6,040 results match your criteria potent antiproliferative


Design, synthesis and in vitro antitumor evaluation of novel pyrazole-benzimidazole derivatives.

Bioorg Med Chem Lett 2021 May 9:128097. Epub 2021 May 9.

Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling, 712100, Shaanxi, PR China.

A series of novel pyrazole-benzimidazole derivatives (6-42) have been designed, synthesized and evaluated for their in vitro antiproliferative activity against the HCT116, MCF-7 and Huh-7 cell lines. Among them, compounds 17, 26 and 35 showed significant antiproliferative activity against HCT116 cell lines with the IC values of 4.33, 5. Read More

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Synthesis of Thio-lignan Analogues, Bioequivalent Salvinal without Unfavored Aldehyde.

J Org Chem 2021 May 12. Epub 2021 May 12.

School of Pharmaceutical Sciences, College of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa 920-1192, Japan.

The oxygen in the benzofuran (BF) of three antiproliferative natural neolignans, salvinal (), obovaten (), and 2-[7-methoxy-2-(4-methoxyphenyl)-3-methylbenzofuran-5-yl]ethanol (), was replaced with sulfur to form the new biological scaffold benzothiophene (BT) thio-lignans -. Compounds - and synthesized derivatives were evaluated for antiproliferative activity against five human cancer cell lines, including a multidrug-resistant cell line. Thio-salvinal () displayed significant antiproliferative effects with half-maximal inhibitory concentration (IC) values of 0. Read More

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Nigella sativa oil inhibits proliferation and stimulates apoptosis of human lymphocytes in vitro.

Hum Immunol 2021 May 8. Epub 2021 May 8.

Department of Pathophysiology, Faculty of Medicine, Medical University of Gdansk, Poland.

The study aimed to examine the in vitro influence of Nigella sativa oil on human lymphocytes. Cells were stimulated with a monoclonal anti-CD3 antibody in the presence of serial oil ethanol dilutions. Then their proliferation and apoptosis rates were assessed using flow cytometry. Read More

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Fractions of Ageratum conyzoides L. (Compositae) induce mitochondrial-mediated apoptosis in rats: Possible option in monosodium glutamate-induced hepatic and uterine pathological disorder.

J Ethnopharmacol 2021 May 8:114192. Epub 2021 May 8.

Laboratories for Biomembrane Research and Biotechnology, Department of Biochemistry, College of Medicine, University of Ibadan, Nigeria. Electronic address:

Ethnopharmacological Relevance: Several pathological disorders have been attributed to either oxidative stress or defect in apoptotic signaling pathway. Some bioactive compounds elicit their antiproliferative properties by induction of apoptosis via mitochondrial permeability transition (mPT) pore opening.

Aim Of Study: The present study therefore investigated the effects of various fractions of methanol extract of Ageratum conyzoides L. Read More

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An improved synthesis of indanocine and antiproliferative activity of 2-benzyl-indanocine via microtubule destabilization.

Chem Biol Drug Des 2021 May 9. Epub 2021 May 9.

CSIR-Central Institute of Medicinal and Aromatic Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow, 226015, India.

Indanocine, a potent anticancer investigational drug of National Cancer Institute-USA has been much discussed in recent years. Present communication aimed at total synthesis of indanocine and its close analogues. Total synthesis was improved by double yields than previously reported yields. Read More

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Hydrazine-Containing Heterocycle Cytochalasan Derivatives From Hydrazinolysis of Extracts of a Desert Soil-Derived Fungus 375.

Front Chem 2021 21;9:620589. Epub 2021 Apr 21.

Zhengzhou Key Laboratory of Synthetic Biology of Natural Products, Zhengzhou Key Laboratory of Medicinal Resources Research, Comprehensive Utilization of Edible and Medicinal Plant Resources Engineering Technology Research Center, Huanghe Science and Technology College, Zhengzhou, China.

"Diversity-enhanced extracts" is an effective method of producing chemical libraries for the purpose of drug discovery. Three rare new cytochalasan derivative chaetoglobosins B-B (-) were obtained from chemically engineered crude broth extracts of 375 prepared by reacting with hydrazine monohydrate and four known metabolite chaetoglobosins () were also identified from the fungus. The structures were identified by NMR and MS analysis and electronic circular dichroism simulation. 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 indoline derivatives as anticancer agents via inhibition of tubulin polymerization.

Bioorg Med Chem Lett 2021 May 6:128095. Epub 2021 May 6.

