Eur J Med Chem 2021 Jun 13;218:113258. Epub 2021 Feb 13.

University of Tours, Faculty of Pharmacy, EA 7502 SIMBA, 31 Avenue Monge, 37200, Tours, France. Electronic address:

Herein, we report the design, synthesis and evaluation of novel bioinspired imidazo[1,2-a:4,5c']dipyridines. The structural optimization identified four anti-proliferative compounds. Compounds 11, 18, 19 and 20 exhibited excellent anticancer activities in vitro with IC of 0. Read More

View Article and Full-Text PDF

Prolonged activity of a recombinant manganese superoxide dismutase through a formulation of polymeric multi-layer nanoassemblies targeting cancer cells.

Eur J Pharm Sci 2021 Jul 2;162:105825. Epub 2021 Apr 2.

BioChem Laboratory, Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, Via D. Montesano, 49, I-80131 Naples, Italy; Consorzio Interuniversitario INBB, Viale Medaglie d'Oro, 305, I-00136, Rome, Italy.

A new isoform of human manganese superoxide dismutase (SOD) has been recently isolated and obtained in a synthetic recombinant form and termed rMnSOD. As compared to other SODs, this isoform exhibits a dramatically improved cellular uptake and an intense antioxidant and antitumoral activity. Unfortunately, its use is severely hampered as this active pharmaceutical ingredient (API) in solution suffers from remarkable instability, which realizes as an interplay of unfolding and aggregation phenomena. Read More

View Article and Full-Text PDF

Design and synthesis of new indole containing biaryl derivatives as potent antiproliferative agents.

Bioorg Chem 2021 May 10;110:104821. Epub 2021 Mar 10.

School of Pharmaceutical Sciences & Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou 450001, PR China. Electronic address:

A new series of indole containing biaryl derivatives were designed and synthesized, and further biological evaluations of their antiproliferative activity against cancer cell lines (MGC-803 and TE-1 cells) were also conducted. Of these synthesized biaryls, compound 4-methyl-2-((5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)methyl)quinazoline (23) performed as the most potent antiproliferative agent that inhibited cell viability of MGC-803 cells with an IC value of 8.28 µM. Read More

View Article and Full-Text PDF

Antiproliferative Properties of Scandium Exopolysaccharide Complexes on Several Cancer Cell Lines.

Mar Drugs 2021 Mar 23;19(3). Epub 2021 Mar 23.

GIP ARRONAX, 1 rue Aronnax, CEDEX 3, F-44817 Nantes, France.

Antimetastatic properties on both murine and human osteosarcoma cell lines (POS-1 and KHOS) have been evidenced using exopolysaccharide (EPS) derivatives, produced by bacterium. These derivatives had no significant effect on the cell cycle neither a pro-apoptotic effect on osteosarcoma cells. Based on this observation, these EPSs could be employed as new drug delivery systems for therapeutic uses. Read More

View Article and Full-Text PDF

Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity.

Molecules 2021 Mar 25;26(7). Epub 2021 Mar 25.

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ein-Helwan, Helwan, Cairo 11795, Egypt.

Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Read More

View Article and Full-Text PDF

The Newly Synthetized Chalcone L1 Is Involved in the Cell Growth Inhibition, Induction of Apoptosis and Suppression of Epithelial-to-Mesenchymal Transition of HeLa Cells.

Molecules 2021 Mar 3;26(5). Epub 2021 Mar 3.

Department of Pharmacology, Faculty of Medicine, P. J. Safarik University, 04011 Košice, Slovakia.

Over the past decades, natural products have emerged as promising agents with multiple biological activities. Many studies suggest the antioxidant, antiangiogenic, antiproliferative and anticancer effects of chalcones and their derivatives. Based on these findings, we decided to evaluate the effects of the newly synthetized chalcone L1 in a human cervical carcinoma cell (HeLa) model. Read More

View Article and Full-Text PDF

Molecular Docking and Biophysical Studies for Antiproliferative Assessment of Synthetic Pyrazolo-Pyrimidinones Tethered with Hydrazide-Hydrazones.

Int J Mol Sci 2021 Mar 8;22(5). Epub 2021 Mar 8.

Laboratory of Heterocyclic Chemistry, Natural Products and Reactivity, Medicinal Chemistry and Natural Products (LR11ES39), Faculty of Sciences of Monastir, University of Monastir, 5000 Monastir, Tunisia.

