Design and development of bioactive compounds: Targeting HIV-1 protease, neuronal PDZ, and anticancer analogs of heterolignans.

摘要

In my current doctoral research study, I worked on projects that were of bioorganic/medicinal chemistry in nature, with a main goal geared toward discovery of molecules that have a biological activity, and may ultimately on further refining be made into drugs. The first project was a method study of the aza-Diels-Alder reaction in the synthesis of anticancer heterolignans using traditional chemistry. The results show that the reaction is not concerted rather it is a stepwise reaction. The second project involved synthesis of dehydroalanine peptides and E-alkene dipeptide isosteres that act as PDZ3 binders. The last project was on synthesis of reduced peptides that inhibit HIV-1 protease enzyme and in so doing are capable of crystallizing in the HIV-1 protease. The X-ray crystal structures obtained would enable design of better drugs that profile lopinavir.