Browsing by Subject "drug structure"

Anti-angiogenic effect of a Palladium(II)-Saccharinate Complex of Terpyridine in vitro and in vivo

Ikitimur-Armutak E.I., Gurel-Gurevin E., Kiyan H.T., Aydinlik S., Yilmaz V.T., Dimas K., Ulukaya E. (2017)

Anti-angiogenic activity of palladium (Pd)(II)-based complexes is unknown despite their quite powerful anticancer activity. This study was therefore carried out to evaluate both in vivo anti-angiogenic effect and in vitro ...

The architecture of hydrogen and sulfur σ-hole interactions explain differences in the inhibitory potency of C-β-D-glucopyranosyl thiazoles, imidazoles and an N-β-D glucopyranosyl tetrazole for human liver glycogen phosphorylase and offer new insights to structure-based design

Kyriakis E., Karra A.G., Papaioannou O., Solovou T., Skamnaki V.T., Liggri P.G.V., Zographos S.E., Szennyes E., Bokor É., Kun S., Psarra A.-M.G., Somsák L., Leonidas D.D. (2020)

C-Glucopyranosyl imidazoles, thiazoles, and an N-glucopyranosyl tetrazole were assessed in vitro and ex vivo for their inhibitory efficiency against isoforms of glycogen phosphorylase (GP; a validated pharmacological target ...

Current status and future prospects of small–molecule protein–protein interaction (PPI) inhibitors of tumor necrosis factor (TNF) and receptor activator of NF-κB ligand (RANKL)

Melagraki G., Leonis G., Ntougkos E., Rinotas V., Papaneophytou C., Mavromoustakos T., Kontopidis G., Douni E., Kollias G., Afantitis A. (2018)

The overexpression of Tumor Necrosis Factor (TNF) is directly related to the development of several autoimmune diseases, such as rheumatoid and psoriatic arthritis, inflammatory bowel disease, Crohn’s disease, refractory ...

Design and Synthesis of Type-IV Inhibitors of BRAF Kinase That Block Dimerization and Overcome Paradoxical MEK/ERK Activation

Beneker C.M., Rovoli M., Kontopidis G., Röring M., Galda S., Braun S., Brummer T., McInnes C. (2019)

Despite the clinical success of BRAF inhibitors like vemurafenib in treating metastatic melanoma, resistance has emerged through "paradoxical MEK/ERK signaling" where transactivation of one protomer occurs as a result of ...

Discovery of N-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors

Wang, S.; Midgley, C. A.; Scaërou, F.; Grabarek, J. B.; Griffiths, G.; Jackson, W.; Kontopidis, G.; McClue, S. J.; McInnes, C.; Meades, C.; Mezna, M.; Plater, A.; Stuart, I.; Thomas, M. P.; Wood, G.; Clarke, R. G.; Blake, D. G.; Zheleva, D. I.; Lane, D. P.; Jackson, R. C.; Glover, D. M.; Fischer, P. M. (2010)

Through cell-based screening of our kinase-directed compound collection, we discovered that a subset of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amines were potent cytotoxic agents against cancer cell lines, suppressed mitotic ...

Effects of short-term saffron (Crocus sativus L.) intake on the in vivo activities of xenobiotic metabolizing enzymes in healthy volunteers

Begas E., Bounitsi M., Kilindris T., Kouvaras E., Makaritsis K., Kouretas D., Asprodini E.K. (2019)

Crocus sativus L., a perennial plant grown mainly around the Mediterranean and Iran, has many medicinal properties including anti-inflammatory, anti-depressive and cancer preventing properties. Aqueous herbal extracts may ...

Glucopyranosylidene-spiro-imidazolinones, a New Ring System: Synthesis and Evaluation as Glycogen Phosphorylase Inhibitors by Enzyme Kinetics and X-ray Crystallography

Szabó K.E., Kyriakis E., Psarra A.-M.G., Karra A.G., Sipos Á., Docsa T., Stravodimos G.A., Katsidou E., Skamnaki V.T., Liggri P.G.V., Zographos S.E., Mándi A., Király S.B., Kurtán T., Leonidas D.D., Somsák L. (2019)

Epimeric series of aryl-substituted glucopyranosylidene-spiro-imidazolinones, an unprecedented new ring system, were synthesized from the corresponding Schiff bases of O-perbenzoylated (gluculopyranosylamine)onamides by ...