Chemotherapy represents the most applied approach to cancer treatment. Owing to the frequent onset of chemoresistance and tumor relapses, there is an urgent need to discover novel and more effective anticancer drugs. In the search for therapeutic alternatives to treat the cancer disease, a series of hybrid pyrazolo[3,4-]pyrimidin-4()-ones tethered with hydrazide-hydrazones, -, was synthesized from condensation reaction of pyrazolopyrimidinone-hydrazide with a series of arylaldehydes in ethanol, in acid catalysis. Read More

View Article and Full-Text PDF

Hypericin-mediated photodynamic therapy for the treatment of cancer: a review.

J Pharm Pharmacol 2021 Mar;73(4):425-436

Department of Radiology, Division of Translational Nanobiomaterials and Imaging, Leiden University Medical Center, Leiden, The Netherlands.

Objectives: Hypericin is a polycyclic aromatic naphthodianthrone that occurs naturally. It is also an active ingredient in some species of the genus Hypericum. Emerging evidence suggests that hypericin has attracted great attention as a potential anticancer drug and exhibits remarkable antiproliferative effect upon irradiation on various tumour cells. Read More

View Article and Full-Text PDF

The antiproliferative effects of ataxia-telangiectasia mutated and ATM- and Rad3-related inhibitions and their enhancements with the cytotoxicity of DNA damaging agents in cholangiocarcinoma cells.

J Pharm Pharmacol 2021 Mar;73(1):40-51

Laboratory of Environmental Toxicology, Chulabhorn Research Institute, Bangkok, Thailand.

Objective: To investigate whether the inhibitions of ataxia-telangiectasia mutated (ATM) and ATM- and Rad3-related (ATR) kinases by their specific inhibitors, KU-55933 and VE-821, respectively, are able to promote the cytotoxic activity of genotoxic agents including gemcitabine, 5-Fluorouracil, cisplatin and doxorubicin, in cholangiocarcinoma (CCA) and immortalized cholangiocyte cell lines.

Methods: Cell viability of cells treated with DNA damaging agents, alone and in combination with KU-55933 and VE-821, was determined by MTT assay. The changes of cell cycle distribution were evaluated by flow cytometry analysis. Read More

View Article and Full-Text PDF

N-1, 3-Benzenedicarbonyl-Bis-(Amino Acid) and Dipeptide Candidates: Synthesis, Cytotoxic, Antimicrobial and Molecular Docking Investigation.

Drug Des Devel Ther 2021 25;15:1315-1332. Epub 2021 Mar 25.

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, 11451, Saudi Arabia.

Purpose: The objective of our work was to prepare a potent and safe antimicrobial and anticancer agents, through synthesis of several peptides and examine their biological activities, namely as, cytotoxically potent and antimicrobial and antifungal agents.

Introduction: Multidrug-resistant microbial strains have arisen against all antibiotics in clinical use. Infections caused by these bacteria threaten global public health and are associated with high mortality rates. Read More

View Article and Full-Text PDF

Discovery of Novel Benzimidazole and Indazole Analogues as Tubulin Polymerization Inhibitors with Potent Anticancer Activities.

J Med Chem 2021 04 31;64(8):4498-4515. Epub 2021 Mar 31.

School of Pharmaceutical Sciences, Guangdong Provincial Key Laboratory of New Drug Screening, Southern Medical University, Guangzhou 510515, China.

Novel indazole and benzimidazole analogues were designed and synthesized as tubulin inhibitors with potent antiproliferative activities. Among them, compound exhibited the strongest inhibitory effects on the growth of cancer cells with an average IC value of 50 nM, slightly better than colchicine. exhibited nearly equal potency against both, a paclitaxel-resistant cancer cell line (A2780/T, IC = 9. Read More

View Article and Full-Text PDF

Albendazole exerts antiproliferative effects on prostate cancer cells by inducing reactive oxygen species generation.

Oncol Lett 2021 May 18;21(5):395. Epub 2021 Mar 18.

Department of Laboratory Animal Medicine, Research Institute for Veterinary Science, BK21 PLUS Program for Creative Veterinary Science Research, College of Veterinary Medicine, Seoul National University, Seoul 08826, Republic of Korea.

Benzimidazole derivatives are used for their antihelmintic properties, but have also been reported to exert anticancer effects. In the present study, the anticancer effects of albendazole on prostate cancer cells were assessed using proliferation, clonogenic and migration assays. To investigate the anticancer mechanisms of albendazole, reactive oxygen species (ROS) levels were measured, and the expression of genes associated with oxidative stress and Wnt/β-catenin signaling was confirmed by reverse transcription-quantitative PCR and western blotting. Read More

View Article and Full-Text PDF

In pursuit of a selective hepatocellular carcinoma therapeutic agent: Novel thalidomide derivatives with antiproliferative, antimigratory and STAT3 inhibitory properties.

