18,895 results match your criteria activity mcf-7


Synthesis of messagenin and platanic acid chalcone derivatives and their biological potential.

Nat Prod Res 2021 May 10:1-10. Epub 2021 May 10.

Organic Chemistry, Martin-Luther-University Halle-Wittenberg, Halle (Saale), Germany.

The chalcone derivatives of 20-oxo-lupanes have been synthesised and screened for some types of biological activity. Ozonolysis of lupanes afforded 20-oxo-derivatives with the following condensation using different aromatic aldehydes by Claisen‒Schmidt reaction to the target compounds. The configuration of 19-[3-(pyridin-3-yl)-prop-2-en-1-one]-fragment was established by X-ray analysis. Read More

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Coronarin K and L: Two Novel Labdane Diterpenes From : An Ayurvedic Crude Drug.

Front Chem 2021 21;9:642073. Epub 2021 Apr 21.

Natural Product and Medicinal Chemistry Division, Indian Institute of Integrative Medicine, Jammu, India.

The main objective of cancer treatment with chemotherapy is to kill the cancerous cells without affecting the healthy normal cells. In the present study, bioactivity-guided purification of the -chloroform soluble fraction from the methanol extract of resulted in the identification of two new labdane diterpenes: coronarin K () and coronarin L (), along with eight known compounds, coronarin A (), bisdemethoxycurcumin (), kaempferol 3--methyl ether (), kaempferol (), fenozan acid (), 3-(3-methoxy,4-hydroxyphenyl)-2-propenoic acid ferulic acid (), caffeic acid (), and gallic acid (). The structural identification of new compounds ( and ) were determined by detailed analysis of 1D (H and C) and 2D NMR (COSY, HSQC, and HMBC) spectroscopic data. Read More

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A Novel Role for Brain and Acute Leukemia Cytoplasmic (BAALC) in Human Breast Cancer Metastasis.

Front Oncol 2021 22;11:656120. Epub 2021 Apr 22.

Cancer Cell Biology Research Group, School of Biomedical Sciences and Pharmacy, College of Health, Medicine and Wellbeing, The University of Newcastle, Callaghan, NSW, Australia.

Brain and Acute Leukemia, Cytoplasmic (BAALC) is a protein that controls leukemia cell proliferation, differentiation, and survival and is overexpressed in several cancer types. The gene is located in the chromosomal region 8q22.3, an area commonly amplified in breast cancer and associated with poor prognosis. Read More

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Green Synthesized Silver Nanoparticles: Antibacterial and Anticancer Activities, Biocompatibility, and Analyses of Surface-Attached Proteins.

Front Microbiol 2021 22;12:632505. Epub 2021 Apr 22.

Department of Microbiology, Nicolaus Copernicus University, Toruń, Poland.

The increasing number of multi-drug-resistant bacteria and cancer cases, that are a real threat to humankind, forces research world to develop new weapons to deal with it. Biogenic silver nanoparticles (AgNPs) are considered as a solution to this problem. Biosynthesis of AgNPs is regarded as a green, eco-friendly, low-priced process that provides small and biocompatible nanostructures with antimicrobial and anticancer activities and potential application in medicine. Read More

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The Tetramethylpyrazine Derivative Statmp-151: A Novel Small Molecule Stat3 Inhibitor With Promising Activity Against Breast Cancer.

Front Pharmacol 2021 15;12:651976. Epub 2021 Apr 15.

College of Pharmacy, Southwest Minzu University, Chengdu, China.

Breast cancer is the most common malignancy in women and is a molecularly heterogeneous disease. Signal transducer and activator of transcription 3 (Stat3) is overexpressed and hyperactivated in a variety of human tumours, including breast cancer, thus representing a promising target for breast cancer treatment. In the present study, we evaluated the activities of a novel Stat3 inhibitor named Statmp-151 in the human breast cancer cell lines MCF-7 and MDA-MB-231 and the murine mammary carcinoma cell line 4T1. Read More

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Novel hybrid conjugates with dual estrogen receptor α degradation and histone deacetylase inhibitory activities for breast cancer therapy.

