Synthesis of 1H-Pyrazole-1-carboxamide derivatives and their antiproliferative activity against melanoma cell line

Mohammed I. El-Gamal; Tae Bo Sim; Jun Hee Hong; Jung Hyuck Cho; Kyung Ho Yoo; Chang Hyun Oh

doi:10.1002/ardp.201000057

Synthesis of 1H-Pyrazole-1-carboxamide derivatives and their antiproliferative activity against melanoma cell line

Mohammed I. El-Gamal, Tae Bo Sim, Jun Hee Hong, Jung Hyuck Cho, Kyung Ho Yoo, Chang Hyun Oh

KU-KIST Graduate School of Converging Science and Technology

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

16 Citations (Scopus)

Abstract

Synthesis of a new series of 1H-pyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with sorafenib. Among all of these derivatives, compound IIe which has N-methylpiperazinyl and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line.

Original language	English
Pages (from-to)	197-204
Number of pages	8
Journal	Archiv der Pharmazie
Volume	344
Issue number	3
DOIs	https://doi.org/10.1002/ardp.201000057
Publication status	Published - 2011 Mar

Keywords

1H-Pyrazole-1-carboxamide
3,4-Diarylpyrazole
A375
Antiproliferative activity
Melanoma

ASJC Scopus subject areas

Pharmaceutical Science
Drug Discovery

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10.1002/ardp.201000057

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abstract = "Synthesis of a new series of 1H-pyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with sorafenib. Among all of these derivatives, compound IIe which has N-methylpiperazinyl and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line.",

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AU - El-Gamal, Mohammed I.

AU - Sim, Tae Bo

AU - Hong, Jun Hee

AU - Cho, Jung Hyuck

AU - Yoo, Kyung Ho

AU - Oh, Chang Hyun

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N2 - Synthesis of a new series of 1H-pyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with sorafenib. Among all of these derivatives, compound IIe which has N-methylpiperazinyl and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line.

AB - Synthesis of a new series of 1H-pyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with sorafenib. Among all of these derivatives, compound IIe which has N-methylpiperazinyl and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line.

KW - 1H-Pyrazole-1-carboxamide

KW - 3,4-Diarylpyrazole

KW - A375

KW - Antiproliferative activity

KW - Melanoma

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Synthesis of 1H-Pyrazole-1-carboxamide derivatives and their antiproliferative activity against melanoma cell line

Abstract

Keywords

ASJC Scopus subject areas

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