Novel anti-tumor agent
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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 Download
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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 Download
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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 Download
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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 Download
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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 Download
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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 Download
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Synovial sarcoma (SS) is a soft tissue sarcoma of unknown histogenesis. Most metastatic or unresectable cases are incurable. Novel antitumor agents and precise prognostication are needed for SS patients.
12p vimale2711 25-08-2020 10 1 Download
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Solid tumors, such as hepato-pancreato-biliary cancer, develop tumor hypoxia with tumor growth. Despite advances in surgery, a majority of these patients are in an unresectable condition. At this stage standard cytotoxic chemotherapy regimens are applied with limited success.
6p vimale2711 25-08-2020 4 1 Download
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Colorectal cancer (CRC) is the 3rd most common type of cancer worldwide. New anti-cancer agents are needed for treating late stage colorectal cancer as most of the deaths occur due to cancer metastasis. A recently developed compound, 3c has shown to have potent antitumor effect; however the mechanism underlying the antitumor effect remains unknown.
12p vimale2711 25-08-2020 5 2 Download
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While multiagent chemotherapy has dramatically improved the prognosis of sarcoma, the novel chemotherapeutics have hardly developed over the past 30 years. Caffeine can induce apoptosis, delays in cell cycle progression and can enhance the cytocidal effects of anti-cancer agents.
11p vikuala271 13-06-2020 16 1 Download
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An efficient and a novel approach for the synthesis of some novel pyrazole based-azoles are described via multi-component reaction under controlled microwave heating conditions.
12p vijiraiya2711 27-05-2020 17 1 Download
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Croton draco is an arboreal species and its latex as well as some other parts of the plant, are traditionally used in the treatment of a wide range of ailments and diseases. Alkaloids, such as magnoflorine, prevent early atherosclerosis progression while taspine, an abundant constituent of latex, has been described as a wound-healer and antitumor-agent.
21p viharuno2711 21-04-2020 11 1 Download
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From the 3-acetyl- and 3-trifluoroacetylaminoindan-1-ones obtained during the course of our work, the synthesis of novel indanes derivatives as new antitumor agents, by acidic hydrolysis of the acetamide group, diazotisation of the amino group and reduction of the carbonyl group was studied.
3p uocvong04 24-09-2015 41 2 Download
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From the 3-acetylaminoindan-1-one obtained during the course of our work, we studied the synthesis of novel indanone derivatives as new antitumor agents, by acidic hydrolysis of the acetamide group, diazotisation and alkylation of the amino group and bromination of the cyclopentanic methylene group.
3p uocvong04 24-09-2015 40 3 Download
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The benzoacronycine derivative, S23906-1, was character-ized recently as a novel potent antitumor agent through alkylation of theN2 positionof guanines inDNA.We show here that its reactivity towards DNA can be modulated by glutathione (GSH). The formation of covalent adducts between GSH and S23906-1 was evidenced by EI-MS, and the use of different GSH derivatives, amino acids and dipeptides revealed that the cysteine thiol group is absolutely required for complex formation because glutathione disul-fide (GSSG) and other S-blocked derivatives failed to react covalently with S23906-1. ...
12p fptmusic 16-04-2013 38 2 Download
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Sulfoquinovosylacylglycerols (SQAGs), in particular compounds with C18 fatty acid(s) on the glycerol moiety, may be clinically promising antitumor and⁄or immunosuppressive agents. They were found originally as inhibitors of mammalian DNA polymerases. However, SQAGs can arrest cultured mammalian cells not only at S phase but also at M phase, suggesting they have several molecular targets.
9p awards 06-04-2013 38 2 Download
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Báo cáo khoa học: Dietary antioxidant curcumin inhibits microtubule assembly through tubulin binding
Curcumin, a component of turmeric, has potent antitumor activity against several tumor types. However, its molecular target and mechanism of anti-proliferative activity are not clear. Here, we identified curcumin as a novel antimicrotubule agent. We have examined the effects of curcumin on cellu-lar microtubules and on reconstituted microtubules in vitro.
13p inspiron33 23-03-2013 51 3 Download
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Abstract Resistance to conventional anticancer therapies in patients with advanced solid tumors has prompted the need of alternative cancer therapies. Moreover, the success of novel cancer therapies depends on their selectivity for cancer cells with limited toxicity to normal tissues. Several decades after Coley's work a variety of natural and genetically modified non-pathogenic bacterial species are being explored as potential antitumor agents, either to provide direct tumoricidal effects or to deliver tumoricidal molecules.
9p toshiba23 18-11-2011 57 2 Download