School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, China. Electronic address:

Human esophageal squamous cell carcinoma (ESCC) is one of the most lethal cancers in human digestive system. It is necessary to discover novel antitumor agents for the treatment of esophageal cancers because of its poor prognosis. Indoline has been reported as an efficient anticancer fragment to design novel anticancer agents. Read More

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Isoflavanquinones from Abrus precatorius roots with their antiproliferative and anti-inflammatory effects.

Phytochemistry 2021 May 4;187:112743. Epub 2021 May 4.

Dr. Panjwani Center for Molecular Medicine and Drug Research (PCMD), International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan; HEJ Research Institute of Chemistry, University of Karachi, Karachi, 75270, Pakistan.

Phytochemical studies on the root of Abrus precatorius Linn. (Fabaceae), leads towards the identification of four undescribed (abruquinones M, N, O, and P), and seven known abruquinones, (abruquinones A, E, B, F, I, D, and G). Spectroscopic analyses (1D, and 2D NMR, HRESI-MS) were used in elucidating structures of the all compounds. Read More

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Computational study on subfamilies of piperidine derivatives: QSAR modelling, model external verification, the inter-subset similarity determination, and structure-based drug designing.

SAR QSAR Environ Res 2021 May 7:1-30. Epub 2021 May 7.

Chemometrics Laboratory, Chemistry Department, Faculty of Science, University of Kurdistan, Sanandaj, Iran.

A new subset of furan-pyrazole piperidine derivatives was used for QSAR model development. These compounds exhibit good Akt1 inhibitory activity; moreover, antiproliferative activities in vitro against OVCAR-8 (Human ovarian carcinoma cells) and HCT116 (human colon cancer cells), were confirmed for them. Based on the relevant three-dimensional (3D) and 2D autocorrelation descriptors, selected by genetic algorithm (GA), multiple linear regression (MLR) was established on half maximal-inhibitory concentration (IC), in Akt1 and cancer cell lines independently. Read More

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Concise synthesis and biological evaluation of 2-Aryl-3-Anilinobenzo[b]thiophene derivatives as potent apoptosis-inducing agents.

Bioorg Chem 2021 Apr 20;112:104919. Epub 2021 Apr 20.

Department of Medical Sciences, Laboratory for Technologies of Advanced Therapies (LTTA), University of Ferrara, 44121 Ferrara, Italy.

Many clinically used agents active in cancer chemotherapy exert their activity through the induction of cell death (apoptosis) by targeting microtubules, altering protein function or inhibiting DNA synthesis. The benzo[b]thiophene scaffold holds a pivotal place as a pharmacophore for the development of anticancer agents, and, in addition, this scaffold has many pharmacological activities. We have developed a flexible method for the construction of a new series of 2-aryl-3-(3,4,5-trimethoxyanilino)-6-methoxybenzo[b]thiophenes as potent antiproliferative agents, giving access to a wide range of substitution patterns at the 2-position of the 6-methoxybenzo[b]thiophene common intermediate. Read More

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Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.

Eur J Med Chem 2021 Apr 25;220:113453. Epub 2021 Apr 25.

School of Pharmacy, Xinxiang Medical University, Xinxiang, Henan, 453003, China. Electronic address:

LSD1 and HDAC are physical and functional related to each other in various human cancers and simultaneous pharmacological inhibition of LSD1 and HDAC exerts synergistic anti-cancer effects. In this work, a series of novel LSD1/HDAC bifunctional inhibitors with a styrylpyridine skeleton were designed and synthesized based on our previously reported LSD1 inhibitors. The representative compounds 5d and 5m showed potent activity against LSD1 and HDAC at both molecular and cellular level and displayed high selectivity against MAO-A/B. Read More

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Prodigiosin induced the caspase-dependent apoptosis in human chronic myelogenous leukemia K562 cell.

Res Pharm Sci 2021 Feb 30;16(1):26-34. Epub 2020 Dec 30.

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Urmia University of Medical Sciences, Urmia, I.R. Iran.

Background And Purpose: Chronic myeloid leukemia (CML) as a myeloproliferative disease is characterized by increased cellularity of bone marrow. Implementing the latest treatment protocols is currently accompanied by serious and life-threatening side effects. There are worldwide attempts to find new effective and potent therapeutic agents with minimal side effects on CML patients. Read More

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February 2021

Synthesis and biological evaluation of novel isoxazole-piperazine hybrids as potential anti-cancer agents with inhibitory effect on liver cancer stem cells.

