Ontology highlight
ABSTRACT:
SUBMITTER: Ravindra M
PROVIDER: S-EPMC6097718 | biostudies-literature | 2018 May
REPOSITORIES: biostudies-literature
Ravindra Manasa M Wilson Mike R MR Tong Nian N O'Connor Carrie C Karim Mohammad M Polin Lisa L Wallace-Povirk Adrianne A White Kathryn K Kushner Juiwanna J Hou Zhanjun Z Matherly Larry H LH Gangjee Aleem A
Journal of medicinal chemistry 20180427 9
Novel fluorinated 2-amino-4-oxo-6-substituted pyrrolo[2,3- d]pyrimidine analogues 7-12 were synthesized and tested for selective cellular uptake by folate receptors (FRs) α and β or the proton-coupled folate transporter (PCFT) and for antitumor efficacy. Compounds 8, 9, 11, and 12 showed increased in vitro antiproliferative activities (∼11-fold) over the nonfluorinated analogues 2, 3, 5, and 6 toward engineered Chinese hamster ovary and HeLa cells expressing FRs or PCFT. Compounds 8, 9, 11, and ...[more]