Research Overview - Dr. Lili Ma

The Ma research group is in the area of organic, medicinal and biochemistry, with particular interests in the following fields:

Design and synthesis of bioactive molecules

To develop novel organic transformations for bioactive scaffold construction using transition metal catalysts.
To investigate organic reaction mechanisms using modern techniques such as NMR, isotope labelling, etc.
To develop highly efficient organic reactions under microwave irradiation.

Biological evaluation of small molecules

To evaluate inhibitor potencies in enzyme inhibition assay.
To understand structure activity relationship (SAR).

Molecular modeling using GOLD and MOE programs

To guide the design of drug candidates.
To rationale crucial ligand/receptor interactions.

Undergraduates in the Ma's lab receive training in the design, synthesis, biological evaluation and computer modeling of bioactive molecules and their application in health-related areas.

Research Project Specifications

Gold and Palladium-catalyzed Organic Reactions under Microwave Irradiation

Transition metal-catalyzed organic reactions have long been an important field in organic laboratory and pharmaceutical industry. Gold and palladium catalysis is especially useful in the synthesis of bioactive compounds for drug discovery because of their broad substrate scope and diverse product scaffolds. We are interested to develop highly efficient gold or palladium-catalyzed organic reactions for the synthesis of bioactive molecules. Microwave irradiation is employed for faster and cleaner reactions. Isotope-labeled compounds and NMR techniques are used to study reactive intermediates and to probe the reaction mechanisms. Information on these fundamental steps is valuable in designing new gold or palladium catalysts or developing new synthetic methods.

Development of Anti-Breast Cancer Drug Candidates

Breast cancer is the second most common type of cancer after lung cancer. Most breast cancers are estrogen receptor positive and estrogen is the main stimulant in the growth of tumor cells. The traditional breast cancer therapy is to block the function of estrogen by medicines such as Tamoxifen. A new promising hormonal treatment is to prevent the synthesis of estrogen by aromatase inhibitors. Research in the Ma group involves the design and synthesis of novel aromatase inhibitors originated from bioactive natural products such as Biochanin A, Genistein and Liquiritigenin. We are currently focusing on the design and synthesis of isoflavone and isocoumarin compounds. The bioactivity of synthesized compounds is evaluated in enzyme inhibition assay. Computer modeling is utilized to rationale crucial enzyme-inhibitor interactions.

Development of Xanthine Oxidase Inhibitors

Xanthine oxidase (XO) plays an important role in purine catabolism by catalyzing the conversion of xanthine and hypoxanthine to uric acid. Chalcones and caffeic acid phenethyl esters (CAPEs) are natural products with a broad range of bioactivities that are widely found in the plant kingdom. These compounds combine good inhibitory potency against xanthine oxidase with high radical scavenging ability in a single molecule, providing potential therapeutic value in the treatment diseases related to hyperuricemia (a condition associated with elevated levels of uric acid in the blood) and/or elevated level of reactive oxygen species (ROS). These diseases include gout, cardiovascular and chronic kidney diseases, cancer, neuropathy, inflammatory diseases, and reperfusion injuries. The synthesis and development of chalcone and CAPE derivatives is conducted in the Ma research lab at NKU. The biological evaluation and computer modeling of charcone and CAPE derivatives are performed in the Paula research lab at Purdue University.