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Anticancer agents

Tìm thấy 19+ kết quả cho từ khóa "Anticancer agents"

An insight into the therapeutic potential of piperazine-based anticancer agents

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The piperazine derivatives of tranylcypromine, compounds 66 and 67, having IC 50 values of µM and µM against KDM1A, were found to be the most effective agents..

Two new coordination polymers containing dicyanidoargentate(I) and dicyanidoaurate(I): synthesis and characterization, and a detailed in vitro investigation of their anticancer activities on some cancer cell lines

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We think that there is a great need for large and well-designed anticancer activity studies of new anticancer agents built from parent compounds C1 and C2 with better solubility in biological fluid and less toxicity.. Synthesis of [Ni(edbea )Ag 3 (CN) 5 ] n (C1. The final volume of the wells was adjusted to 200 µ L with supplemented DMEM..

Synthesis and biological evaluation of new pyrazolebenzene-sulphonamides as potential anticancer agents and hCA I and II inhibitors

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First, the question that whether the compounds have cytotoxic/anticancer properties should be answered. The cytotoxicities of the compounds towards tumor cell lines were in the range of 6.7 – 400 µM (Table 1). This shows that the compounds had anticancer properties.

Chapter 081. Principles of Cancer Treatment (Part 8)

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High-dose chemotherapy regimens are predicated on the observation that the dose-. response curve for many anticancer agents is rather steep, and increased dose can produce markedly increased therapeutic effect, although at the cost of potentially life-threatening complications that require intensive support, usually in the form of hematopoietic stem cell support from the patient (autologous) or from donors matched for histocompatibility loci (allogeneic).

Innovational combination of hetero-bifunctional N-PEG quinoline scaffolds derivatives with improved anticancer activity against breast and colon cancer cell lines and P-glycoprotein, cytochrome p450 enzyme activity prediction

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IC 50 values of the anticancer agents (controls).. About 25 mL of the contents of the flask were poured and evenly spread in a Petri dish (13 cm in diameter) and allowed to set for 2h. The sample size for all of the compounds was fixed as 10 µL.. The plates were incubated at 37 °C for 24 h, the control was similarly maintained with 1 mL of DMSO, and the zones of inhibition of the bacterial growth were measured in mm using a zone reader..

Chapter 081. Principles of Cancer Treatment (Part 7)

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The usefulness of any drug is governed by the extent to which a given dose causes a useful result (therapeutic effect. in the case of anticancer agents, toxicity to tumor cells) as opposed to a toxic effect. Really useful drugs have large therapeutic indices, and this usually occurs when the drug target is expressed in the disease-causing compartment as opposed to the normal compartment..

Synthesis and evaluation of novel 1,3,4-thiadiazole–fluoroquinolone hybrids as antibacterial, antituberculosis, and anticancer agents

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Nalidixic acid is the first of the quinolone antibacterial agents, although technically it is a naphthyri- dine structure-containing compound, not quinolone. 5 It was discovered as the synthetic by-product of the antimalarial agent chloroquine and indicated to have antibacterial activity towards gram-negative bacteria, 5 decades ago. The first one was the introduc- tion of a fluorine atom to the sixth position of the quinolone ring.

Achillea millefolium L. ethyl acetate fraction induces apoptosis and cell cycle arrest in human cervical cancer (HeLa) cells

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The cell cycle pro fi le and apoptosis analysis of the EtOAc fraction was studied in HeLa cells. millefolium, which may be a promising and valuable source of natural antioxidant and anticancer agents to be used in the development of new functional and therapeutic compounds in the future.. Cancer is considered one of the most lethal ailments worldwide.. Therapeutic herbs were used previously to treat cancer (Holohan et al., 2013).

Synthesis of novel 1,2,4-triazoles and triazolo-thiadiazines as anticancer agents

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1 H NMR 8.0-10.16 ppm. Yellow solid, yield (0.53 g, 60. 6.92 (d, J = 9.0 Hz, 2H, Ar-H), 7.29 (d, J = 9.0 Hz, 2H, Ar-H), 10.29 (s, 1H, NH). H, 3.11. H, 3.29. Yellow solid, yield (0.62 g, 73. H, 3.25. H, 3.47. Yellow solid, yield (0.65 g, 76. 6.8–7.18 (m, 4H, Ar H), 10.32 (s, 1H, NH)....

Endoplasmic reticulum stress and oncomir-associated chemotherapeutic drug resistance mechanisms in breast cancer tumors

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The DNA damage response (DDR) of cells touched by anticancer agents by reducing the DNA repair mechanisms and effectiveness of drugs, may lead to the progress of MDR (Wang et al., 2019). The frequency of HRD is low in response to endocrine therapy in HER2-overexpressing (HER2+) cell line (Manié et al., 2015)..

Antibacterial, antibiofilm and antitumor activities of grape and mulberry leaves ethanolic extracts towards bacterial clinical strains

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Natural products have received increasing attention over the past 30 years for their potential as novel anticancer agents (Rajendran et al., 2016).. Overall, they have been shown to possess anticancer activities including the antioxidant process, tumor growth inhibition, apoptosis induction and cancer cell cytotoxicity (Gupta et al., 2014. Lei et al., 2015.