Eur J Med Chem 2021 Apr 24;221:113489. Epub 2021 Apr 24.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey. Electronic address:

In our effort for the development of novel anticancer therapeutics, a series of isoxazole-piperazine analogues were prepared, and primarily screened for their antiproliferative potential against hepatocellular carcinoma (HCC; Huh7/Mahlavu) and breast (MCF-7) cancer cells. All compounds demonstrated potent to moderate cytotoxicity on all cell lines with IC values in the range of 0.09-11. Read More

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Development of genistein-loaded gold nanoparticles and their antitumor potential against prostate cancer cell lines.

Mater Sci Eng C Mater Biol Appl 2021 May 27;124:112078. Epub 2021 Mar 27.

Institute for Biological Research "Siniša Stanković" - National Institute of the Republic of Serbia, University of Belgrade, Bulevar despota Stefana 142, 11060 Belgrade, Serbia. Electronic address:

Soy isoflavone genistein (Gen) exerts beneficial effects against prostate cancer cells in vitro and in vivo. However, its use as a chemoprevention/therapeutic agent is largely limited due to its low bioavailability. In this study we synthesized two variants of a new delivery system, genistein-gold nanoparticles conjugates Gen@AuNPs1 and Gen@AuNPs2, by an environmentally friendly method, using a dual role of Gen to reduce Au and stabilize the formed AuNPs, with no additional component. Read More

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MDM2 inhibitor APG-115 exerts potent antitumor activity and synergizes with standard-of-care agents in preclinical acute myeloid leukemia models.

Cell Death Discov 2021 May 3;7(1):90. Epub 2021 May 3.

Ascentage Pharma (Suzhou) Co., Ltd., 218 Xinghu Street, Suzhou, Jiangsu Province, China.

Acute myeloid leukemia (AML) is a clinically and genetically heterogeneous clonal disease associated with unmet medical needs. Paralleling the pathology of other cancers, AML tumorigenesis and propagation can be ascribed to dysregulated cellular processes, including apoptosis. This function and others are regulated by tumor suppressor P53, which plays a pivotal role in leukemogenesis. Read More

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Exploring fruits from genus Prunus as a source of potential pharmaceutical agents - In vitro and in silico study.

Food Chem 2021 Apr 19;358:129812. Epub 2021 Apr 19.

iBET, Instituto de Biologia Experimental e Tecnológica, Avenida da República, Quinta do Marquês, 2780-157 Oeiras, Portugal; Instituto de Tecnologia Química e Biológica António Xavier, Universidade Nova de Lisboa (ITQB NOVA), Avenida da República, Quinta do Marquês, 2780-157 Oeiras, Portugal.

Prunus fruits are recognized to be rich sources of polyphenols with health promoting effect. In this work we evaluated the phenolic profile and bioactivity, namely antioxidant capacity, antiproliferative effect in HT29, and inhibition capacity of α-glucosidase (α-Gls), α-amylase (α-Amy) and human dipeptidyl peptidase III (hDPP III) activities, of traditional Prunus fruits grown in Serbia. Fifteen Prunus samples were investigated and compared: common European plum and three old plum subspecies ('vlaškača', damson plum and white damson), purple-leaf cherry plum, red and white cherry plum, sweet cherry, sweet cherry-wild type, sour cherry, steppe cherry, mahaleb cherry, blackthorn, peach, and apricot. Read More

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Resveratrol and Its Analogs: Potent Agents to Reverse Epithelial-to-Mesenchymal Transition in Tumors.

Front Oncol 2021 16;11:644134. Epub 2021 Apr 16.

The First Clinical Medical College of Zhejiang Chinese Medical University, Hangzhou, China.

Epithelial-to-mesenchymal transition (EMT), a complicated program through which polarized epithelial cells acquire motile mesothelial traits, is regulated by tumor microenvironment. EMT is involved in tumor progression, invasion and metastasis reconstructing the cytoskeleton and degrading the tumor basement membrane. Accumulating evidence shows that resveratrol, as a non-flavonoid polyphenol, can reverse EMT and inhibit invasion and migration of human tumors diverse mechanisms and signaling pathways. Read More

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Dichloroacetate and PX-478 exhibit strong synergistic effects in a various number of cancer cell lines.

BMC Cancer 2021 Apr 30;21(1):481. Epub 2021 Apr 30.

Charité - Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin, Humboldt-Universität zu Berlin, and Berlin Institute of Health, Charitéplatz 1, 10117, Berlin, Germany.

