ACS South Jersey Local Section Meeting

November 2023 Special Seminar Event!

Dr. Jacqueline Smith

Multicomponent Reactions in the Synthesis of New Cancer Drugs 

November 28^th, 2023

Time: 5:30PM Social Reception - Science Hall 329

6:30 PM Seminar - Science Hall 324

Rowan University 

Science Hall Room 

201 Mullica Hill Rd, Glassboro, NJ 08028

Abstract

Multicomponent reactions are highly useful in organic synthesis as they create complex molecules in fewer synthetic steps and require fewer purification processes. These reactions are well-known for creating aromatic heterocycles which have utility in many areas of chemistry, especially drug discovery. Aromatic heterocycles are often privileged scaffolds that show high efficacy in biological system. Therefore, the ease of access provided by MCRs allows libraries of compounds to be designed through the modulation of one or more reagents. The Groebke-Blackburn-Bienayme' Reaction (GBBR) is a well-known MCR which has been used to form a variety of heterocyclic compounds.

In recent years several treatments for cancer have been developed. Despite these gains, the development of resistance remains a challenge. About 25% of women with ER+ breast cancer experience recurrence within 5 to 10 years of treatment. Over the past few decades, studies have shown that cancer cells exploit the body’s natural repair systems in order to avoid death. One such system is the Ubiquitin Proteasome System (UPS). This system is responsible for the degradation of mis- or unfolded proteins through the proteasome. A key component of the UPS is the valosin-containing protein (VCP). VCP is an ATPase that hydrolyzes ATP to provide the energy required for ubiquitin-tagged proteins to reach the proteasome. Small molecules have been designed to inhibit VCP by binding to its enzyme active site or an allosteric site. We have designed new compounds to target VCP through a novel microwave-assisted GBB multicomponent reaction that uses acyclic amidines. This approach allows for the derivatization of up to three aromatic rings which can produce a small library of more than 60 compounds. Molecular docking has shown that these compounds are likely to be binders of VCP and preliminary testing for enzymatic activity is underway. Ultimately expanding the scope of the GBBR will allow a variety of novel compounds to be designed as potential VCP inhibitors.

Location:  The November meeting will be held at Rowan University.  There will be a social hour at   530PM with the seminar following at 630PM

There is no cost associated with attending this event. 

Please RSVP by 11/22 here:

Parking on campus: 

Our guests will need to go to https://rowanu.thepermitstore.com/ and select Guest Permits. From there, you can click on Search and a list of different permit options will drop down. Please select “Request for Temp Pass 2023-2024” and add the item to their cart. The item is free of charge but you will still need to check out as if purchasing it. During check out, you will need to create an account to complete the order. When creating account, you’ll enter all the necessary information the Parking office needs (Plate #, Make/Model, etc). Once the order request is approved, the Parking Office will email them an electronic temporary pass.

Speaker Bio: Dr. Jacqueline Smith completed her undergraduate studies at the University of Maryland Baltimore County (UMBC) where she was a part of the Meyerhoff Scholarship Program. She earned her Ph.D. in Chemistry from the University of Maryland College Park under Dr. Herman Sintim and conducted postdoctoral research at Georgetown University in the Drug Discovery Lab of Dr. Milton Brown. She is currently an Associate Professor of Chemistry at Bowie State University, an HBCU in Maryland. Since arriving at Bowie in 2016, Jacqueline has developed a research program focused on small molecule therapeutics to target resistant breast cancer and as bioanalytical tools for drug delivery. Dr. Smith is co-author of several peer-reviewed publications and has 2 US Patents. Dr. Smith has also earned substantial funding from the NSF including the HBCU-UP Research Initiation Award (2020), CAREER Award (2023) and Excellence in Research Award (2023). Since 2016 Dr. Smith has mentored over 30 undergraduate students in her lab. Several of Dr. Smith's students continue to pursue research in graduate school or post baccalaureate programs while many others enter professional school. Dr. Smith has a passion for outreach and works with local schools to enhance K-12 exposure to STEM.

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