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Search for "prostate cancer" in Full Text gives 42 result(s) in Beilstein Journal of Organic Chemistry.
Microwave-assisted synthesis of biologically relevant steroidal 17-exo-pyrazol-5'-ones from a norpregnene precursor by a side-chain elongation/heterocyclization sequence
Beilstein J. Org. Chem. 2018, 14, 2589–2596, doi:10.3762/bjoc.14.236
- hormones, and therefore, in the development of prostate cancer [1]. According to extensive structure–activity relationship and docking studies, a potent steroidal inhibitor should possess certain structural characteristics for efficient P45017α inhibition [1][2][3], such as (i) a five or six-membered non
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
- [4Lys(Ac)]-GnRH-III(Dau=Aoa) after 48 h or 72 h of incubation (Table 2). A similar enhanced antitumor activity was also detected for conjugates modified with acylated 4Lys in the HT-29 human colon [19], LNCaP [17] and DU145 [37] human prostate cancer cell lines compared to the conjugate containing
- responsiveness of A2058 cells. Our present results are in harmony with studies demonstrating the migration inhibitory effect of GnRH agonists on melanoma [25] and prostate cancer cell lines [54][55]. These studies also suggested that modulation of cell adhesion or actin cytoskeleton remodelling (morphological
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
- ) showed a higher antitumor effect on MCF-7 human breast, HT-29 human colon and LNCaP human prostate cancer cells in vitro than that of conjugate 4, but not of conjugate 5. Conjugates 13 and 15 containing one Mtx and one Dau were more effective only on HT-29 cells in comparison with conjugate 4
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
- ; Introduction Current cancer chemotherapy Cancer is one of the leading causes of death globally behind the heart and circulatory disorders based on statistics of World Health Organization (WHO) [1]. Among all different types of cancer, the most fatal for males are lung and prostate cancer, while for females are
- . The results demonstrated the stronger inhibition of AN-152 on the tumor with respect to the free DOX [126]. Similarly, in vivo experiments were conducted regarding AN-207 in nude mice bearing xenografts of MDA-PCa-2b prostate cancer cells, showing identical results like AN-152 [127]. Gründker et. al
- phase I and phase II studies (AN-152 was renamed to AEZS-108 for the clinical trials) of LHRH-R positive recurrent endometrial and ovarian cancers. The phase I/II study in castration-resistant prostate cancer (CRPC) and chemotherapy refractory bladder cancer also showed promising results. Due to the
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
- novel compounds to the GnRH-receptor, an in vitro ligand competition assay has been performed on human pituitary and GnRH-R positive human prostate cancer tissues. Hereby, the displacement of radiolabeled triptorelin by the unlabeled bioconjugates 1, 2, 4 and 5 was determined. For a better comparison
- slightly higher binding affinity on human prostate cancer (3.0–10.4 nM) than on human pituitary tissue (3.9–23.5 nM) being in accordance with our previous observations [29]. The lowest ligand concentration causing 50% inhibition of radioligand binding was obtained for K2 with 3.9 nM on pituitary and 3.0 nM
- on prostate cancer tissues which is only slightly higher than the reported values for GnRH-I–[D-Lys6(Dau=Aoa)] (1.6 nM and 0.9 nM) and GnRH-II–[D-Lys6(Dau=Aoa)] (4.2 nM and 2.1 nM) [29][50]. Nevertheless, it has to be considered that the determined IC50 values are within a narrow, low nanomolar range
Synthesis and evaluation of anti-oxidant and cytotoxic activities of novel 10-undecenoic acid methyl ester based lipoconjugates of phenolic acids