Synthesis, characterization, and investigation of singlet oxygen, DNA interaction, and topoisomerase I inhibition properties of novel zinc(II) phthalocyanine

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A comprehensive review of topoisomerase inhibitors as anticancer agents in the past decade. doi: 10.1016/j.ejmech . doi: 10.18632/oncotarget.6490. doi: 10.1039/C6DT02720B. doi: 10.1016/j.molstruc . doi: 10.1016/j.saa . doi: 10.1016/j.synthmet . doi: 10.1016/j.ijbiomac . doi: 10.3906/kim- 1805-18. doi: 10.1016/j.poly . Singlet oxygen quantum yield (Φ Δ. Singlet oxygen quantum yield. determinations were carried out using the experimental set-up described in the literature [1].

Hiện trạng của lĩnh vực nghiên cứu và phát triển thuốc có sự trợ giúp của máy tính

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Ahmed et al., “Modification of Remdesivir as a Better Inhibitor of COVID-19 : A Computational Docking Study,” ChemRxiv, no. [21] Baishakhi De et al, “Computational Studies in Drug Design Against Cancer,” Anticancer Agents Med Chem, vol. Rigby, “Successful Applications of Computer Aided Drug Discovery:. Chem., vol. Kawai et al., “A comparison of the effectiveness of zanamivir and oseltamivir for the treatment of influenza A and B,” J. Infect., vol.

Synthesis and biological evaluation of new pyridines containing imidazole moiety as antimicrobial and anticancer agents

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doi:10.3906/kim-1410-25 h t t p. Most of the tested compounds exhibited promising activity.. Mechanism of the synthesis of pyridine derivatives 6a–e and 8a–e.. We extended our protocol to the synthesis of bipyridine derivatives (10–12) via reacting 5-acetylimidazole 1 (1.0 mmol) with terephthaldehyde (0.5 mmol), malononitrile (or ethyl cyanoacetate or diethyl malonate) (1.0 mmol) under optimized conditions to give the corresponding...

Synthesis and cytotoxicity evaluation of [(2,4-dichlorophenoxy)methyl]-5-aryl-1,3,4-oxadiazole/4H -1,2,4-triazole analogues

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Key words: Anticancer activity, cancer cell lines, cytotoxicity, one dose assay, oxadiazole, triazole. 1 In new cancer cases and 609,640 cancer deaths are projected to occur in the United States. 4 Extensive research and development, especially in the design and discovery anticancer agents, is the need of the present day.. 16,17 The literature on oxadizoles and our previous published work 18 is a source of inspiration to continue research on further exploration of oxadiazole, and in the present investigation

Biochemistry, 4th Edition P3

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IMP Is the Immediate Precursor to GMP and AMP 814 A DEEPER LOOK: Tetrahydrofolate and One-Carbon Units 816 HUMAN BIOCHEMISTRY: Folate Analogs as Antimicrobial and Anticancer Agents 818. 26.3 Can Cells Salvage Purines? 821 26.4 How Are Purines Degraded? 821. HUMAN BIOCHEMISTRY: Lesch-Nyhan Syndrome—HGPRT Deficiency Leads to a Severe Clinical Disorder 822 The Major Pathways of Purine Catabolism Lead to Uric Acid 822.

Recent synthetic methodologies for pyrimidine and its derivatives

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Synthesis of pyrimidine derivatives 174 and 176.. described the synthesis of different pyrimidine derivatives 183 (anticancer agents) by treating ketones 183 with acetamidines 22/guanidine 50 (Scheme 52). Preparations of pyrimidine derivatives.. Synthetic layout for the synthesis of pyrimidine derivatives 193..

Promotion of cell cycle arrest and inhibition of anchorage independent growth of cervical cancer HeLa cells by ethanol extract of croton kongensis

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Ito, Ent-kaurane Diterpenoids from Croton Tonkinensis Induce Apoptosis in Colorectal Cancer Cells Through the Phosphorylation of JNK Mediated by Reactive Oxygen Species and Dual-specificity JNK Kinase MKK4, Anticancer Agents in Medicinal Chemistry, Vol. Thang, Toxicity and Anti-Proliferative Properties of Anisomeles indica Ethanol Extract on Cervical Cancer HeLa Cells and Zebrafish Embryos, Life, Vol.

Synthesis of 2-substituted 8-propargyloxyquinoline derivatives and determination of their antioxidant, antibacterial, and DNA binding activities

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The quinoline ring plays an important role in the development of new anticancer agents as their deriva- tives have shown excellent results through different mechanisms of action such as growth inhibitors by cell cycle arrest, apoptosis, inhibition of angiogenesis, disruption of cell migration, and modulation of nuclear receptor responsiveness.

Screening of the small molecule library of Meinox enables the identification of anticancer compounds in pathologically distinct cancers

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Tumor Targeting of Polymeric Nanoparticles Conjugated with Peptides, Saccharides, and Small Molecules for Anticancer Drugs.. Boztas AO, Karakuzu O, Galante G, Ugur Z, Kocabas F et al.. Boztas AO, Karakuzu O, Galante G, Ugur Z, Kocabas F et al. Small-Molecule Screens: A Gateway to Cancer Therapeutic Agents with Case Studies of Food and Drug Administration–Approved Drugs. A Structural Perspective on the Modulation of Protein-Protein Interactions with Small Molecules.