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Full-Text Articles in Physical Sciences and Mathematics
Semi-Synthesis Of A Novel Library Of Alkaloids As Potential Selective Analgesics, Brittany M. Gallagher
Semi-Synthesis Of A Novel Library Of Alkaloids As Potential Selective Analgesics, Brittany M. Gallagher
Theses and Dissertations
Semi-synthetic compounds are an important part of the therapeutic drug discovery process. The goals of the project were to synthesize different generations of matrine analogues in order to gain many opportunities to manipulate the core structure. The long-term goal was, by manipulating the structure, the possibility to increase the biological activity of the original compound while also decreasing the toxicity. The first-generation matrine analogue allows for a synthesis similar to the Striker reaction producing aminonitriles. An alkyne coupling reaction was also possible with the modification, producing propargyl-amines. Both of the reactions resulted in the addition of a triple bond substituent …
Development Of Novel Alkaloid Derivatives For The Treatment Of Chronic Myeloid Leukemia, Lindsay Michelle Renn
Development Of Novel Alkaloid Derivatives For The Treatment Of Chronic Myeloid Leukemia, Lindsay Michelle Renn
Theses and Dissertations
The majority of chronic myeloid leukemia (CML) patients can be treated with and respond to imatinib mesylate (Gleevec). Imatinib is known to inhibit BCR-ABLl kinase activity, and is effective for the treatment of the majority of CML patients. Multiple mutations have been found in patients resistant to imatinib treatment, including many located in the BCR-ABLl tyrosine kinase domain (e.g. E255K and T315I). Matrine is a bioactive alkaloid from Sophora flavescens and has been shown to inhibit several types of cancers and is used in Chinese medicine. The goal of this study is to develop new matrine derivatives that inhibit growth …