Beilstein J. Org. Chem. 2017, 13, 26–32, doi:10.3762/bjoc.13.4
- different cancer cell lines viz., MDA-MB-231, breast cancer (ATCC® HTB-26™); SKOV3, ovarian cancer (ATCC® HTB-77™); MCF7, breast cancer (ATCC® HTB-22™); DU 145, prostate cancer (ATCC® HTB-81™); HepG2, liver hepatocellular carcinoma (ATCC® HB-8065™) were obtained from the ATCC (Bethesda, MD, USA) and
Synthesis of acylhydrazino-peptomers, a new class of peptidomimetics, by consecutive Ugi and hydrazino-Ugi reactions
Beilstein J. Org. Chem. 2016, 12, 2865–2872, doi:10.3762/bjoc.12.285
- peptomers by Ostergaard and Holm [45]) prodrugs that can be selectively activated by prostate cancer cells. Peptidomimetics can be conveniently synthesized using the so called "submonomer approach" either in solution [41] or in solid-phase [46][47]. However, some disadvantages have been reported for long or
Synthesis and in vitro cytotoxicity of acetylated 3-fluoro, 4-fluoro and 3,4-difluoro analogs of D-glucosamine and D-galactosamine
Beilstein J. Org. Chem. 2016, 12, 750–759, doi:10.3762/bjoc.12.75
- by fluoridolysis of 1,6:3,4-dianhydro-2-azido-β-D-galactopyranose with KHF2. The amino group was introduced and masked as an azide in the synthesis. The 1-O-deacetylated 3-fluoro and 4-fluoro analogs of acetylated D-galactosamine inhibited proliferation of the human prostate cancer cell line PC-3
- leukemia cells in micromolar range (IC50 27–35 μM). Compound 5 also inhibited the proliferation of the human pancreatic cancer cell line KP1-NL (IC50 30 μM) [20] and 4-fluoro-D-glucosamine analogs 1 and 2 were reported to inhibit the proliferation of the human prostate cancer cell line PC-3 (IC50 61 µm for
- ][29]. Herein we also report on the cytotoxicity of prepared fluoro analogs in the human ovarian cancer A2780 and prostate cancer PC-3 cell lines. Preliminary results for the synthesis of compounds 5 and 6 were communicated earlier in a letter [30]. Results and Discussion Synthesis The synthesis
Self and directed assembly: people and molecules
Beilstein J. Org. Chem. 2016, 12, 391–405, doi:10.3762/bjoc.12.42
- , Defence Science and Technology Laboratory (DSTL), the Nuffield Foundation, Prostate Cancer UK, Dunhill Medical Trust, Alzheimer's Research UK (ARUK), Beckman-Coulter Inc, Zeneca Group PLC, Unipath Ltd, Smart Holograms, Glysure Ltd, Quotient Diagnostics, the Royal Society and the Royal Society of Chemistry
Synthesis, antimicrobial and cytotoxicity evaluation of new cholesterol congeners
Beilstein J. Org. Chem. 2015, 11, 1922–1932, doi:10.3762/bjoc.11.208
- antifungal activities against the filamentous fungal strain Aspergillus flavus (Link) and the yeast forming fungal strain Candida albicans (ATCC 7102) were moderate compared with amphotericin B in vitro. In the cytotoxicity study, this derivative was the most cytotoxic one against the prostate cancer PC3
- microbial organisms and the prostate cancer PC3 cell line. It is worth mentioning that the bacterial [27][28] and fungal [29][30] strains in this consideration were elected as they represent the main microbial classes for our in vitro antimicrobial evaluation. On the other hand, prostate cancer was
- group of target cholesterols were screened in vitro as cytotoxic agents against the human prostate cancer cell line PC3 using the sulforhodamine B colorimetric (SRB) assay and doxorubicin as positive control (IC50 = 8.8 μM) (Figure 3) [48]. As shown in Figure 3, cholesterol–lactoside conjugate 27
Glycodendrimers: tools to explore multivalent galectin-1 interactions
Beilstein J. Org. Chem. 2015, 11, 739–747, doi:10.3762/bjoc.11.84
- are quite homogeneous, we used these nanoparticles in cellular aggregation assays with galectin-1 and DU145 human prostate cancer cells. The DU145 cell line was chosen because it expresses a putative galectin-1 ligand – the Thomsen Friedenreich (TF) antigen on Mucin-1 [34][35]. As shown in Figure 7