Bioorg Med Chem 2021 May 1;40:116185. Epub 2021 May 1.

Hubei Key Laboratory of Cell Homeostasis, College of Life Sciences, Wuhan University, Wuhan 430072, China. Electronic address:

Hormone therapy targeting estrogen receptors is widely used clinically for the treatment of breast cancer, such as tamoxifen, but most of them are partial agonists, which can cause serious side effects after long-term use. The use of selective estrogen receptor down-regulators (SERDs) may be an effective alternative to breast cancer therapy by directly degrading ERα protein to shut down ERα signaling. However, the solely clinically used SERD fulvestrant, is low orally bioavailable and requires intravenous injection, which severely limits its clinical application. Read More

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Discovery of thieno[2,3-d]pyrimidine-based derivatives as potent VEGFR-2 kinase inhibitors and anti-cancer agents.

Bioorg Chem 2021 Apr 27;112:104947. Epub 2021 Apr 27.

Department of Pharmaceutical Sciences, College of Pharmacy, AlMaarefa University, Ad Diriyah 13713, Riyadh, Saudi Arabia; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt. Electronic address:

Vascular endothelial growth factor-2 (VEGFR-2) is considered one of the most important factors in tumor angiogenesis, and consequently a number of anticancer therapeutics have been developed to inhibit VEGFR-2 signaling. Accordingly, eighteen derivatives of thieno[2,3-d]pyrimidines having structural characteristics similar to VEGFR-2 inhibitors were designed and synthesized. Anticancer activities of the new derivatives were assessed against three human cancer cell lines (HCT-116, HepG2, and MCF-7) using MTT. Read More

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New indenopyrazole linked oxadiazole conjugates as anti-pancreatic cancer agents: Design, synthesis, in silico studies including 3D-QSAR analysis.

Bioorg Med Chem Lett 2021 May 5:128094. Epub 2021 May 5.

Organic Synthesis and Process Chemistry Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India; Academy of Scientific and Innovative Research, Ghaziabad 201002, India; School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi 110062, India. Electronic address:

To continue the quest of newer anticancer agents, herein a novel class of 1,4-Dihydroindenopyrazole linked oxadiazole conjugates 9(a-r) was designed, synthesized and experimented for their anti-proliferative activities against four different cancer cell lines (human) such as MDA MB-231 (breast), PANC-1 (pancreatic), MCF-7 (breast), and Caco-2 (Colorectal) by using MTT assay. Among the series compound 9h and 9m demonstrated significant potency against the PANC-1 (human pancreatic cancer cells) with IC value 7.4 μM and 4. Read More

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Metabolomic fingerprinting of Brazilian marine sponges: a case study of Plakinidae species from Fernando de Noronha Archipelago.

Anal Bioanal Chem 2021 May 8. Epub 2021 May 8.

Laboratório de Produtos Naturais (LAPROMAR), Instituto de Química, Universidade Federal Fluminense, Niterói, RJ, 24020-005, Brazil.

Marine sponges from the Plakinidae family are well known for hosting cytotoxic secondary metabolites and the Brazilian Atlantic coast and its oceanic islands have been considered as a hotspot for the discovery of new Plakinidae species. Herein, we report the chemical profile among cytotoxic extracts obtained from four species of Plakinidae, collected in Fernando de Noronha Archipelago (PE, Northeastern Brazil). Crude organic extracts of Plakinastrella microspiculifera, Plakortis angulospiculatus, Plakortis insularis, and Plakortis petrupaulensis showed strong antiproliferative effects against two different cancer cell lines (HCT-116: 86. Read More

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Cancer-Cell-Derived Hybrid Vesicles from MCF-7 and HeLa Cells for Dual-Homotypic Targeting of Anticancer Drugs.

