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Antitumor agents
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Ebook "Stereoselective desymmetrization methods in the assembly of complex natural molecules" describes the inception, design, and implementation of stereoselective desymmetrization reactions in the total synthesis of the natural products pactamycin and paspaline. In the case of pactamycin, the author develops a novel asymmetric Mannich reaction and symmetry-breaking reduction strategy to enable facile construction of the complex core architecture in fifteen steps using commercially available materials – the shortest synthesis to date.
290p
tracanhphuonghoa1007
22-04-2024
6
2
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Selective activation of Delta-like 1 (DLL1)-Notch signaling is a new approach to activate CD8+ T cell and suppress tumor growth, while the efficacy remains modest. Lentinan (LNT) is a clinically used immunomodulation agent. Thus, we hypothesized that LNT could improve the efficacy of DLL1.
11p
vialfrednobel
23-12-2023
4
3
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In this paper, we report the synthesis of five new 4-aza-2,3-didehydropodophyllotoxins by a straightforward multicomponent reaction in the hope of finding new structures with interesting anticancer activity. The novelty in our work is the preparation of quinoline structural compounds of podophyllotoxin derivatives, in two simple steps, having functional groups which are available for further modifications.
8p
vidudley
20-02-2023
6
2
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Quercetin, a multifunctional therapeutic agent, is used in various types of cancer. However, its therapeutic effect is limited by virtue of poorly aqueous solubility and instability in the physiological medium. To overcome these limitations, we aimed (i) to design quercetin loaded liposomes with unlinked-PEG4000 with regard to not only surface modification but also solubility enhancement, and (ii) to investigate the antineoplastic effects on HeLa cells.
13p
lyhuyenthu
31-01-2023
2
2
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Several studies have demonstrated the antitumor activity of rosiglitazone (RGZ) in cancer cells, including breast cancer cells. However, the molecular targets of RGZ in the inhibition of angiogenesis in breast cancer cells remain unclear.
17p
vihagrid
30-01-2023
7
3
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The objective of this study was to evaluate the toxicity assessment of Pseudomonas silesiensis strain A3 CuNPs against human normal (Wi38) and cancer (A549) cell lines as well as antimicrobial activity agent.
8p
schindler
30-12-2021
8
0
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Novel benzimidazolium bromides salts having (4-methoxyphenyl)ethyl, (phthalimide-2-yl)methyl, 4-nitrobenzyl, 2-phenylethyl, penthyl, or allyl groups were synthesized and their characterizations were conducted by 1 H and 13 C NMR and IR spectroscopic methods, and microanalysis. In vitro antitumor activities of the novel benzimidazole compounds (1–7) were determined by using ovarian (A2780) and prostate (PC-3) cancer cell lines. Antitumor properties of all compounds were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.
22p
langthannam
29-12-2021
3
0
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Signaling through VEGF/VEGFR induces cancer angiogenesis and affects immune cells. An increasing number of studies have recently focused on combining anti-VEGF/VEGFR agents and immune checkpoint inhibitors (ICIs) to treat cancer in preclinical and clinical settings. BD0801 is a humanized rabbit anti-VEGF monoclonal antibody in the clinical development stage.
14p
vimahuateng
26-11-2021
4
0
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Hepatocellular carcinoma (HCC) is the most common primary liver malignancy and is a leading cause of cancer-related death worldwide. However, there is no effective chemotherapeutic treatment for HCC and its prognosis remains poor. Consequently, it is urgent to find an efficient antitumor agent to treat HCC. In this study, 7-ethyl-10- hydroxycamptothecin (SN38), the bioactive metabolite of the anticancer drug irinotecan (CPT-11), which is 100–1000 times more potent than CPT-11, was coupled with aspirin to give 4 prodrugs. Their structures were characterized by 1H NMR and elemental analysis.
11p
tudichquannguyet
29-11-2021
12
2
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Cancer is one of the main global health problems. In order to develop novel antitumor agents, we synthesized 3,4-dihydropyrimidine-2(1H)-one (DHPM) and 2,6-diaryl-substituted pyridine derivatives as potential antitumor structures and evaluated their cytotoxic effects against several cancer cell lines. An easy and convenient method is reported for the synthesis of these derivatives, employing cobalt ferrite (CoFe 2 O4 @SiO2 -SO3 H) magnetic nanoparticles under microwave irradiation and solvent-free conditions.
