Medicinal-Pharmaceutical Chemistry Commons^™

Synthesis Of Vorinostat And Cholesterol Conjugate To Enhance The Cancer Cell Uptake Selectivity, Nethrie D. Idippily, Chunfang Gan, Paul Orefice, Jane Peterson, Bin Su Ph.D.

Chemistry Faculty Publications

Histone deacetylase (HDAC) inhibitors modulate various cellular functions including proliferation, differentiation, and apoptosis. Vorinostat (SuberAniloHydroxamic Acid, SAHA) is the first HDAC inhibitor approved by FDA for cancer treatment. However, SAHA distributes in cancer tissue and normal tissue in similar levels. It will be ideal to selectively deliver SAHA into cancer cells. Rapidly growing cancer cells have a great need of cholesterol. Low-density lipoprotein (LDL) is the major cholesterol carrier in plasma and its uptake is mediated by LDL-receptor (LDL-R), a glycoprotein overexpressed on the surface of cancer cells. Herein, we designed and synthesized a SAHA cholesterol conjugate, and further formed …

Correlation Between The Structure And The Anticorrosion Barrier Properties Of Hybrid Sol–Gel Coatings: Application To The Protection Of Aa2024-T3 Alloys, Maikki Cullen, Muhammad Morshed, Mary O'Sullivan, Emma Mchugh, Brendan Duffy, Mohamed Oubaha

Articles

Hybrid sol–gel materials have been extensively studied as viable alternatives to toxic chromate (VI)-based coatings for the corrosion protection of AA2024-T3 in the aerospace industry, due to the wide range of available chemistries they offer and the tremendous development potential of innovative functional coatings. However, so far, little work has been performed in identifying the effect of the employed chemistries on the structure and anticorrosion properties of the coatings. This work proposes to contribute to a better understanding of the relationship existing between the structure, morphology and anticorrosion properties of hybrid sol–gel coatings deposited on AA2024- T3 aluminium surfaces, the …

Analysis Of Novel Cyanide Antidote Dimethyl Trisulfide For Pharmacokinetic Studies, And Sulfur Mustard Metabolites For Identification Of Biomarker Of Inhaled Dose, Erica Manandhar

Electronic Theses and Dissertations

Cyanide poisoning by accidental or intentional exposure poses a severe health risk. The current FDA approved antidotes for cyanide poisoning can be effective, but each suffers from specific major limitations. Dimethyl trisulfide (DMTS), a sulfur donor that detoxifies cyanide by converting it into thiocyanate, is a promising next generation cyanide antidote. Although a validated analytical method to analyze DMTS is not currently available from any matrix, one will be vital for the approval of DMTS as a therapeutic agent against cyanide poisoning. Hence, a stir bar sorptive extraction (SBSE) gas chromatography – mass spectrometry (GC-MS) method was developed and validated …

Structure And Characterization Of A Class 3b Proline Utilization A: Ligand-Induced Dimerization And Importance Of The C-Terminal Domain For Catalysis, David A. Korasick, Thameesha T. Gamage, Shelbi Christgen, Kyle M. Stiers, Lesa J. Beamer, Michael T. Henzl, Donald F. Becker, John J. Tanner

Department of Chemistry: Faculty Publications

The bifunctional flavoenzyme proline utilization A (PutA) catalyzes the two-step oxidation of proline to glutamate using separate proline dehydrogenase (PRODH) and L-glutamate-y-semialdehyde dehydrogenase active sites. Because PutAs catalyze sequential reactions, they are good systems for studying how metabolic enzymes communicate via substrate channeling. Although mechanistically similar, PutAs vary widely in domain architecture, oligomeric state, and quaternary structure, and these variations represent different structural solutions to the problem of sequestering a reactive metabolite. Here, we studied PutA from Corynebacterium freiburgense (CfPutA), which belongs to the uncharacterized 3B class of PutAs.A2.7A˚ resolution crystal structure showed the canonical arrangement of PRODH, L-glutamate-y-semialdehyde dehydrogenase, …

Clozaril, Gillian Jones

Natural Sciences Student Research Presentations

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Clozaril (Clozapine, Fazaclo, Versacloz) an atypical antipsychotic used to manage schizophrenia and schizoaffective disorder as well as bipolar disorder, dementia-related behavior disorders, and tremors.