Macromol Biosci 2021 May 8:e2100067. Epub 2021 May 8.

Department of Bioscience and Biotechnology, Konkuk University, Seoul, 143-701, Republic of Korea.

Here, as a proof of concept, hybrid vesicles (VEs) are developed from two types of cancer cells, MCF-7 and HeLa, for the dual targeting of the anticancer drug doxorubicin (Dox) to cancer cells via homotypic interactions. Hybrid VEs with a size of 181.8 ± 28. Read More

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Enhancing the and activity of itraconazole against breast cancer using miltefosine-modified lipid nanocapsules.

Drug Deliv 2021 Dec;28(1):906-919

Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.

Itraconazole (ITC), a well-tolerated antifungal drug, exerts multiple anticancer effects which justified its preclinical and clinical investigation as potential anti-cancer agent with reduced side effects. Enhancement of ITC anti-cancer efficacy would bring valuable benefits to patients. We propose herein lipid nanocapsules (LNCs) modified with a subtherapeutic dose of miltefosine (MFS) as a membrane bioactive amphiphilic additive (M-ITC-LNC) for the development of an ITC nanoformulation with enhanced anticancer activity compared with ITC solution (ITC-sol) and unmodified ITC-LNC. Read More

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December 2021

Promotion of the anticancer activity of curcumin based on a metal-polyphenol networks delivery system.

Int J Pharm 2021 May 3:120650. Epub 2021 May 3.

College of Food Science, Southwest University, Chongqing, 400715, People's Republic of China; Research Center of Food Storage & Logistics, Southwest University, Chongqing 400715, People's Republic of China. Electronic address:

Curcumin (Cur), a hydrophobic active pharmaceutical ingredient with high anticancer activity, has poor water solubility and low bioavailability. Although many delivery systems have been developed to improve their bioavailability, some limitation such as low drug loading efficiency and poor stability are still remained. The metal-polyphenol networks (MPNs) delivery system designed in this subject solved above problems and effectively improved the anticancer activity of Cur. Read More

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Modulation of Apoptosis and Epithelial-Mesenchymal Transition E-cadherin/TGF-β/Snail/TWIST Pathways by a New Ciprofloxacin Chalcone in Breast Cancer Cells.

Anticancer Res 2021 May;41(5):2383-2395

Department of Biochemistry, Faculty of Pharmacy, Minia University, Minia, Egypt.

Background/aim: This study aimed to investigate the effect of the new ciprofloxacin chalcone [7-(4-(N-substituted carbamoyl methyl) piperazin-1 yl)] on the proliferation, migration, and metastasis of MCF-7 and MDA-MB-231 breast cancer cell lines.

Materials And Methods: Cell viability, colony formation and cell migration abilities were analysed. Cell cycle distribution and apoptosis were examined by flow cytometry. Read More

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Pyridine-derived VEGFR-2 inhibitors: Rational design, synthesis, anticancer evaluations, in silico ADMET profile, and molecular docking.

Arch Pharm (Weinheim) 2021 May 5:e2100085. Epub 2021 May 5.

Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.

Novel pyridine-derived compounds (5-19) were designed and synthesized, and their anticancer activities were evaluated against HepG2 and MCF-7 cells, targeting the VEGFR-2 enzyme. Compounds 10, 9, 8, and 15 were found to be the most potent derivatives against the two cancer cell lines, HepG2 and MCF-7, respectively, with IC  = 4.25 and 6. Read More

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CIP2A silencing alleviates doxorubicin resistance in MCF7/ADR cells through activating PP2A and autophagy.

Authors:
Z Zhu Z Wei

Clin Transl Oncol 2021 May 4. Epub 2021 May 4.

Thyroid and Breast Department, Cangzhou Central Hospital, No.16 Xinhua West Rd, Cangzhou city, Hebei Province, 061000, China.