Background: One key approach for anticancer therapy is drug combination. Drug combinations can help reduce doses and thereby decrease side effects. Furthermore, the likelihood of drug resistance is reduced. Read More

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Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes.

Materials (Basel) 2021 Apr 18;14(8). Epub 2021 Apr 18.

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

A library of 21 novel chiral 1,2,3-triazole-based 2-azabicycloalkane conjugates was designed and synthesized using the copper(I)-catalyzed click reaction. The obtained hybrids were assessed for their antiproliferative potency against three selected human cancer cell lines: Hs294T (melanoma), MIA PaCa-2 (pancreas tumor) and NCI-H1581 (lung tumor). The majority of the synthesized compounds demonstrated moderate to potent activity, and some of them appeared more selective than cisplatin, with selectivity index exceeding 9. Read More

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Genomic and Metabolomic Investigation of a Rhizosphere Isolate WLXQSS-4 Associated with a Traditional Chinese Medicine.

Molecules 2021 Apr 8;26(8). Epub 2021 Apr 8.

Department of Natural Products Chemistry, School of Pharmacy, China Medical University, Shenyang 110122, China.

Rhizosphere microorganisms play important ecological roles in promoting herb growth and producing abundant secondary metabolites. Studies on the rhizosphere microbes of traditional Chinese medicines (TCMs) are limited, especially on the genomic and metabolic levels. In this study, we reported the isolation and characterization of a WLXQSS-4 strain from the rhizospheric soil of Rupr. Read More

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Photocytotoxic Activity of Ruthenium(II) Complexes with Phenanthroline-Hydrazone Ligands.

Molecules 2021 Apr 6;26(7). Epub 2021 Apr 6.

Departamento de Química, Universidade Federal de Minas Gerais, Avenida Antônio Carlos, 6627, Belo Horizonte (MG) 31270-901, Brazil.

This paper reports on the synthesis and characterization of two new polypyridyl-hydrazone Schiff bases, ()-'-(6-oxo-1,10-phenanthrolin-5(6)-ylidene)thiophene-2-carbohydrazide () and ()-'-(6-oxo-1,10-phenanthrolin-5(6)-ylidene)furan-2-carbohydrazide (), and their two Ru(II) complexes of the general formula [RuCl(DMSO)(phen)(L)](PF6). Considering that hydrazides are a structural part of severa l drugs and metal complexes containing phenanthroline derivatives are known to interact with DNA and to exhibit antitumor activity, more potent anticancer agents can be obtained by covalently linking the thiophene acid hydrazide or the furoic acid hydrazide to a 1,10-phenanthroline moiety. These ligands and the Ru(II) complexes were characterized by elemental analyses, electronic, vibrational, H NMR, and ESI-MS spectroscopies. Read More

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Nutritional Value and Preventive Role of L. and Its Main Component Thymoquinone in Cancer: An Evidenced-Based Review of Preclinical and Clinical Studies.

Molecules 2021 Apr 7;26(8). Epub 2021 Apr 7.

Department of Clinical Sciences, Polytechnic University of Marche, 60131 Ancona, Italy.

In recent times, scientific attention has been paid to different foods and their bioactive components for the ability to inhibit the onset and progress of different types of cancer. extract, powder and seed oil and its main components, thymoquinone and α-hederin, have showed potent anticancer and chemosensitizing effects against various types of cancer, such as liver, colon, breast, renal, cervical, lung, ovarian, pancreatic, prostate and skin tumors, through the modulation of various molecular signaling pathways. Herein, the purpose of this review was to highlight the anticancer activity of and it constitutes, focusing on different in vitro, in vivo and clinical studies and projects, in order to underline their antiproliferative, proapoptotic, cytotoxic and antimetastatic effects. Read More

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Synthesis and Biological Screening of New Cyano-Substituted Pyrrole Fused (Iso)Quinoline Derivatives.

Molecules 2021 Apr 3;26(7). Epub 2021 Apr 3.

Department of Chemistry, Faculty of Chemistry, Alexandru Ioan Cuza University of Iași, 11 Carol I, 700506 Iași, Romania.

Several new cyano-substituted derivatives with pyrrolo[1,2-]quinoline and pyrrolo[2,1-]isoquinoline scaffolds were synthesized by the [3 + 2] cycloaddition of (iso)quinolinium ylides to fumaronitrile. The cycloimmonium ylides reacted in situ as 1,3-dipoles with fumaronitrile to selectively form distinct final compounds, depending on the structure of the (iso)quinolinium salt. Eleven compounds were evaluated for their anticancer activity against a panel of 60 human cancer cell lines. Read More

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Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2.

