TY - JOUR
T1 - Synthesis and evaluation of novel 7H-pyrrolo-[2,3-d]pyrimidine derivatives as potential anticancer agents
AU - Liu, Yi-Min
AU - Chen, Chun-Han
AU - Yeh, Teng-Kuang
AU - Liou, Jing-Ping
PY - 2019/2/21
Y1 - 2019/2/21
N2 - AIM: Bladder cancer is a highly recurrent urologic malignancy with limited treatment approaches. Previously, we reported compound 11 is a FGFR3 inhibitor with significant antibladder cancer activity.MATERIALS & METHODS: In this study, a series of 7H-pyrrolo-[2,3-d]pyrimidine derivatives were synthesized through ring formation and modification of compound 11 for anticancer activity evaluation.RESULTS: Compound 13i is the most effective agent against human RT-112 bladder cancer cells. Notably, 13i strongly inhibits CK1δ without affecting FGFR3 activity. We generated 13i HCl to increase solubility and showed profound cell cycle accumulation at the sub-G1 phase and apoptosis in CK1δ-overexpressed bladder and ovarian cancer cells.CONCLUSION: These results indicate that compound 13i could be a lead compound for further development of novel anticancer agents.
AB - AIM: Bladder cancer is a highly recurrent urologic malignancy with limited treatment approaches. Previously, we reported compound 11 is a FGFR3 inhibitor with significant antibladder cancer activity.MATERIALS & METHODS: In this study, a series of 7H-pyrrolo-[2,3-d]pyrimidine derivatives were synthesized through ring formation and modification of compound 11 for anticancer activity evaluation.RESULTS: Compound 13i is the most effective agent against human RT-112 bladder cancer cells. Notably, 13i strongly inhibits CK1δ without affecting FGFR3 activity. We generated 13i HCl to increase solubility and showed profound cell cycle accumulation at the sub-G1 phase and apoptosis in CK1δ-overexpressed bladder and ovarian cancer cells.CONCLUSION: These results indicate that compound 13i could be a lead compound for further development of novel anticancer agents.
UR - http://www.mendeley.com/research/synthesis-evaluation-novel-7-h-pyrrolo23-d-pyrimidine-derivatives-potential-anticancer-agents
U2 - 10.4155/fmc-2018-0564
DO - 10.4155/fmc-2018-0564
M3 - Article
C2 - 30789758
SN - 1756-8919
JO - Future Medicinal Chemistry
JF - Future Medicinal Chemistry
ER -