Background: Cancerous inhibitor of protein phosphatase 2A (CIP2A) plays a critical role in the pathogenesis of various types of cancer. Here, we investigated whether manipulating CIP2A abundance could enhance the treatment effects of doxorubicin in MCF-7/ADR cells.

Methods: CIP2A silencing was achieved by specific siRNAs. Read More

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Selenium nanoparticles: Synthesis, cytotoxicity, antioxidant activity and interaction studies with ct-DNA and HSA, HHb and Cyt c serum proteins.

Biotechnol Rep (Amst) 2021 Jun 15;30:e00615. Epub 2021 Apr 15.

Center of Medical Biology Research, Health Technology Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran.

The aim of this study was the synthesis of selenium nanoparticles (SeNPs) employing vitamin C as a biocompatible and low toxic reducing agent. The synthesized selenium nanoparticles were characterized by using UV-vis, FT-IR, SEM-EDX, TEM, DLS, and zeta potential measurements. The results of the DPPH free radical scavenging assay demonstrate that this synthesized nano-selenium has strong potentials to scavenge the free radicals and cytotoxicity against MCF-7 and Raji Burkitt's lymphoma cancer cell lines. Read More

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Hyaluronic acid (HA)-coated naproxen-nanoparticles selectively target breast cancer stem cells through COX-independent pathways.

Mater Sci Eng C Mater Biol Appl 2021 May 10;124:112024. Epub 2021 Mar 10.

Biomaterials Group, Institute of Polymer Science and Technology (ICTP-CSIC), 28006 Madrid, Spain; Networking Biomedical Research Centre in Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), 28029 Madrid, Spain. Electronic address:

Cytotoxic chemotherapy continues to be the main therapeutic option for patients with metastatic breast cancer. Several studies have reported a significant association between chronic inflammation, carcinogenesis and the presence of cancer stem cells (CSC). We hypothesized that the use of non-steroidal anti-inflammatory drugs targeted to the CSC population could help reducing tumor progression and dissemination in otherwise hard to treat metastatic breast cancer. Read More

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Synthesis, biological evaluation and docking studies of 1,2,4-oxadiazole linked 5-fluorouracil derivatives as anticancer agents.

BMC Chem 2021 May 4;15(1):30. Epub 2021 May 4.

Sreenidhi Institute of Science and Technology (Autonomous), Yamnampet, Ghatkesar, Hyderabad, Telangana, India.

Background: 1,2,4-oxadiazole derivatives exhibited significant anti-cancer activity when they were evaluated, against human cancer cell lines. They also showed anti-inflammatory, analgesic, diabetic, immunosuppressive, α,β-receptor antagonist, antimicrobial, anti-helminthic, histamine-H3 and antiparasitic properties. A pyrimidine analog, 5 fluoro-uracil is a chemotherapeutic drug used for treating multiple solid malignant tumors. Read More

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Synthesis and Evaluation of the Cytotoxic Activity of Water-Soluble Cationic Organometallic Complexes of the Type [Pt(η-CHOMe)(L)(Phen)] (L = NH, DMSO; Phen = 1,10-Phenanthroline).

Pharmaceutics 2021 Apr 30;13(5). Epub 2021 Apr 30.

Dipartimento di Scienze e Tecnologie Biologiche ed Ambientali, Università del Salento, Prov.le Lecce-Monteroni, Centro Ecotekne, 73100 Lecce, Italy.

Starting from the [PtCl(η-CHOMe)(phen)] (phen = 1,10-phenanthroline, ) platinum(II) precursor, we synthesized and characterized by multinuclear NMR new [Pt(η-CHOMe)(L)(phen)] (L = NH, ; DMSO, ) complexes. These organometallic species, potentially able to interact with cell membrane organic cation transporters (OCT), violating some of the classical rules for antitumor activity of cisplatin analogues, were evaluated for their cytotoxicity. Interestingly, despite both complexes and resulting in greater cell uptake than cisplatin in selected tumor cell lines, only showed comparable or higher antitumor activity. Read More

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Comparison of Anticancer Activity of Extract on MCF-7 and MCF-12A Cell Line: Correlation with Invasion and Adhesion.