Natural phenolic metabolites with anti-angiogenic properties – a review from the chemical point of view
Beilstein J. Org. Chem. 2015, 11, 249–264, doi:10.3762/bjoc.11.28
- . For example, it can inhibit androgen receptor signaling and tumor growth in athymic nude mice [87], it can cause apoptosis and cell-cycle arrest in human prostate cancer LNCaP cells [88] and in HCT-116 human colon cancer cells, and it can induce apoptosis associated with an increased level of p53 [89
The chemistry of isoindole natural products
Beilstein J. Org. Chem. 2013, 9, 2048–2078, doi:10.3762/bjoc.9.243
- yielding synthesis, ample quantities could be obtained for a preliminary evaluation of the biological activity of 79. In a first screen against A2058 melanoma and DU145 prostate cancer cell lines, 79 showed to be inactive [73]. Isoindolinones derived from isoquinoline alkaloids: The aporhoeadane alkaloids
Design and synthesis of tag-free photoprobes for the identification of the molecular target for CCG-1423, a novel inhibitor of the Rho/MKL1/SRF signaling pathway
Beilstein J. Org. Chem. 2013, 9, 966–973, doi:10.3762/bjoc.9.111
- functional activity in a PC-3 prostate cancer cell model of migration. Cells (5.0 × 105) were plated in DMEM containing 10% FBS and grown to confluence in a 12-well plate. After 24 h, a scratch was made using a 200 µL pipette tip. Medium was replaced with DMEM containing 0.5% FBS and varying concentrations
- photolabeling studies with 24 were undertaken in PC-3 prostate cancer cells. Intact cells were treated with 0.3 µM 24 for 30 min. To facilitate the identification of specifically labeled proteins, a parallel competition experiment was also performed by treating cells with 0.3 µM 24 and a large excess (10 µM) of
- with the most potent photoprobe 24 in whole prostate cancer cells was successful at detecting specific binding to one or more proteins at 24 kDa. Future work will focus on identifying the labeled protein(s). We first plan to repeat the photolabeling study with 24 and tag the labeled proteins by
Cyclodextrin-based nanosponges as drug carriers
Beilstein J. Org. Chem. 2012, 8, 2091–2099, doi:10.3762/bjoc.8.235
- effective nanotechnology for the treatment of both androgen-sensitive and castrate-refractory prostate cancer in cell-line experiments [42]. Nanosponges can be used to store and prolong the release of volatile molecules, such as essential oils, following their encapsulation. Linalool, a liquid component of
Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors
Beilstein J. Org. Chem. 2012, 8, 841–849, doi:10.3762/bjoc.8.94
- cancers was first confirmed through a study of Gorlin syndrome predisposing to basal cell carcinoma, arising from autosomal dominant mutations in Ptch [3]. Indeed, aberrant Hh signaling has been reported in a variety of other malignancy diseases, such as small-cell lung cancer, pancreatic cancer, prostate
- cancer, breast cancer and multiple myeloma [4][5][6][7][8][9]. Taken together, the development of Hh pathway antagonists has thus represented an attractive strategy for anticancer therapy [10][11]. Because mutated Ptch or Smo proteins are mostly responsible for the abnormal activation of Hh related to
Multiple hydride reduction pathways in isoflavonoids
Beilstein J. Org. Chem. 2006, 2, No. 16, doi:10.1186/1860-5397-2-16
- possible cancer preventing agents, particularly in hormone based cancers such as breast and prostate cancer. [57][58][59] Epidemiological studies have shown that they decrease the risk of colon cancer, osteoporosis, and coronary heart disease. [1][2][3] Significantly, health claims of soy foods, rich in
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