20p
tudichquannguyet
29-11-2021
7
1
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3-acetyl coumarin derivatives (1a-d) are formed as a result of condensation of salicylaldehyde derivatives and ethyl acetoacetate and were converted into coumarin-selenophene hybrid compounds (2a-d) in the basic medium by modified Gewald reaction in the presence of malononitrile and selenium. Products are characterized by nuclear magnetic resonance (NMR). The prepared compounds are screened for their anticancer activity against DU-145 cell line. In addition, selected target compounds are evaluated for apoptosis and oxidative stress on DU-145 (prostate carcinoma) cell lines.
16p
tudichquannguyet
29-11-2021
10
1
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The clinical use of cisplatin, which is a first-line anticancer agent, is highly restricted due to its adverse effects on kidneys that lead to nephrotoxicity. Therefore, some potential reno-protective substances have been used in combination with cisplatin to cope with nephrotoxicity. Due to its high antitumor activity and oxygen-carrying capacity, we investigated the molecular effects of squalene against cisplatin-induced oxidative stress and kidney damage in mice. Single dose of cisplatin (7 mg/kg) was given to male Balb/c mice.
10p
thiencuuchu
27-11-2021
15
1
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Albendazole (ABZ) is a microtubule-targeting anthelmintic with a remarkable activity against a variety of human cancer cells. In this study, we examined if the antitumor activity of ABZ could be enhanced by its combination with other microtubule-binding agents.
13p
vijisoo2711
29-09-2020
13
1
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Survivin, a member of the family of inhibitor of apoptosis proteins, functions as a key regulator of mitosis and programmed cell death. YM155, a novel molecular targeted agent, suppresses survivin, which is overexpressed in many tumor types. The aim of this study was to determine the antitumor activity of YM155 in SK-NEP-1 cells.
13p
vijisoo2711
30-09-2020
7
1
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Melanoma represents one of the most aggressive and therapeutically challenging malignancies as it often gives rise to metastases and develops resistance to classical chemotherapeutic agents. Although diverse therapies have been generated, no major improvement of the patient prognosis has been noticed.
11p
vijennie2711
29-09-2020
34
1
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Zalypsis® is a marine compound in phase II clinical trials for multiple myeloma, cervical and endometrial cancer, and Ewing’s sarcoma. However, the determinants of the response to Zalypsis are not well known. The identification of biomarkers for Zalypsis activity would also contribute to broaden the spectrum of tumors by selecting those patients more likely to respond to this therapy.
10p
virose2711
24-09-2020
14
0
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Celastrol is a promising anti-tumor agent, yet it also elevates heat shock proteins (HSPs), especially HSP70, this effect believed to reduce its anti-tumor effects. Concurrent use of siRNA to increase celastrol’s antitumor effects through HSP70 interference has been reported, but because siRNA technology is difficult to clinically apply, an alternative way to curb unwanted HSP70 elevation caused by celastrol treatment is worth exploring.
9p
virose2711
25-09-2020
15
1
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Natural products from plants have been proven to be important resources of antitumor agents. In this study, we exploited the antitumor activity of (E)-3-(4-chlorophenyl)-N-(7-hydroxy-6-methoxy-2-oxo-2Hchromen-3-yl) acrylamide (SC-III3), a newly synthesized derivative of scopoletin, by in vitro and in vivo experiments.
13p
vialabama2711
21-09-2020
14
3
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Patients with dedifferentiated or anaplastic thyroid carcinomas currently lack appropriate treatment options. Kinase inhibitors are among the most promising new agents as alternative strategies. The BRAF- and multi-kinase inhibitor, sorafenib, has already shown antitumor effects in thyroid carcinoma patients in a phase III clinical trial.
13p
vialabama2711
21-09-2020
14
0
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The lymph node metastasis is a key early step of the tumor metastatic process. VEGFD-mediated tumor lymphangiogenesis plays a key role, since down-regulation of p-VEGFR-3 could block the lymph node metastasis.
12p
viamsterdam
18-09-2020
11
1
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