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Showing 1 to 20 of 218 for “"Biological Evaluation"”.
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Discovery and biological evaluation of ferroptocide
… collections, and as such are a rich source for biological discovery. Herein, we subject the complexity-to-diversity library of compounds to an anticancer phenotypic screen. This effort resulted in identification of an active class of compounds derived from pleuromutilin natural product. …
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Synthesis and Biological Evaluation of Novel Glycomimetics
… enzyme assay has to be performed to confirm the biological activity of the synthesised compound. The third chapter describes the synthesis of glucose-6-phosphoramidic acid and glucose-6-triazole derivatives as inhibitors of HK II and the biological evaluation of the synthesised compounds on …
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Synthesis and Biological Evaluation of Paclitaxel Analogs
… of paclitaxel were synthesized, and their biological activities have been evaluated. For the investigation of possible synergistic effects, concurrent modifications on selected positions have been performed and their biological evaluation were studied.
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Synthesis and Biological Evaluation of Novel Epibatidine Analogues
In an effect to develop for more selective neuronal nicotinic acetylcholine receptor analgesics that have less toxicity and adverse side effects relative to epibatidine, three new classes of epibatidine analogues were synthesized and evaluated in vitro as potential potent selective nAChR ligands. …
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Design, synthesis and biological evaluation of antidiabetic agents
… prevent the formation of the RBP4-TTR complex. Biological assays (SPR, fluorometric binding assay) were performed on these compounds to verify their ability to bind within the protein cavity of RBP4 and inhibit the formation of the RBP4-TTR complex. A SAR study of compound 1 uncovered compound 4 …
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Synthesis and Biological Evaluation of 2'-Deoxyribonucleotide Analogs
Two new methods for the synthesis of 2'-deoxyribonucleosides have been developed. The first involves regioselective reductive deoxygenation of a suitably derivatized ribonucleoside. Tri-n-butyltin hydride reduction of a 2'-thiobenzoate derivative affords the desired 2'-deoxyribonucleoside in good …
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Design, synthesis and biological evaluation of bioorganometallic metallarectangles
… by cisplatin at the same concentration. Upon evaluation in a multidose screen, ligand L and metallarectangle [{Ir(μCl)(Cp*)}4(μ-L)2](OTf)4 displayed antiproliferative activity almost two-fold greater than cisplatin, in the MCF-7 cell line, while [{Ru(p-cymene)}4(μ-ƞ 2 -ƞ 2 -C2O4)2(μ-L)2](OTf)4 …
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Synthetic studies and biological evaluation of chromone - 3 - carbaldehydes
… chemistry is due to their wide range of their biological activity. In this study, three classes of target compounds were synthesized through three different pathways. The first pathway, chromone-3-carbaldehyde analogues were afforded in good to excellent yield followed by the oxidation thereof …
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Design, Synthesis and Biological Evaluation of Novel Cannabinoid Antagonist
… and keto derivatives as lead compounds for biological evaluation. Here in the design rationale, synthesis and CB1 receptor affinity for a series of 4,5-diaryl-1-substituted-1,2,3-triazoles of ester and ketones is described. These derivatives were synthesized via a one-pot regiospecific …
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Synthesis and Biological Evaluation of Rigid Analogues of Methamphetamines
<p>A series of rigid azetidenyl-based methamphetamine analogs were synthesized from commercially available <em>N</em>-Boc-azetidinone. The benzylideneazetidine analogs were prepared via a Wittig olefination via the ylides generated from the corresponding triphenylphosphonium benzylhalide salts. The …
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Synthesis, characterization, and biological evaluation of gelatin-based scaffolds
This work presents the development of entropy-elastic gelatin based networks in the form of films or scaffolds. The materials have good prospects for biomedical applications, especially in the context of bone regeneration. Entropy-elastic gelatin based hydrogel films with varying crosslinking …
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CHEMICAL SYNTHESIS AND BIOLOGICAL EVALUATION OF CHONDROITIN SULFATE DISACCHARIDES
… procurement of pure, homogenous CS motifs for biological evaluation is a challenging task due to isolation difficulty and structural complexity. To probe the ?sulfation code? in CS, a synthetic strategy was devised to obtain all 16 theoretically possible sulfation patterns in the CS repeat …
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Design, synthesis, and biological evaluation of non-symmetric smal
<p>Plasminogen activator inhibitor-1 (PAI-1) is a member of the serpin family of proteins, a primary inhibitor of both tissue-type and urokinase-type plasminogen activators in plasma, and is a well-established risk factor in various disease conditions. Increased levels of active PAI-1 in plasma are …
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Proteomics and Biological Evaluation of Marshmallow (Althea officinalis) Seeds
… However, there is no data reported on the biological activity and the structure of proteins isolated from the seeds. Therefore, this study is carried out to purify and characterize proteins and peptides from Marshmallow seeds as well as to evaluate their antimicrobial activity against …
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Synthesis and biological evaluation of potential anti-cancer agents
… combinatorial mixtures of known composition for biological testing. Novel catechol derivatives have been prepared by traditional solution-phase chemistry with the intention of transferring their synthesis to a solid-phase support. Catechol derivatives prepared were found to be active inhibitors …
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Biological Evaluation and Detoxification of Cassava (Manihot Esculenta Crantz)
Made available in DSpace on 2014-12-13T19:42:44Z (GMT). No. of bitstreams: 1 7804161.pdf: 4128816 bytes, checksum: 12fee3453ab4b6b9bc91259badddc569 (MD5) Previous issue date: 1977
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SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL ANTIPARASITIC AND ANTICANCER AGENTS
… of the work was focused on design, synthesis and biological evaluation of novel agents for the treatment of VBPDs. The first study explores the potential of nature-inspired hybrids (NIHs), a molecular hybridization approach combining distinct pharmacophores to enhance biological activity and …
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Synthesis and biological evaluation of novel small molecule bromodomain inhibitors
… human carboxyesterase 1 (CES-1) to produce the biologically-active acid. Outside of the liver, this enzyme’s expression profile is limited to the mononuclear monocyte and macrophage lineages, therefore providing the opportunity to treat immuno-inflammation diseases. The investigation of two …
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Progressing the Synthesis, Coordination Chemistry and Biological Evaluation of Phenanthrolines
The work described in this thesis concerns: (i) the synthesis and characterisation of ternary 1,10-phenenthroline/dicarboxylate Ag(I), Cu(II) and Mn(II) complexes and their in vitro/in vivo antifungal, antibacterial and antineoplastic capabilities; (ii) the development of a novel, high yielding, …
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Solid-supported synthesis of peptidoglycan fragments and their biological evaluation
In this work, a new methodology for the synthesis of peptidoglycan fragments containing (2S,6R)-A2pm is proposed. Thanks to a solid phase platform, cross metathesis was achieved between two easily manufactured chiral synthons, allylglycine anchored to a resin and vinylglycine derivatives. Due to …
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