Angew Chem Int Ed Engl 2021 Apr 29. Epub 2021 Apr 29.

Harvard Medical School, Dana Farber Cancer Institute, 360 Longwood Avenue, 2115, Boston, UNITED STATES.

Aberrant activation of FGFR signaling occurs in many cancers, and ATP-competitive FGFR inhibitors have received regulatory approval. Despite demonstrating clinical efficacy, these inhibitors exhibit dose-limiting toxicity, potentially due to a lack of selectivity amongst the FGFR family and are poorly tolerated. Here, we report the discovery and characterization of DGY-09-192, a bivalent degrader that couples the pan-FGFR inhibitor BGJ398 to a CRL2 VHL E3 ligase recruiting ligand, which preferentially induces FGFR1&2 degradation while largely sparing FGFR3&4. Read More

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Anticancer effects against colorectal cancer models of chloro(triethylphosphine)gold(I) encapsulated in PLGA-PEG nanoparticles.

Biometals 2021 Apr 27. Epub 2021 Apr 27.

Department of Chemistry and Industrial Chemistry (DCCI), University of Pisa, Via G. Moruzzi 13, 56124, Pisa, Italy.

Chloro(triethylphosphine)gold(I), (EtPAuCl hereafter), is an Auranofin (AF)-related compound showing very similar biological and pharmacological properties. Like AF, EtPAuCl exhibits potent antiproliferative properties in vitro toward a variety of cancer cell lines and is a promising anticancer drug candidate. We wondered whether EtPAuCl encapsulation might lead to an improved pharmacological profile also considering the likely reduction of unwanted side-reactions that are responsible for adverse effects and for drug inactivation. Read More

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The Apoptotic Properties of Leaf Extracts of Simarouba glauca against Human Leukemic Cancer Cells.

Asian Pac J Cancer Prev 2021 Apr 1;22(4):1305-1312. Epub 2021 Apr 1.

Department of Dentistry, Oral Health Institute, Hamad Medical corporation, Doha, Qatar.

Background And Objective: Simarouba glauca is a plant belonging to the family of Simaroubaceae. It is a potent source of secondary metabolites. The aim of this study was to evaluate the apoptotic properties of leaf extracts of Simarouba glauca against human leukemic cancer cells. Read More

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Synthesis, molecular modeling and biological evaluation of new benzo[4,5]thieno[3,2-b]pyran derivatives as topoisomerase I-DNA binary complex poisons.

Bioorg Chem 2021 Apr 15;112:104915. Epub 2021 Apr 15.

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Menoufia University, Shibin El kom, Gamal Abd El-Nasir Street, Menoufia, Egypt. Electronic address:

A series of new benzo[b]thiophenes 2a-f and benzo[4,5]thieno[3,2-b]pyran derivatives 3a-f and 4a-f were synthesized and their structures were confirmed by elemental analyses and spectral data. All synthesized compounds were evaluated by the National Cancer Institute (NCI, USA) against 60 human tumor cell lines. Compounds 3a-f and 4a-f showed potent cytotoxic effects in one dose assay with mean growth inhibition ranging from 62% to 80%. Read More

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A comprehensive mechanistic insight into the dietary and estrogenic lignans, arctigenin and sesamin as potential anticarcinogenic and anticancer agents. Current status, challenges, and future perspectives.

Crit Rev Food Sci Nutr 2021 Apr 27:1-17. Epub 2021 Apr 27.

Department of Pharmacology, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

A large body of evidence indicates that lignans as polyphenolic compounds are beneficial against life-threatening diseases such as cancer. Plant lignans have the potential to induce cancer cell death and interfere with carcinogenesis, tumor growth, and metastasis. Epidemiological studies have revealed that the intake of lignans is inversely associated with the risk of several cancers. Read More

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Antiproliferative and cytotoxic activities of C-Geranylated flavonoids from Paulownia tomentosa Steud. Fruit.

Bioorg Chem 2021 Mar 5;111:104797. Epub 2021 Mar 5.

Department of Natural Drugs, Faculty of Pharmacy, Masaryk University, Palackého tř. 1946/1, 61200 Brno, Czech Republic.

Prenylated or geranylated flavonoids have been studied for their promising antiproliferative and cytotoxic activities. Twelve natural geranylated flavonoids (1-12) were isolated from the fruit of Paulownia tomentosa Steud. Their structures were elucidated using UV and IR spectroscopy, mass spectrometry, and 1D and 2D NMR spectroscopy. Read More

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