Pyrazoline bearing benzimidazoles: Search for anticancer agent

Mohammad Shaharyar; M. M. Abdullah; M. A. Bakht; Jaseela Majeed

doi:10.1016/j.ejmech.2009.09.032

Pyrazoline bearing benzimidazoles: Search for anticancer agent

Mohammad Shaharyar, M. M. Abdullah, M. A. Bakht, Jaseela Majeed

Jamia Hamdard University

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

176 Scopus citations

Abstract

2-acetyl benzimidazole was allowed to react with substituted aromatic aldehydes to get desired intermediate chalcones (2a-g), the cyclocondensation of these intermediates with hydrazine hydrate and phenyl hydrazine in two separate reactions yielded pyrazoline derivatives (3a-g & 4a-g respectively). Among the synthesize compounds, six compounds were granted NSC code and screened at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10^-5 M) in full NCI 60 cell panel. Among the selected compounds, (4f) 2-[5-(3,4-dimethoxyphenyl)-1-phenyl-4,5-dihydro-1H-3-pyrazolyl]-1H-benzimidazole (NSC 748326) was found to be the most active candidate of the series and selected for further evaluation at five dose level screening.

Original language	English
Pages (from-to)	114-119
Number of pages	6
Journal	European Journal of Medicinal Chemistry
Volume	45
Issue number	1
DOIs	https://doi.org/10.1016/j.ejmech.2009.09.032
State	Published - Jan 2010
Externally published	Yes

Keywords

Anticancer activity
Antiproliferative activity
Benzimidazole
NCI
Pyrazoline

UN SDGs

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

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10.1016/j.ejmech.2009.09.032

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title = "Pyrazoline bearing benzimidazoles: Search for anticancer agent",

abstract = "2-acetyl benzimidazole was allowed to react with substituted aromatic aldehydes to get desired intermediate chalcones (2a-g), the cyclocondensation of these intermediates with hydrazine hydrate and phenyl hydrazine in two separate reactions yielded pyrazoline derivatives (3a-g \& 4a-g respectively). Among the synthesize compounds, six compounds were granted NSC code and screened at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10-5 M) in full NCI 60 cell panel. Among the selected compounds, (4f) 2-[5-(3,4-dimethoxyphenyl)-1-phenyl-4,5-dihydro-1H-3-pyrazolyl]-1H-benzimidazole (NSC 748326) was found to be the most active candidate of the series and selected for further evaluation at five dose level screening.",

keywords = "Anticancer activity, Antiproliferative activity, Benzimidazole, NCI, Pyrazoline",

author = "Mohammad Shaharyar and Abdullah, \{M. M.\} and Bakht, \{M. A.\} and Jaseela Majeed",

year = "2010",

month = jan,

doi = "10.1016/j.ejmech.2009.09.032",

language = "English",

volume = "45",

pages = "114--119",

journal = "European Journal of Medicinal Chemistry",

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TY - JOUR

T1 - Pyrazoline bearing benzimidazoles

T2 - Search for anticancer agent

AU - Shaharyar, Mohammad

AU - Abdullah, M. M.

AU - Bakht, M. A.

AU - Majeed, Jaseela

PY - 2010/1

Y1 - 2010/1

N2 - 2-acetyl benzimidazole was allowed to react with substituted aromatic aldehydes to get desired intermediate chalcones (2a-g), the cyclocondensation of these intermediates with hydrazine hydrate and phenyl hydrazine in two separate reactions yielded pyrazoline derivatives (3a-g & 4a-g respectively). Among the synthesize compounds, six compounds were granted NSC code and screened at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10-5 M) in full NCI 60 cell panel. Among the selected compounds, (4f) 2-[5-(3,4-dimethoxyphenyl)-1-phenyl-4,5-dihydro-1H-3-pyrazolyl]-1H-benzimidazole (NSC 748326) was found to be the most active candidate of the series and selected for further evaluation at five dose level screening.

AB - 2-acetyl benzimidazole was allowed to react with substituted aromatic aldehydes to get desired intermediate chalcones (2a-g), the cyclocondensation of these intermediates with hydrazine hydrate and phenyl hydrazine in two separate reactions yielded pyrazoline derivatives (3a-g & 4a-g respectively). Among the synthesize compounds, six compounds were granted NSC code and screened at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10-5 M) in full NCI 60 cell panel. Among the selected compounds, (4f) 2-[5-(3,4-dimethoxyphenyl)-1-phenyl-4,5-dihydro-1H-3-pyrazolyl]-1H-benzimidazole (NSC 748326) was found to be the most active candidate of the series and selected for further evaluation at five dose level screening.

KW - Anticancer activity

KW - Antiproliferative activity

KW - Benzimidazole

KW - NCI

KW - Pyrazoline

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U2 - 10.1016/j.ejmech.2009.09.032

DO - 10.1016/j.ejmech.2009.09.032

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AN - SCOPUS:72049105061

SN - 0223-5234

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EP - 119

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 1

ER -

Pyrazoline bearing benzimidazoles: Search for anticancer agent

Abstract

Keywords

UN SDGs

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