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Full-Text Articles in Physical Sciences and Mathematics
Synthesis, Characterization And Biological Evaluation Of Pyrrolo[2,1-C][1,4]Benzodiazepines For Cytotoxicity And Serine Β-Lactamases Inhibition, Joel K. Annor-Gyamfi
Synthesis, Characterization And Biological Evaluation Of Pyrrolo[2,1-C][1,4]Benzodiazepines For Cytotoxicity And Serine Β-Lactamases Inhibition, Joel K. Annor-Gyamfi
Electronic Theses and Dissertations
Pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives possess cancerostatic and anti-infective properties thus making them candidates of possible antibacterial agents. ²-lactam antibiotics are vital weapons for the treatment of bacterial infections, but their existence and effectiveness has been faced with resistance from ²-lactamases. Therefore, the need for new effective antimicrobial drugs is very crucial. In this work, we synthesized in high yields, PBD analogs 1−3, 5 and 7−9 in three to four synthetic steps from commercially available L-proline and isatoic anhydride. MTT Assay was employed to test the in vitro cytotoxicity of PBD analogs 1, 2, 5 …
Rhenium(I) Complexes Of Tetraazatetrapyridopentacene (Tatpp): Synthesis, Characterization, Reactivity, Anticancer Potential And Luminescent Probe To Determine Cellular Localization, Pooja Ahuja
Chemistry & Biochemistry Dissertations
The ruthenium polypyridyl complexes [(phen)2Ru(tatpp)Ru(phen)2]4+ ([P]4+) and [(phen)2Ru(tatpp)]2+ ([MP]2+) are promising anti-tumor agents that arrest H358 NSCLC tumor growth in mouse tumor models and show cytotoxicity in the low micromolar range towards a number of platinum sensitive NSCLC lines (H358, H226, HOP62, H2087). Dose escalation toxicity studies in mice reveal that [MP]2+ and [P]4+ are tolerated without any short term side effects at levels up to 40 mg drug/kg mouse and >160 mg drug/kg mouse respectively with no obvious side effects, when administered as IP injection. Mechanistic studies reveal that much of the anti-tumor activity is primarily due to the …
Bioactivity/Cytotoxicity Of Micro-/Nano-Materials And Novel Development Of Fiber-Optic Probes For Single Cell Monitoring, Qingbo Yang
Doctoral Dissertations
"Manufactured nano-/micro-materials (MNMs) have been widely used and their interactions with niche biological environment are highly concerned for both of their biohazardous and bioactive effects, whereas no available comprehensive evaluations or regulations have been provided yet. This dissertation thus focuses on three major aspects: 1) fundamental toxicity understandings of a typical MNMs (zinc oxide nanoparticles), 2) bioactivity evaluations of representative bioactive MNMs, and 3) development of novel micro-probes for high spatial resolution monitoring. Firstly, the NP's concentration, irradiation, hydrodynamic size, and the localized pH, ionic strength, NP zeta-potential as well as dissolved oxygen levels were found correlated with the production …
Effect Of Disulfide Bond Scrambling On Protein Stability, Aggregation, And Cytotoxicity, Colina Dutta
Effect Of Disulfide Bond Scrambling On Protein Stability, Aggregation, And Cytotoxicity, Colina Dutta
Dissertations, Master's Theses and Master's Reports
Proteins are nano-machines that carry out majority of the cellular functions. Thermodynamically they are functional and stable within a very narrow range (1 kcal/mol). External perturbations in the form of pH change, thermal, or oxidative/reducing stress can destabilize the protein resulting in misfolding and aggregation. Prolonged environmental stress can affect the cells adaptive response resulting in loss of ability to refold or recycle proteins. This can lead to accumulation of misfolded or aggregated proteins within the cell. Such accumulation of aggregated proteins have been associated with neurodegenerative disorders such as Amyotrophic Lateral Sclerosis (ALS), Parkinson’s, Huntington’s, and Alzheimer’s disease. There …