Eur J Med Chem 2021 May 10;217:113353. Epub 2021 Mar 10.

School of Molecular Sciences, The University of Western Australia, Crawley, WA, 6009, Australia. Electronic address:

Advanced stage liver cancer is predominantly treated with the multi-kinase inhibitor sorafenib; however, this therapeutic agent lacks selectivity in its cytotoxic actions and is associated with poor survival outcomes. Herein we report the design and preparation of several thalidomide derivatives, including a variety of novel thioether-containing forms that are especially rare in the literature. Importantly, two of the derivatives described are potent antiproliferative agents with dose-dependent selectivity for tumorigenic liver progenitor cells (LPC) growth inhibition (up to 36% increase in doubling time at 10 μM) over non-tumorigenic cells (no effect at 10 μM). Read More

View Article and Full-Text PDF

Better outcome of COVID-19 positive kidney transplant recipients during the unremitting stage with optimized anticoagulation and immunosuppression.

Clin Transplant 2021 06 12;35(6):e14297. Epub 2021 May 12.

Chest Department, Zagazig University, Zagaziz, Egypt.

Introduction: COVID-19 is an ongoing pandemic with high morbidity and mortality and with a reported high risk of severe disease in kidney transplant recipients (KTR).

Aim: We aimed to report the largest number of COVID-19-positive cases in KTR in a single center and to discuss their demographics, management, and evolution.

Methods: We enrolled all the two thousand KTR followed up in our center in Kuwait and collected the data of all COVID-19-positive KTR (104) from the start of the outbreak till the end of July 2020 and have reported the clinical features, management details, and both patient and graft outcomes. Read More

View Article and Full-Text PDF

A novel anthraquinone‑quinazoline hybrid 7B blocks breast cancer metastasis and EMT via targeting EGFR and Rac1.

Int J Oncol 2021 05 24;58(5). Epub 2021 Mar 24.

Life Sciences Institute, Guangxi Medical University, Nanning, Guangxi Zhuang Autonomous Region 530021, P.R. China.

At present, effective therapeutic drugs for triple‑negative breast cancer (TNBC) are lacking due to the absence of identified or available targets. Therefore, the present study aimed to identify key molecular targets and a specific targeted therapeutic drug to aid with the development of novel therapeutic strategies for TNBC. Based on the high expression of EGFR and Rac1 in TNBC and inspired by a novel antitumor strategy termed combi‑targeting, novel anthraquinone‑quinazoline hybrid 7B was synthesized to simultaneously target EGFR and Rac1. Read More

View Article and Full-Text PDF

Discovery and resistance mechanism of a selective CDK12 degrader.

Nat Chem Biol 2021 Jun 22;17(6):675-683. Epub 2021 Mar 22.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.

Cyclin-dependent kinase 12 (CDK12) is an emerging therapeutic target due to its role in regulating transcription of DNA-damage response (DDR) genes. However, development of selective small molecules targeting CDK12 has been challenging due to the high degree of homology between kinase domains of CDK12 and other transcriptional CDKs, most notably CDK13. In the present study, we report the rational design and characterization of a CDK12-specific degrader, BSJ-4-116. Read More

View Article and Full-Text PDF

An amide mimic of desTHPdactylolide: Total synthesis and antiproliferative evaluation.

Bioorg Med Chem Lett 2021 May 19;40:127970. Epub 2021 Mar 19.

Department of Chemistry, California State University, Fresno, 2555 E. San Ramon Avenue, M/S SB70, Fresno, CA 93740, United States. Electronic address:

(-)-Zampanolide is a unique microtubule stabilizing agent (MSA) with covalent-binding mechanism and low nanomolar anitproliferative potency towards multi-drug resistant cancer cells. MSAs have a special connection with prostate cancer by inhibiting androgen receptor nuclear translocation. Zampanolide and the structurally related dactylolide have thus been sought after by us as lead compounds for development of anti-prostate cancer agents. Read More

View Article and Full-Text PDF

OMA1520 and OMA1774, novel 1,2,4-triazole bearing analogs of combretastatin A-4, inhibit hepatocellular carcinoma: Histological and immunohistochemical studies.

