Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines

Junghun Lee; Hwan Kim; Hana Yu; Jae Yoon Chung; Chang Hyun Oh; Kyung Ho Yoo; Taebo Sim; Jung Mi Hah

doi:10.1016/j.bmcl.2010.01.064

Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines

Junghun Lee, Hwan Kim, Hana Yu, Jae Yoon Chung, Chang Hyun Oh, Kyung Ho Yoo, Taebo Sim, Jung Mi Hah

KU-KIST Graduate School of Converging Science and Technology

Research output: Contribution to journal › Article › peer-review

26 Citations (Scopus)

Abstract

The synthesis of a novel series of pyrimidin-4-yl-1H-imidazol-2-yl derivatives 7, 8, 9 and their antiproliferative activities against A375P human melanoma cell line and WM3629 cell line were described. Most compounds showed superior antiproliferative activities compared to Sorafenib, the well-known RAF inhibitor. Among them, 7a exhibited potent activities on both cell lines (IC₅₀ = 0.62 and 4.49 μM, respectively) and turned out to be a selective and potent CRAF inhibitor.

Original language	English
Pages (from-to)	1573-1577
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2010.01.064
Publication status	Published - 2010 Mar 1

Keywords

Antiproliferative activity
BRAF
CRAF
Melanoma cell line
Pyrimidin-4-yl-1H-imidazol-2-yl derivatives
Selectivity

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines. / Lee, Junghun; Kim, Hwan; Yu, Hana; Chung, Jae Yoon; Oh, Chang Hyun; Yoo, Kyung Ho; Sim, Taebo; Hah, Jung Mi.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 5, 01.03.2010, p. 1573-1577.

Research output: Contribution to journal › Article › peer-review

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abstract = "The synthesis of a novel series of pyrimidin-4-yl-1H-imidazol-2-yl derivatives 7, 8, 9 and their antiproliferative activities against A375P human melanoma cell line and WM3629 cell line were described. Most compounds showed superior antiproliferative activities compared to Sorafenib, the well-known RAF inhibitor. Among them, 7a exhibited potent activities on both cell lines (IC50 = 0.62 and 4.49 μM, respectively) and turned out to be a selective and potent CRAF inhibitor.",

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