Prednisone, Donna K. Broderick

Natural Sciences Student Research Presentations

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Predinisone, trade name Deltasone, Apo-Prednisone, Meticorton, Orasone, Panasol, Panasal, Prenicen-M Sterapred, Winred, an adrenal corticosteroid used to treat a variety of symptoms.

Aricept, Colleen M. Westburg

Natural Sciences Student Research Presentations

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Donepizil Hydrocholide, trade name Aricept, used to treat the symtoms of mild, moderate, or severe dementia of Alzheimer’s type. Unlabeled uses include treatment of symptoms of vascular dementia, poststroke aphasia, and memory improvement in multiple sclerosis patients.

Sertraline Hydrochloride, Michelle L. Fehr

Natural Sciences Student Research Presentations

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Sertraline Hydrochloride, trade name Zoloft, used to treat the symptoms of depression, obsessive compulsive disorder, panic disorder, social anxiety disorder, premenstual dysphoric disorder, generalized anxiety, and post-traumatic stress disorder.

Benazepril Hydrochloride, Tuan A. Nguyen

Natural Sciences Student Research Presentations

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Benazepril Hydrochloride, trade names Briem, Cibacen, Fortekor, and Iotensin, used to treat mild to moderate hypertension.

Lunesta, Mary Kreie

Natural Sciences Student Research Presentations

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Eszopiclone, trade name Lunesta, used to treat insomnia.

Zoloft/Sertraline Hcl, Loretta Banks

Natural Sciences Student Research Presentations

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Sertraline Hydrochloride, trade name Zoloft, used to treat the symptoms of depression, obsessive compulsive disorder, panic disorder, social anxiety disorder, premenstual dysphoric disorder, generalized anxiety, and post-traumatic stress disorder.

Nortriptyline Hyrdochloride, Israel R. Gomez Raffoul

Natural Sciences Student Research Presentations

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Nortriptyline Hydrochloride, trade names Acetexa, Allegron, Aventyl, Noritren, Nortrilen, Sensaval, and Vividyl, used to treat endogenous drpression. Unlabeled uses include treatment of nocturnal enuresis in children, ADJD, and diabetic neuropathy.

Citalopram Hydrobromide, Maria Parks

Natural Sciences Student Research Presentations

This poster, presented at the Natural Sciences Poster Session at Parkland College, provides the chemical makeup, dosage, and effects of Citalopram Hydrobromide, trade name Celexa, used to treat depression.

Naloxone Therapy In Opioid Overdose Patients: Intranasal Or Intravenous?, Leiah Carney

Natural Sciences Student Research Presentations

This slide presentation for the Natural Science Poster Session at Parkland College describes the chemical makeup and effect of Naloxone, an opioid antagonist used in the treatment opioid overdose and summarizes a study comparing intravenous and intranasal delivery methods. Concludes that although there are conflicting studies, evidence supports intranasal delivery.

Target Based Design And Synthesis Of Heterocycles In The Potential Treatment Of Cancer And Opportunistic Infection, Shruti Choudhary

Electronic Theses and Dissertations

Dose limiting toxicity and development of multidrug resistance by the tumors are the major limitations of current cancer chemotherapy. Microtubule targeting agents (MTAs) are a structurally diverse set of compounds that disrupt microtubule dynamics and exert their anticancer effect. Among the various classes of such agents, the colchicine site binding agents are particularly important as they circumvent the Pgp and β-III tubulin mediated clinical resistance. These resistance mechanisms, when manifested, are a major reason for the failure of clinically used agents such as taxanes and vinca alkaloids. A series of monocyclic pyrimidine analogs were designed and synthesized as colchicine site …

