Abstract

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.

Original languageEnglish
JournalFuture Medicinal Chemistry
Early online dateFeb 21 2019
DOIs
Publication statusPublished - Feb 21 2019

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Urinary Bladder Neoplasms
Antineoplastic Agents
G1 Phase
Ovarian Neoplasms
Solubility
Neoplasms
Cell Cycle
Apoptosis
Pyrrolo(2,3-d)pyrimidine

Cite this

@article{ebef19b1c7b24b4181ba9dc3fcded8b9,
title = "Synthesis and evaluation of novel 7H-pyrrolo-[2,3-d]pyrimidine derivatives as potential anticancer agents",
abstract = "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.",
author = "Yi-Min Liu and Chun-Han Chen and Teng-Kuang Yeh and Jing-Ping Liou",
year = "2019",
month = "2",
day = "21",
doi = "10.4155/fmc-2018-0564",
language = "English",
journal = "Future Medicinal Chemistry",
issn = "1756-8919",
publisher = "Future Science",

}

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

JO - Future Medicinal Chemistry

JF - Future Medicinal Chemistry

SN - 1756-8919

ER -