Developing Small Molecule Inhibitors To Restore Nuclear p27 As A Novel Therapeutic Method Against Endometrial Carcinoma Developing Bivalent Molecules Against Pathogens With Antimicrobial Resistance




Journal Title

Journal ISSN

Volume Title



Development of novel therapeutics has been one of the most pivotal parts in medicinal chemistry, especially towards severe or terminal diseases. As time goes by, the research mode of interdisciplinary collaboration has greatly pushed the boundaries of new drugs, where lead compounds are identified via screening, and structure-activity relationship studies are followed up for better efficacy. Endometrial carcinoma is one of the most common cancers in the US and the world with low 5-year survival rate at its late stages. Studies of p27, a cyclin-dependent kinase inhibitor, have shown that regulating the level of p27 in the cell nucleus may serve as a new approach to treat this cancer. The lead compound was identified and synthesized with a couple of analogs. The chemistry involved and their biological activity will be discussed. Infections caused by antimicrobial resistant pathogens have been a grave threat to human health for the last few decades. Three non-antibiotic drugs, amoxapine, trifluoperazine, and doxapram, were found able to reduce the virulence in the cell upon the infection caused by various antimicrobial resistant pathogens. The synergistic effect of administering those lead drugs along with known antibiotics has been confirmed in vivo as well. Chemistry of synthesizing a bivalent molecule with one of the lead drugs attached to an antibiotic by click reaction will be discussed.



p27, ubiquitination, quinolinone, antimicrobial resistance, bivalent molecule, host directed therapeutics, click reaction