Restricted Research - Award List, Note/Discussion Page
Fiscal Year: 2023
2308 The University of Texas at San Antonio (144196)
Principal Investigator: McHardy, Stanton
Total Amount of Contract, Award, or Gift (Annual before 2011): $ 598,305
Exceeds $250,000 (Is it flagged?): Yes
Start and End Dates: 9/1/22 - 8/31/27
Restricted Research: YES
Academic Discipline: SCIENCES
Department, Center, School, or Institute: Center For Drug Discovery
Title of Contract, Award, or Gift: Development of Potent Estrogen Receptor Beta Agonists for Treating Glioblastoma
Name of Granting or Contracting Agency/Entity:
University of Texas Health Science Center San Antonio
CFDA Link: HHS
93.395
Program Title:
none
CFDA Linked: Cancer Treatment Research
Note:
SAMs 1.1.1; The overall goal of this highly collaborative and multi-disciplinary proposal is to capitalize on preliminary data we have generated around novel small molecule ER-beta inhibitors for use in glioblastoma therapies. Dr. McHardy's lab at UTSA will focus on the design, synthesis and iterative structure-activity relationship (SAR) studies to improve the ER-beta potency and physical chemical properties of lead compounds. In collaboration with Dr. Brenner and Dr. Vadlamudi, these medicinal chemistry studies in years 1-3 plan to improve ER-beta potency, in vitro ADME characteristics and in vivo activity of lead compounds, in order to ultimately identify 2-3 select compounds for more detailed in vivo efficacy and pk work. In years 4-5 of the grant, Dr. McHardy's lab will provide all of the necessary synthesis support to provide suitable gram quantities of lead compounds for more advanced studies. Additional work will also include salt/formulation and aqueous solubility screening to support in vivo studies. All compounds prepared in the McHardy lab at UTSA will be fully characterized by 1H and 13C NMR, and HPLC/MS, targeting a chemical purity of >96% and will be registered in the CIDD compound file, and assigned a CIDD identification number. Dr. McHardy's lab will work closely with Dr. Brenner and Dr. Vadlamudi to establish an efficient synthesis/screening/data sharing strategy to support a productive iterative process to identify compounds with suitable activity to advance this ER-beta program.
Discussion: No discussion notes