Nitric Oxide Release From Poly(Lactic-Co-Glycolic Acid) Nanoparticles And Titanium Alloy, Nina A. Reger

Electronic Theses and Dissertations

Current methods for the treatment of bacterial infection involve the use of systemic antibiotics, which are high concentrations of antibiotics delivered over a long period time. Unfortunately, the use of systemic antibiotics can cause harmful side effects to the patient and increases the possibility for antibiotic resistance. The delivery of antibiotics or alternative antimicrobial compounds, such as nitric oxide, directly to the site of infection would decrease the amount of antibiotic necessary to treat a bacterial infection.

Poly (lactic-co-glycolic acid)/polyvinyl alcohol nanoparticles and a titanium- aluminum-vanadium metal oxide alloy implant were surface functionalized to deliver nitric oxide. Polymer nanoparticles can …

Literature Review On The Use Of Nucleic Acid-Based Logic Gates For The Detection Of Human Diseases, Enrique J. Blanco Martinez

Honors Undergraduate Theses

Conventional methods for diagnosis of human disease are, at times, limited in different regards including time requirement, either experimental or data processing, sensitivity, and selectivity. It is then that a Point of Care Criteria, which considers the true utility and usefulness of the device, is employed to propose new diagnostic devices capable of overcoming the aforementioned shortcomings of conventional tools. Nucleic acid, characterized for its predictable base-pairing nature, is considered to be a highly-selective, yet greatly modifiable device. Its behavior is then described through Boolean Logic, where “true” or “false” outputs are mathematically described as “1” and “0”, respectively. This …

Development Of Diverse Size And Shape Rna Nanoparticles And Investigation Of Their Physicochemical Properties For Optimized Drug Delivery, Daniel L. Jasinski

Theses and Dissertations--Pharmacy

RNA nanotechnology is an emerging field that holds great promise for advancing drug delivery and materials science. Recently, RNA nanoparticles have seen increased use as an in vivo delivery system. RNA was once thought to have little potential for in vivo use due to biological and thermodynamic stability issues. However, these issues have been solved by: (1) Finding of a thermodynamically stable three-way junction (3WJ) motif; (2) Chemical modifications to RNA confer enzymatic stability in vivo; and (3) the finding that RNA nanoparticles exhibit low immunogenicity in vivo.

In vivo biodistribution and pharmacokinetics are affected by the physicochemical …

Phage Display To Identify Functional Resistance Mutations To Rigosertib, Nedim Filipovic

CMC Senior Theses

In vitro protein selection has had major impacts in the field of protein engineering. Traditional screens assay individual proteins for specific function. Selection, however, analyzes a pool of mutants and yields the best variants. Phage display, a successful selection technique, also provides a reliable link between variant phenotype and genotype. It can also be coupled with high throughput sequencing to map protein mutations; potentially highlighting vital mutations in variants. We propose to apply this technique to cancer therapy. RAF, a serine/threonine kinase, is critical for cell regulation in mammals. RAF can be activated by oncogenic RAS, found in over 30% …

Ligands Of Therapeutic Utility For The Liver X Receptors., Rajesh Komati, Dominick Spadoni, Shilong Zheng, Jayalakshmi Sridhar

Faculty and Staff Publications

Liver X receptors (LXRs) have been increasingly recognized as a potential therapeutic target to treat pathological conditions ranging from vascular and metabolic diseases, neurological degeneration, to cancers that are driven by lipid metabolism. Amidst intensifying efforts to discover ligands that act through LXRs to achieve the sought-after pharmacological outcomes, several lead compounds are already being tested in clinical trials for a variety of disease interventions. While more potent and selective LXR ligands continue to emerge from screening of small molecule libraries, rational design, and empirical medicinal chemistry approaches, challenges remain in minimizing undesirable effects of LXR activation on lipid metabolism. …