Abstract by Reuben Dass

Personal Infomation

Presenter's Name

Reuben Dass

Degree Level



JD Singleton
Alex Quinn

Abstract Infomation


Chemistry and Biochemistry

Faculty Advisor

Matt Peterson


Synthesis and biological evaluation of novel pyrazolo[1,5-a]pyrimidines: Discovery of a selective inhibitor of JAK1 JH2 pseudokinase and VPS34


A series of novel 3,6-di-substituted or 3-substituted pyrazolo[1,5-a]pyrimidines were prepared via a microwave-assisted approach that generated a broad array of derivatives in good yields (average = 59%). The synthesized compounds were screened for antimitotic activities against MCF7 breast cancer and/or A2780 ovarian 
cancer cell lines in vitro. The most active compounds exhibited EC50 values ranging from 0.5 - 4.3μM, with two derivatives (34e and 35a) being two-three fold more active than Compound C (Dorsomorphin) in A2780 and MCF7 assays, respectively. A monosubstituted 3-(benzothiazol-2-yl) derivative (13) was equipotent with the more synthetically challenging 3,6-disubstituted derivatives (34 a–e and 35 a–e) and exhibited a promising and unique selectivity profile when screened against a panel consisting of 403 protein kinases (Kinomescan™) selectivity score = 0.005, Kd = 0.55 ± 0.055μM and 0.410 ± 0.20μM for JAK1 JH2 pseudokinase and VPS34, respectively).