Halophytic herbs of the Mediterranean basin: An alternative approach to health

Petropoulos S.A., Karkanis A., Martins N., Ferreira I.C.F.R. (2018)

Wild native species are usually grown under severe and stressful conditions, while a special category includes halophytic species that are tolerant to high salinity levels. Native halophytes are valuable sources of bioactive ...

Heparin-coated extracorporeal circulation systems in heart surgery

Tagarakis, G. I.; Tsilimingas, N. B. (2009)

Despite the progress accomplished in the field of off-pump heart surgery, the vast majority of cardiac operations are still performed with the use of extracorporeal circulation, otherwise known as "heart-lung machine." ...

Marine bromophenol bis(2,3,6-tribromo-4, 5-dihydroxybenzyl)ether inhibits angiogenesis in human umbilical vein endothelial cells and reduces vasculogenic mimicry in human lung cancer a549 cells

Dong S., Chen Z., Wang L., Liu Y., Stagos D., Lin X., Liu M. (2021)

Angiogenesis, including the growth of new capillary blood vessels from existing ones and the malignant tumors cells formed vasculogenic mimicry, is quite important for the tumor metastasis. Anti-angiogenesis is one of the ...

Multicomponent reaction of aldehydes, amines and oxalacetate analogues leading to biologically attractive pyrrole derivatives

Manta S., Kollatos N., Mitsos C., Chatzieffraimidi G.-A., Papanastasiou I., Gallos J.K., Komiotis D. (2020)

Pyrrole is a very important pharmacophoric moiety. It has been widely incorporated into the skeleton of antitumor, anti-inflammatory, antibacterial, antioxidant and antifungal active substances. Access to this key heterocycle ...

A multidisciplinary study of 3-(β-D-glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors

Kun S., Begum J., Kyriakis E., Stamati E.C.V., Barkas T.A., Szennyes E., Bokor É., Szabó K.E., Stravodimos G.A., Sipos Á., Docsa T., Gergely P., Moffatt C., Patraskaki M.S., Kokolaki M.C., Gkerdi A., Skamnaki V.T., Leonidas D.D., Somsák L., Hayes J.M. (2018)

3-(β-D-Glucopyranosyl)-5-substituted-1,2,4-triazoles have been revealed as an effective scaffold for the development of potent glycogen phosphorylase (GP) inhibitors but with the potency very sensitive to the nature of the ...

Nanosystems for the encapsulation of natural products: The case of chitosan biopolymer as a matrix

Detsi A., Kavetsou E., Kostopoulou I., Pitterou I., Pontillo A.R.N., Tzani A., Christodoulou P., Siliachli A., Zoumpoulakis P. (2020)

Chitosan is a cationic natural polysaccharide, which has emerged as an increasingly interesting biomaterialover the past few years. It constitutes a novel perspective in drug delivery systems and nanocarriers’ formulations ...

Novel oligomeric proanthocyanidin derivatives interact with membrane androgen sites and induce regression of hormone-independent prostate cancer

Kampa, M.; Theodoropoulou, K.; Mavromati, F.; Pelekanou, V.; Notas, G.; Lagoudaki, E. D.; Nifli, A. P.; Morel-Salmi, C.; Stathopoulos, E. N.; Vercauteren, J.; Castanas, E. (2011)

Prostate cancer is the most common malignancy among men in Western societies, and current therapeutic approaches are evolving to manage growth, recurrence, and mortality neoplasia. Membrane androgen receptors (mARs) have ...

Petals of Crocus sativus L. as a potential source of the antioxidants crocin and kaempferol

Zeka K., Ruparelia K.C., Continenza M.A., Stagos D., Vegliò F., Arroo R.R.J. (2015)

Saffron from the province of L'Aquila, in the Abruzzo region of Italy, is highly prized and has been awarded a formal recognition by the European Union with EU Protected Designation of Origin (PDO) status. Despite this, ...

Phytogenic polyphenols as glycogen phosphorylase inhibitors: The potential of triterpenes and flavonoids for glycaemic control in type 2 diabetes

Stravodimos G.A., Chetter B.A., Kyriakis E., Kantsadi A.L., Chatzileontiadou D.S.M., Skamnaki V.T., Kato A., Hayes J.M., Leonidas D.D. (2017)

Glycogen phosphorylase (GP) is a validated pharmaceutical target for the development of antihyperglycaemic agents. Phytogenic polyphenols, mainly flavonoids and pentacyclic triterpenes, have been found to be potent inhibitors ...