Biomolecules 2021 Apr 30;11(5). Epub 2021 Apr 30.

Department of Pharmacy, Università degli Studi "Gabriele d'Annunzio", Via dei Vestini 31, 66100 Chieti, Italy.

subsp. is an important medicinal plant in several countries, including Turkey. This study aimed to evaluate the cytotoxicity of a crude extract of subsp. Read More

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Pterostilbene nanoparticles with small particle size show excellent anti-breast cancer activity in vitro and in vivo.

Nanotechnology 2021 May 4. Epub 2021 May 4.

Chinese Academy of Medical Sciences and Peking Union Medical College Institute of Medicinal Plant Development, Beijing, CHINA.

Pterostilbene (PTE) is known as resveratrol of the next generation and it has attracted extensive attention in recent years. PTE can inhibit the growth of a variety of tumor cells. To overcome the problem of insolubility, PTE was loaded into nanoparticles (NPs) by anti-solvent precipitation technique using soybean lecithin (SPC) and D-α-tocopheryl polyethylene glycol succinate (TPGS) as stabilizers. Read More

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Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors.

Eur J Med Chem 2021 Apr 24;220:113501. Epub 2021 Apr 24.

Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, Liaoning, China.

Lysine-specific demethylase 1 (LSD1) is a FAD-dependent enzyme, which has been proposed as a promising target for therapeutic cancer. Herein, a series of benzofuran derivatives were designed, synthesized and biochemical evaluated as novel LSD1 inhibitors based on scaffold hopping and conformational restriction strategy. Most of the compounds potently suppressed the enzymatic activities of LSD1 and potently inhibited tumor cells proliferation. Read More

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Development and interpretation of a QSAR model for in vitro breast cancer (MCF-7) cytotoxicity of 2-phenylacrylonitriles.

J Comput Aided Mol Des 2021 May 4. Epub 2021 May 4.

Department of Chemistry, Tschannen Science Center, California State University at Sacramento, 6000 J Street, Sacramento, CA, 95819, USA.

The Arylhydrocarbon Receptor (AhR), a member of the Per-ARNT-SIM transcription factor family, has been as a potential new target to treat breast cancer sufferers. A series of 2-phenylacrylonitriles targeting AhR has been developed that have shown promising and selective activity against cancerous cell lines while sparing normal non-cancerous cells. A quantitative structure-activity relationship (QSAR) modeling approach was pursued in order to generate a predictive model for cytotoxicity to support ongoing synthetic activities and provide important structure-activity information for new structure design. Read More

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Design, synthesis, and anticancer evaluation of novel andrographolide derivatives bearing an α,β-unsaturated ketone moiety.

Bioorg Chem 2021 Apr 24;112:104941. Epub 2021 Apr 24.

Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 211198, China. Electronic address:

A series of 1,2-didehydro-3-ox-andrographolide derivatives based on two Michael acceptors were designed, synthesized and evaluated for their anticancer activity against two human cancer cell lines (HCT116 and MCF-7). All tested compounds exhibited significant growth inhibitory effect on HCT116 and moderate to good inhibitory effect on MCF-7 cell proliferation. Compound 10b displayed the best inhibitory activities against both HCT116 and MCF-7 cell lines, with IC values of 2. Read More

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Bioactive sesterterpenoids from the fungus Penicillium roqueforti YJ-14.

Phytochemistry 2021 Apr 30;187:112762. Epub 2021 Apr 30.

Functional Molecules Analysis and Biotransformation Key Laboratory of Universities in Yunnan Province, Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, People's Republic of China. Electronic address:

Seven previously undescribed sesterterpenes were characterized from Penicillium roqueforti YJ-14 by solid fermentation. Their structures were initially investigated in detail by spectroscopic analyses and HR-ESI-MS and were further confirmed by X-crystallography. In in vitro bioassays, compounds 1, 5 and 7 showed cytotoxic activity against the MCF-7 breast cancer cell line with IC values of 7. Read More

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A new synthetic antitumor naphthoquinone induces ROS-mediated apoptosis with activation of the JNK and p38 signaling pathways.