Biomed Pharmacother 2021 Jun 19;138:111417. Epub 2021 Mar 19.

Medicinal Chemistry Department, Faculty of Pharmacy, Minia University, Minia, Egypt.

Combretastatin A-4 (CA-4) received significant interest as a potential anticancer agent in recent years. Several CA-4 analogs were synthesized and investigated to enhance the activity or solve the in vivo decreased activity of CA-4.

Aim: The present study aims to investigate the chemotherapeutic and the antiproliferative effects of the mono and the dual therapy of the newly synthesized CA-4 analogs OMA1520 and OMA1774 against hepatocellularcarcinoma (HCC) induced in male adult rats by N-methylnitrosourea (MNU). Read More

View Article and Full-Text PDF

Synthesis, biological evaluation, and docking studies of novel pyrrolo[2,3-b]pyridine derivatives as both ectonucleotide pyrophosphatase/phosphodiesterase inhibitors and antiproliferative agents.

Eur J Med Chem 2021 May 10;217:113339. Epub 2021 Mar 10.

Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad, 22060, Pakistan. Electronic address:

Ecto-nucleotide pyrophosphatases/phosphodiesterases (NPPs) together with nucleoside triphosphate diphosphohydrolases (NTPDases) and alkaline phosphatases (APs) are nucleotidases located at the surface of the cells. NPP1 and NPP3 are important members of NPP family that are known as druggable targets for a number of disorders such as impaired calcification, type 2 diabetes, and cancer. Sulfonylurea derivatives have been reported as antidiabetic and anticancer agents, therefore, we synthesized and investigated series of sulfonylurea derivatives 1a-m possessing pyrrolo[2,3-b]pyridine core as inhibitors of NPP1 and NPP3 isozymes that are over-expressed in cancer and diabetes. Read More

View Article and Full-Text PDF

Folic acid-hydrophilic polymer coated mesoporous silica nanoparticles target doxorubicin delivery.

Pharm Dev Technol 2021 Jun 5;26(5):582-591. Epub 2021 Apr 5.

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan.

Mesoporous silica nanoparticles (MSNs) gained significant attention, particularly in the pharmaceutical field. Folic acid (FA) shows marked promise as a targeting agent for its specific interaction with the folate receptor. This receptor is over-expressed on the cell surface of several cancerous cells like breast cancer. Read More

View Article and Full-Text PDF

Discovery of MTR-106 as a highly potent G-quadruplex stabilizer for treating BRCA-deficient cancers.

Invest New Drugs 2021 Mar 12. Epub 2021 Mar 12.

Division of Anti-Tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica,, Chinese Academy of Sciences, Shanghai, 201203, China.

G-quadruplexes (G4s) are DNA or RNA structures formed by guanine-rich repeating sequences. Recently, G4s have become a highly attractive therapeutic target for BRCA-deficient cancers. Here, we show that a substituted quinolone amide compound, MTR-106, stabilizes DNA G-quadruplexes in vitro. Read More

View Article and Full-Text PDF

Miconazole induces autophagic death in glioblastoma cells via reactive oxygen species-mediated endoplasmic reticulum stress.

Oncol Lett 2021 Apr 25;21(4):335. Epub 2021 Feb 25.

Department of Microbiology, School of Medicine, Keimyung University, Dalseogu, Daegu 42601, Republic of Korea.

Miconazole is an antifungal agent that is used for the treatment of superficial mycosis. However, recent studies have indicated that miconazole also exhibits potent anticancer effects in various types of cancer via the activation of apoptosis. The main aim of the present study was to observe the effect of miconazole on autophagic cell death of cancer cells. Read More

View Article and Full-Text PDF

Suppression of molecular targets and antiproliferative effect of citronellal in triple-negative breast cancer cells.

Curr Mol Pharmacol 2021 Mar 9. Epub 2021 Mar 9.

Bioprospection and Product Development Division, Biotechnology Division, CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow 226015, Uttar Pradesh. India.

Background: Triple-negative breast cancer (TNBC) requires targeted therapies to better manage and prevent metastatic mammary gland tumors. Due to the resistance problem associated with the approved drugs, researchers are now focusing on phytochemicals for the treatment of TNBC as they possess a pleiotropic mode of action and fewer side effects.

Objective: To investigate the antiproliferative effect of citronellal in triple negative breast cancer cells. Read More

View Article and Full-Text PDF

The Multi-Level Mechanism of Action of a Pan-Ras Inhibitor Explains its Antiproliferative Activity on Cetuximab-Resistant Cancer Cells.

