Browsing by Subject "Indoles"
Now showing items 1-14 of 14
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The 1.76 Å resolution crystal structure of glycogen phosphorylase b complexed with glucose, and CP320626, a potential antidiabetic drug
(2002)CP320626, a potential antidiabetic drug, inhibits glycogen phosphorylase in synergism with glucose. To elucidate the structural basis of synergistic inhibition, we determined the structure of muscle glycogen phosphorylase ...
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Antirestenotic effects of a novel polymer-coated d-24851 eluting stent. Experimental data in a rabbit iliac artery model
(2007)Experimental and clinical data suggest that stents eluting antiproliferative agents can be used for the prevention of in-stent restenosis. Here we investigate in vitro the antiproliferative and apoptotic effect of D-24851 ...
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Cancer chemopreventive activity of brassinin, a phytoalexin from cabbage
(1995)Brassinin [3-(S-methyldithiocarbamoyl aminomethyl indole], a phytoalexin first identified as a constituent of cabbage, was synthesized and evaluated for cancer chemopreventive activity. Dose-dependent inhibition of ...
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Carzelesin phase II study in advanced breast, ovarian, colorectal, gastric, head and neck cancer, non-Hodgkin's lymphoma and malignant melanoma: A study of the EORTC early clinical studies group (ECSG)
(2000)Purpose: In a phase II trial, the activity of carzelesin, a cyclopropylpyrroloindole prodrug analog, was assessed. Patients and methods: Carzelesin was used as second- or third-line chemotherapy in patients with breast, ...
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EO9 phase II study in advanced breast, gastric, pancreatic and colorectal carcinoma by the EORTC early clinical studies group
(1996)In a phase II trial, the activity of EO9, a new bioreductive alkylating agent, was assessed. EO9 was used as second-line chemotherapy in breast cancer patients and as first-line chemotherapy for patients with gastric, ...
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Evaluation of PVP/Au nanocomposite fibers as heterogeneous catalysts in indole synthesis
(2016)Electrospun nanocomposite fibers consisting of crosslinked polyvinylpyrrolidone (PVP) chains and gold nanoparticles (Au NPs) were fabricated, starting from highly stable PVP/Au NP colloidal solutions with different NP ...
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Evaluation of PVP/Au nanocomposite fibers as heterogeneous catalysts in indole synthesis
(2016)Electrospun nanocomposite fibers consisting of crosslinked polyvinylpyrrolidone (PVP) chains and gold nanoparticles (Au NPs) were fabricated, starting from highly stable PVP/Au NP colloidal solutions with different NP ...
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Induction of discrete apoptotic pathways by bromo-substituted indirubin derivatives in invasive breast cancer cells
(2012)Indirubin derivatives gained interest in recent years for their anticancer and antimetastatic properties. The objective of the present study was to evaluate and compare the anticancer properties of the two novel bromo-substituted ...
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Kinetics, in silico docking, molecular dynamics, and MM-GBSA binding studies on prototype indirubins, KT5720, and staurosporine as phosphorylase kinase ATP-binding site inhibitors: The role of water molecules examined
(2011)With an aim toward glycogenolysis control in Type 2 diabetes, we have investigated via kinetic experiments and computation the potential of indirubin (IC 50 > 50 μM), indirubin-3'-oxime (IC 50 = 144 nM), KT5720 (K i = 18.4 ...
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Population pharmacokinetics and dynamics in phase II studies of the novel bioreductive alkylating cytotoxic indoloquinone EO9
(2001)Population pharmacokinetic-dynamic analysis was prospectively integrated in the clinical phase II programme of EO9 to determine the population pharmacokinetic profile in a larger population of patients, to estimate individual ...
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Structure-activity relationships of brassinin in preventing the development of carcinogen-induced mammary lesions in organ culture
(1994)Brassinin, a pkytoalexin, is found in Chinese cabbage. Previously, we showed that brassinin significantly inhibited dimethylbenz(a)anthracene (DMBA)-induced mammary lesions in organ culture. Moreover, it was an effective ...
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Targeting c-KIT, PDGFR in cancer of unknown primary: A screening study for molecular markers of benefit
(2008)Aims: In view of available targeted therapies, we investigated the presence of c-kit, PDGFR gene mutations and protein expression in cancer of unknown primary (CUP) in order to study their contribution in pathogenesis, ...
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Tropisetron in the prevention of acute nausea and vomiting in patients treated with high dose epirubicin
(1998)Tropisetron is a novel selective antagonist of the type-3 serotonin (5- HT3) receptor, with proven efficacy in the control of emesis related to cancer treatment. Epirubicin in doses of >100 mg/m2 has a high emetogenic ...
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Two-step total syntheses of Canthin-6-one alkaloids: New one-pot sequential Pd-catalyzed Suzuki-Miyaura coupling and Cu-catalyzed amidation reaction
(2010)"Chemical Equation Presented" Canthin-6-one (1) and nine analogues including the naturally occurring 9-methoxycanthin-6-one (2) and amaroridine (3) are prepared rapidly and in high yields via a convergent "non-classical" ...