Medicine and Health Sciences Commons^™

Synthesis And Cytotoxicity Of Azaheterocyclic Compounds, Keyur M. Pandya

Theses and Dissertations

Multicomponent coupling reactions (MCRs) have been known for a long time and one such reaction that utilizes isocyanides is Passerini reaction. It is a powerful tool to synthesize libraries of different compounds. Azaheterocyclic compounds play an important role in medicinal chemistry. Motifs such as imidazoles, piperazines, pyrazoles, pyridines, triazoles, etc. are routinely observed in several compounds of pharmacological interest. Several natural products also contain these motifs in them. We have undertaken a library synthesis of heterocyclic molecules driven by our group's long-standing interest of synthesizing medicinally relevant small molecules employing green chemistry techniques.

This thesis details our efforts on the …

Synthesis And Cytotoxicity Evaluation Of Functionalized Betulin Derivatives, Amardeep Patel

Theses and Dissertations

Betulin and betulinic acid are complex natural compounds that can be readily extracted in high quantities from external bark of yellow and white birch trees. Birch tree is native to northern New Jersey and is also commonly available for purchase as firewood. Betulinic acid is found to exhibit very good activity against few cancer cell lines, and is relatively non-toxic to normal cells. The ready availability and selective cytotoxicity coupled with the favorable therapeutic index have made betulinic acid an attractive and promising anticancer agent. However, this molecule is almost insoluble in water and shows anti-cancer activity only on very …

Novel Aminobenzoboroxoles As Potential Anti-Cancer Agents, Bhawankumar Pravinchandra Patel

Theses and Dissertations

Boronic acids are a promising class of compounds due to their wide range of applications in medicinal and materials chemistry, and as coupling agents in organic synthesis. B-hydroxy-1,2-oxaborolanes (benzoboroxoles) are categorized as cyclic boronic acid derivatives and they are very important organic molecules because of their metabolic stability and their ability to undergo important C-C bond forming reactions such as Suzuki cross coupling. Several of these cyclic boronic acids are found to have promising pharmacological properties as antifungal, antimalarial and anti-inflammatory agents. However, based on the literature reports, synthesis of highly functionalized benzoboroxoles is typically cumbersome and not very conducive …