Anticancer activity

Aim of the thesis: Synthesis of several derivatives and tubulysin analogues with the replacement of the amino acid methylpipecolic (Mep) at the N-terminal, replacing N,O-acetyl group by methyl group, and researching the role of tubuphenylalanine (Tup) group at the C-terminal.

26p extraenglish 24-05-2021 18 4   Download

Synthesis of several derivatives and tubulysin analogues with the replacement of the amino acid methylpipecolic (Mep) at the N-terminal, replacing N,O-acetyl group by methyl group, and researching the role of tubuphenylalanine (Tup) group at the C-terminal .

26p capheviahe27 23-02-2021 19 5   Download

Obtained by the interaction of 2-amino-3,3-dichloroacrylonitrile and chlorosulphonyl isocyanate (Z)-(5-(dichloromethylene)-2-oxoimidazolidin-4-ylidene)sulfamoyl chloride reacts easily with excess of the aliphatic amine to form new (Z)-N-(5-(dichloromethylene)-2-oxoimidazolidin-4-ylidene)-N'-substituted sulfonamides.

12p tocectocec 25-05-2020 10 1   Download

Nuclear factor erythroid-2 related factor 2 (Nrf2) is a crucial transcription factor that regulates the expression of defensive antioxidants and detoxification enzymes in cells. In a previous study, we showed that expression of the Nrf2 gene is regulated by an epigenetic modification. Rauvolfia verticillata, a traditional Chinese herbal medicine widely used in China, possesses anticancer and antioxidant effects. In this study, we investigated how Nrf2 is epigenetically regulated by reserpine, the main active component in R. verticillata, in mouse skin epidermal JB6 P+ cells.

11p caothientrangnguyen 09-05-2020 17 2   Download

Imidazolium trans-imidazoledimethyl sulfoxide-tetrachlo-roruthenate (NAMI-A) is a novel ruthenium-containing experimental antimetastatic agent. Compelling evidence ascribes apivotal role toendothelial cells in theorchestration of tumor angiogenesis and metastatic growth, suggesting antiangiogenic therapy as an attractive approach for anticancer treatment.

10p tumor12 22-04-2013 44 2   Download

A large number of bioactive peptides have been isolated from amphibian skin secretions. These peptides have a variety of actions including antibiotic and anticancer acti-vities and the inhibition of neuronal nitric oxide synthase. We have investigated the structure–activity relationship of citropin 1.1, a broad-spectrum antibiotic and anticancer agent that also causes inhibition of neuronal nitric oxide synthase, by making a number of synthetically modified analogues.

13p tumor12 20-04-2013 37 3   Download

Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) is amember of theTNFfamilyandapotent inducer of apoptosis. TRAIL has been shown to effectively limit tumor growthin vivowithout detectable cytotoxic side-effects. Interferon (IFN)-coften modulates the anticancer activities of TNF family members including TRAIL. How-ever, little is known about the mechanism. To explore the mechanism, A549, HeLa, LNCaP, Hep3B andHepG2 cells were pretreated with IFN-c, and then exposed to TRAIL.

7p awards 05-04-2013 48 4   Download

The spontaneous acquisition of resistance to a variety of unrelated cytotoxic compounds has important implications in medical treatment of infectious diseases and anticancer therapy. In the yeast Saccharomyces cerevisiaethis pheno-menon is caused by overexpression of membrane efflux pumps and is called pleiotropic drug resistance. We have found that allelic forms of the genes for the transcription activators Pdr1p and Pdr3p, designated PDR1-12and PDR3-33,respectively, mediate resistance to diazaborine....

8p dell39 03-04-2013 38 3   Download

A number of drugs used in cancer chemotherapy induce oxidative stress by generation of oxygen free radicals (ROS) which might be an alternative mechanism for their cytotoxic effect via indu-cing apoptosis. In order to clarify the roles of antioxidants in chemotherapy, we investigated Quercetin (3,3’,4’,5,7-pentahyd-roxyflavone) and N-acetylcysteine (NAC) in different cell types treated with anticancer drugs. We studied cytotoxic activity of Topotecan alone and/or in combination with Quercetin in two human breast cancer cell lines, MCF-7 and MDA-MB-231. ...

7p inspiron33 26-03-2013 56 4   Download

Saporin is a type I ribosome-inactivating protein that is often appended with a cell-binding domain to specifically target and kill cancer cells. Uroki-nase plasminogen activator (uPA)-saporin, for example, is an anticancer toxin that consists of a chemical conjugate between the human uPA and native saporin.

12p media19 04-03-2013 25 2   Download

Taxanes and other microtubule-stabilizing agents comprise an important class of anticancer drugs. It is well known that taxanes act by binding to b-tubulin on the lumenal side of microtubules. However, experimental evi-dence obtained in recent years led to the hypothesis of an external site on the microtubule wall to which taxanes and other microtubule-stabilizing agents could bind before being internalized to their lumenal site.

12p viettel02 22-02-2013 28 4   Download

In this study, curcumin, a potential anticancer agent, was found to dampen the dynamic instability of individual microtubules in living MCF-7 cells. It strongly reduced the rate and extent of shortening states, and modestly reduced the rate and extent of growing states. In addition, curcumin decreased the fraction of time microtubules spent in the growing state and strongly increased the time microtubules spent in the pause state.

12p viettel02 19-02-2013 54 5   Download

Previous studies have shown an anticancer effect of vitamin D, but the mechanisms underlying this action have not been fully explored. Here we show that 1,25-dihydroxyvitamin D3 (VD3, the active form of vitamin D) significantly promoted apoptosis in the undifferentiated gastric cancer cell line HGC-27, and this was accompanied by a concurrent increase in phos-phatase and tensin homolog deleted on chromosome 10 (PTEN) expression on VD3 treatment.

11p mobifone23 18-01-2013 42 5   Download

Tuyển tập báo cáo các nghiên cứu khoa học quốc tế ngành y học dành cho các bạn tham khảo đề tài: Anticancer activity of the iron facilitator LS081

10p toshiba22 21-11-2011 51 3   Download

Tuyển tập các báo cáo nghiên cứu khoa học ngành y học tạp chí Medical Sciences dành cho các bạn sinh viên ngành y tham khảo đề tài: Anticancer Activity of the PR Domain of Tumor Suppressor RIZ1...

7p thulanh9 07-10-2011 49 2   Download