Design, synthesis, and preliminary cytotoxicity evaluation of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold

Won Kyoung Choi; Mohammed I. El-Gamal; Hong Seok Choi; Jun Hee Hong; Daejin Baek; Kihang Choi; Chang Hyun Oh

doi:10.5012/bkcs.2012.33.9.2991

Design, synthesis, and preliminary cytotoxicity evaluation of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold

Won Kyoung Choi, Mohammed I. El-Gamal, Hong Seok Choi, Jun Hee Hong, Daejin Baek, Kihang Choi, Chang Hyun Oh

Department of Chemistry

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

14 Citations (Scopus)

Abstract

A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.

Original language	English
Pages (from-to)	2991-2998
Number of pages	8
Journal	Bulletin of the Korean Chemical Society
Volume	33
Issue number	9
DOIs	https://doi.org/10.5012/bkcs.2012.33.9.2991
Publication status	Published - 2012 Sept 20

Keywords

1,3,4-triarylpyrazole
A375P
Anticancer
Diarylamide
Diarylurea

ASJC Scopus subject areas

Chemistry(all)

UN SDGs

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

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10.5012/bkcs.2012.33.9.2991

Cite this

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title = "Design, synthesis, and preliminary cytotoxicity evaluation of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold",

abstract = "A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.",

keywords = "1,3,4-triarylpyrazole, A375P, Anticancer, Diarylamide, Diarylurea",

author = "Choi, {Won Kyoung} and El-Gamal, {Mohammed I.} and Choi, {Hong Seok} and Hong, {Jun Hee} and Daejin Baek and Kihang Choi and Oh, {Chang Hyun}",

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doi = "10.5012/bkcs.2012.33.9.2991",

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AU - Choi, Won Kyoung

AU - El-Gamal, Mohammed I.

AU - Choi, Hong Seok

AU - Hong, Jun Hee

AU - Baek, Daejin

AU - Choi, Kihang

AU - Oh, Chang Hyun

PY - 2012/9/20

Y1 - 2012/9/20

N2 - A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.

AB - A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.

KW - 1,3,4-triarylpyrazole

KW - A375P

KW - Anticancer

KW - Diarylamide

KW - Diarylurea

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VL - 33

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EP - 2998

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IS - 9

ER -

Design, synthesis, and preliminary cytotoxicity evaluation of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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