Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line

Junsang Lee; Bong Soo Nam; Hwan Kim; Chang Hyun Oh; So Ha Lee; Seung Joo Cho; Tae Bo Sim; Jung Mi Hah; Dong Jin Kim; Jinsung Tae; Kyung Ho Yoo

doi:10.1016/j.bmcl.2010.08.010

Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line

Junsang Lee, Bong Soo Nam, Hwan Kim, Chang Hyun Oh, So Ha Lee, Seung Joo Cho, Tae Bo Sim, Jung Mi Hah, Dong Jin Kim, Jinsung Tae, Kyung Ho Yoo

Department of Chemistry

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

14 Citations (Scopus)

Abstract

The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC₅₀ = 0.006 μM) and good selectivity over HS27 fibroblast cell line.

Original language	English
Pages (from-to)	5722-5725
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2010.08.010
Publication status	Published - 2010 Oct 1

Bibliographical note

Funding Information:
This research was supported by a grant ( K00060-282 ) from the Fundamental R&D Program for Core Technology of Materials funded by the Ministry of Knowledge Economy, Republic of Korea .

All Science Journal Classification (ASJC) codes

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

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10.1016/j.bmcl.2010.08.010

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title = "Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line",

abstract = "The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC50 = 0.006 μM) and good selectivity over HS27 fibroblast cell line.",

author = "Junsang Lee and Nam, {Bong Soo} and Hwan Kim and Oh, {Chang Hyun} and Lee, {So Ha} and Cho, {Seung Joo} and Sim, {Tae Bo} and Hah, {Jung Mi} and Kim, {Dong Jin} and Jinsung Tae and Yoo, {Kyung Ho}",

note = "Funding Information: This research was supported by a grant ( K00060-282 ) from the Fundamental R&D Program for Core Technology of Materials funded by the Ministry of Knowledge Economy, Republic of Korea .",

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doi = "10.1016/j.bmcl.2010.08.010",

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T1 - Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line

AU - Lee, Junsang

AU - Nam, Bong Soo

AU - Kim, Hwan

AU - Oh, Chang Hyun

AU - Lee, So Ha

AU - Cho, Seung Joo

AU - Sim, Tae Bo

AU - Hah, Jung Mi

AU - Kim, Dong Jin

AU - Tae, Jinsung

AU - Yoo, Kyung Ho

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N2 - The synthesis of a novel series of aminoquinazoline derivatives 1a-r and their antiproliferative activities against A375 human melanoma cell line were described. Among them, six compounds showed superior antiproliferative activities to Sorafenib as a reference compound. In particular, the representative compound 1q bearing chromen-4-one moiety exhibited excellent antiproliferative activity (IC50 = 0.006 μM) and good selectivity over HS27 fibroblast cell line.

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Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line

Abstract

Bibliographical note

All Science Journal Classification (ASJC) codes

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