Front Mol Biosci 2021 17;8:625979. Epub 2021 Feb 17.

Department of Biotechnology and Biosciences, University of Milan-Bicocca, Milan, Italy.

Ras oncoproteins play a crucial role in the onset, maintenance, and progression of the most common and deadly human cancers. Despite extensive research efforts, only a few mutant-specific Ras inhibitors have been reported. We show that cmp4-previously identified as a water-soluble Ras inhibitor- targets multiple steps in the activation and downstream signaling of different Ras mutants and isoforms. Read More

View Article and Full-Text PDF
February 2021

Synthesis and Biological Evaluation of 1-(Diarylmethyl)-1-1,2,4-triazoles and 1-(Diarylmethyl)-1-imidazoles as a Novel Class of Anti-Mitotic Agent for Activity in Breast Cancer.

Pharmaceuticals (Basel) 2021 Feb 22;14(2). Epub 2021 Feb 22.

School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, Trinity Biomedical Sciences Institute, 152-160 Pearse Street, Dublin 2, DO2R590 Dublin, Ireland.

We report the synthesis and biochemical evaluation of compounds that are designed as hybrids of the microtubule targeting benzophenone phenstatin and the aromatase inhibitor letrozole. A preliminary screening in estrogen receptor (ER)-positive MCF-7 breast cancer cells identified 5-((2-1,2,3-triazol-1-yl)(3,4,5-trimethoxyphenyl)methyl)-2-methoxyphenol as a potent antiproliferative compound with an IC value of 52 nM in MCF-7 breast cancer cells (ER+/PR+) and 74 nM in triple-negative MDA-MB-231 breast cancer cells. The compounds demonstrated significant G/M phase cell cycle arrest and induction of apoptosis in the MCF-7 cell line, inhibited tubulin polymerisation, and were selective for cancer cells when evaluated in non-tumorigenic MCF-10A breast cells. Read More

View Article and Full-Text PDF
February 2021

Dipeptides of -Substituted Dehydrocysteine as Artzyme Building Blocks: Synthesis, Complexing Abilities and Antiproliferative Properties.

Int J Mol Sci 2021 Feb 22;22(4). Epub 2021 Feb 22.

Department of Bioorganic Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.

Background: Dehydropeptides are analogs of peptides containing at least one conjugate double bond between α,β-carbon atoms. Its presence provides unique structural properties and reaction centre for chemical modification. In this study, the series of new class of dipeptides containing -substituted dehydrocysteine with variety of heterocyclic moieties was prepared. Read More

View Article and Full-Text PDF
February 2021

LvHemB1, a novel cationic antimicrobial peptide derived from the hemocyanin of Litopenaeus vannamei, induces cancer cell death by targeting mitochondrial voltage-dependent anion channel 1.

Cell Biol Toxicol 2021 Feb 25. Epub 2021 Feb 25.

Institute of Marine Sciences and Guangdong Provincial Key Laboratory of Marine Biotechnology, Shantou University, Shantou, 515063, China.

Current cancer treatment regimens such as chemotherapy and traditional chemical drugs have adverse side effects including the appearance of drug-resistant tumor cells. For these reasons, it is imperative to find novel therapeutic agents that overcome these factors. To this end, we explored a cationic antimicrobial peptide derived from Litopenaeus vannamei hemocyanin (designated LvHemB1) that induces cancer cell death, but sparing normal cells. Read More

View Article and Full-Text PDF
February 2021

Grzybowski's Generalized Eruptive Keratoacanthomas in a Patient with Terminal Kidney Disease-An Unmet Medical Need Equally Ameliorated by Topical Imiquimod Cream and Lapacho Tea Wraps: A Case Report.

Dermatol Ther (Heidelb) 2021 Apr 23;11(2):625-638. Epub 2021 Feb 23.

Department of Dermatology and Allergy, University Hospital Bonn, Venusberg Campus 1, 53127, Bonn, Germany.

Introduction: Development of singular keratoacanthoma (KA) is generally considered a benign condition as it has a tendency to regress spontaneously in spite of histological similarity to squamous cell carcinoma. Most KAs undergo excision to rule out differential diagnoses. Several alternative treatment modalities (keratinolytic, ablative, immunomodulating, antiproliferative, or targeted therapy) have been described in the past with varying success, underlining the therapeutic challenges associated with large or multiple lesions. Read More

View Article and Full-Text PDF