Chem Biol Interact 2021 Apr 30;343:109444. Epub 2021 Apr 30.

Laboratory of Biological Activity, Faculty of Pharmaceutical Sciences, Federal University of Amazonas - UFAM, Manaus, Amazonas, 69077-000, Brazil. Electronic address:

Quinones are plant-derived secondary metabolites that present diverse pharmacological properties, including antibacterial, antifungal, antiviral, anti-inflammatory, antipyretic and anticancer activities. In the present study, we evaluated the cytotoxic effect of a new naphthoquinone 6b,7-dihydro-5H-cyclopenta [b]naphtho [2,1-d]furan-5,6 (9aH)-dione) (CNFD) in different tumor cell lines. CNFD displayed cytotoxic activity against different tumor cell lines, especially in MCF-7 human breast adenocarcinoma cells, which showed IC values of 3. Read More

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Disposition of Dietary Polyphenols in Breast Cancer Patients' Tumors, and Their Associated Anticancer Activity: The Particular Case of Curcumin.

Mol Nutr Food Res 2021 May 3:e2100163. Epub 2021 May 3.

Laboratory of Food & Health, Research Group on Quality, Safety and Bioactivity of Plant Foods, CEBAS-CSIC, Campus de Espinardo, Murcia, 30100, Spain.

Scope: Some polyphenol-derived metabolites reach human breast cancer (BC) tissues at concentrations that induce cell senescence. However, this is unknown for isoflavones, curcuminoids, and lignans. Here, their metabolic profiling in normal (NT) and malignant (MT) mammary tissues of newly-diagnosed BC patients and the tissue-occurring metabolites' anticancer activity are evaluated. Read More

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Biosynthesis of Silver Nanoparticles by : Characterization, Optimization, and Biological Activities.

Front Bioeng Biotechnol 2021 15;9:633468. Epub 2021 Apr 15.

Department of Botany and Microbiology, Faculty of Science, Alexandria University, Alexandria, Egypt.

In this study, mycelial filtrate of BA6 was used to reduce AgNO to form silver nanoparticles (AgNPs). The effect of seven independent variables on the diameter of AgNPs was studied by applying design of experiments (DOE). At optimal conditions, the diameter of AgNPs was reduced by approximately 26. Read More

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Molecular characteristics supporting l-Type amino acid transporter 1 (LAT1)-mediated translocation.

Bioorg Chem 2021 Apr 22;112:104921. Epub 2021 Apr 22.

School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, P.O. Box 1627, FI-70211 Kuopio, Finland. Electronic address:

l-Type amino acid transporter 1 (LAT1) is an interesting protein due to its peculiar expression profile. It can be utilized not only as a carrier for improved or targeted drug delivery, e.g. Read More

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Design, synthesis and biological evaluation of novel imidazole-chalcone derivatives as potential anticancer agents and tubulin polymerization inhibitors.

Bioorg Chem 2021 Apr 20;112:104904. Epub 2021 Apr 20.

Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.

Novel imidazole-chalcone derivatives were designed and synthesized as tubulin polymerization inhibitors and anticancer agents. The antiproliferative activity of the imidazole-chalcone was assessed on some human cancer cell lines including A549 (adenocarcinoma human alveolar basal epithelial cells), MCF-7 (human breast cancer cells), MCF-7/MX (mitoxantrone resistant human breast cancer cells), and HEPG2 (human hepatocellular carcinoma cells). Generally, the imidazole-chalcone derivatives exhibited more cytotoxicity on A549 cancer cells in comparison to the other three cell lines, among them compounds 9j' and 9g showed significant cytotoxicity with IC values ranging from 7. Read More

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