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Search for "daunorubicin" in Full Text gives 6 result(s) in Beilstein Journal of Organic Chemistry.
Synthesis of a tubugi-1-toxin conjugate by a modulizable disulfide linker system with a neuropeptide Y analogue showing selectivity for hY1R-overexpressing tumor cells
Beilstein J. Org. Chem. 2019, 15, 96–105, doi:10.3762/bjoc.15.11
- [36][37]. However, in most cases they lost more or less the hY1R binding, or selectivity, or receptor-activation efficacy, and had low metabolic stability. Besides diagnostic approaches, several therapeutic NPY-derived PDCs have been reported. Langer and co-workers conjugated daunorubicin and
Comparative cell biological study of in vitro antitumor and antimetastatic activity on melanoma cells of GnRH-III-containing conjugates modified with short-chain fatty acids
Beilstein J. Org. Chem. 2018, 14, 2495–2509, doi:10.3762/bjoc.14.226
- cell responses, and (iii) to compare the activities of conjugates with the free drug. Results: In the tested conjugates, daunorubicin (Dau) was coupled to 8Lys of GnRH-III (GnRH-III(Dau=Aoa)) or its derivatives modified with 4Lys acylated with short-chain fatty acids (acetyl group in [4Lys(Ac)]-GnRH
- of GnRH, could display strong antiproliferative effects in the breast, prostate, colon carcinoma cell lines, whereas induce 500–1000 times less LH-release than GnRH-I derivatives [14]. In our previous studies, the side chain of Lys8 was used for attachment of daunorubicin (Dau) via a more stable
- 2.5% water (v/v/v) for 2.5 h at room temperature (rt) and then precipitated with ice-cold diethyl ether followed by purification on RP-HPLC. Daunorubicin was attached to the purified peptides via oxime linkage that was formed under slightly acidic conditions (0.2 M NH4OAc buffer at pH 5) at rt
Drug targeting to decrease cardiotoxicity – determination of the cytotoxic effect of GnRH-based conjugates containing doxorubicin, daunorubicin and methotrexate on human cardiomyocytes and endothelial cells
Beilstein J. Org. Chem. 2018, 14, 1583–1594, doi:10.3762/bjoc.14.136
- Chemistry, Pázmány P. stny 1/A, Hungarian Academy of Science, Budapest, 1117, Hungary 10.3762/bjoc.14.136 Abstract Background: Cardiomyopathy induced by the chemotherapeutic agents doxorubicin and daunorubicin is a major limiting factor for their application in cancer therapy. Chemotactic drug targeting
- -conjugates containing doxorubicin, daunorubicin and methotrexate were investigated in this study. Their cytotoxicity was determined on primary human cardiac myocytes (HCM) and human umbilical vein endothelial cells (HUVEC) using the xCELLigence SP system, which measures impedance changes caused by adhering
- cells on golden electrode arrays placed at the bottom of the wells. Slopes of impedance–time curves were calculated and for the quantitative determination of cytotoxicity, the difference to the control was analysed. Results: Doxorubicin and daunorubicin exhibited a cytotoxic effect on both cell types
On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site
Beilstein J. Org. Chem. 2018, 14, 930–954, doi:10.3762/bjoc.14.80
- anticancer drugs utilized to treat malignancies at the moment. Among this large pool of cytotoxic drugs, an array of them has been utilized as toxic warheads in PDCs and five representative examples are gemcitabine, doxorubicin, daunorubicin, paclitaxel and camptothecin (Figure 4). The main drawback of these
- therapeutic window of the parent cytotoxic agent. Since different drugs may employ a different mechanistic approach to kill cells, the appropriate drug is selected according to features characterizing the targeted cancerous cells. For instance, daunorubicin and doxorubicin possess similar mechanisms of action
- highlighted in Figure 4. Anthracyclines: Anthracyclines are among the main anti-cancer drugs that are applied in combinations with other chemotherapeutic agents. They are utilized against a variety of cancers including leukemias, lymphomas, breast, ovarian, bladder and lung. Daunorubicin (Dau) was the first
Synthesis and in vitro biochemical evaluation of oxime bond-linked daunorubicin–GnRH-III conjugates developed for targeted drug delivery
Beilstein J. Org. Chem. 2018, 14, 756–771, doi:10.3762/bjoc.14.64
- reported on the identification of a novel daunorubicin–GnRH-III conjugate (GnRH-III–[4Lys(Bu), 8Lys(Dau=Aoa)] with efficient in vitro and in vivo antitumor activity. To get a deeper insight into the mechanism of action of our lead compound, the cellular uptake was followed by confocal laser scanning
- microscopy. Hereby, the drug daunorubicin could be visualized in different subcellular compartments by following the localization of the drug in a time-dependent manner. Colocalization studies were carried out to prove the presence of the drug in lysosomes (early stage) and on its site of action (nuclei
- after 10 min). Additional flow cytometry studies demonstrated that the cellular uptake of the bioconjugate was inhibited in the presence of the competitive ligand triptorelin indicating a receptor-mediated pathway. For comparative purpose, six novel daunorubicin–GnRH-III bioconjugates have been
Marine-derived myxobacteria of the suborder Nannocystineae: An underexplored source of structurally intriguing and biologically active metabolites
Beilstein J. Org. Chem. 2016, 12, 969–984, doi:10.3762/bjoc.12.96
- derivatives 12 and 13. Phenylnannolone A was proven to restore daunorubicin sensitivity in cancer cells by inhibiting P-glycoprotein (P-gp), an ATP-binding cassette transporter (ABC transporter). In tumor cells, P-gp serves as an efflux transporter of drugs, ultimately leading to treatment failure [46]. Apart
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