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

^*Corresponding author for this work

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 .

Keywords

A375 human melanoma cell line
Aminoquinazolines
Antiproliferative activity
Selectivity
Synthesis

ASJC Scopus subject areas

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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2010.08.010

Cite this

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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.",

keywords = "A375 human melanoma cell line, Aminoquinazolines, Antiproliferative activity, Selectivity, Synthesis",

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 .",

year = "2010",

month = oct,

day = "1",

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

language = "English",

volume = "20",

pages = "5722--5725",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd",

number = "19",

}

TY - JOUR

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

N1 - 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 .

PY - 2010/10/1

Y1 - 2010/10/1

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.

AB - 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.

KW - A375 human melanoma cell line

KW - Aminoquinazolines

KW - Antiproliferative activity

KW - Selectivity

KW - Synthesis

UR - https://www.scopus.com/pages/publications/77957592790

U2 - 10.1016/j.bmcl.2010.08.010

DO - 10.1016/j.bmcl.2010.08.010

M3 - Article

C2 - 20797858

AN - SCOPUS:77957592790

SN - 0960-894X

VL - 20

SP - 5722

EP - 5725

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

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