Synthesis of 1,2,3-triazole tethered bifunctional hybrids by click chemistry and their cytotoxic studies

Jagjeet Singh; Sahil Sharma; A. K. Saxena; Kunal Nepali; Preet Mohinder Singh Bedi

doi:10.1007/s00044-012-0312-7

Synthesis of 1,2,3-triazole tethered bifunctional hybrids by click chemistry and their cytotoxic studies

Jagjeet Singh, Sahil Sharma, A. K. Saxena, Kunal Nepali, Preet Mohinder Singh Bedi

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

29 Citations (Scopus)

Abstract

In view of the drug resistance with most of the currently used anticancer drugs, molecular hybrids of pyrazolyl chalcones and p-nitro benzyl functionalities tethered by triazole ring have been synthesised and evaluated for cytotoxic studies against three human cancer cell lines (THP, COLO-205, A-549). The results of the preliminary investigation exhibited marked dependence of the cytotoxic activity on the electronic factors. Placement of naphthyl (JGPT-11) and trimethoxy phenyl ring (JGPT-6) as ring A proved to be extremely beneficial in enhancing the cytotoxic potential. Thus we herein report the synthesis and cytotoxic studies of a new class of molecular hybrids. Detailed investigation on the biological mechanistic insights of JGPT-11 and 6 is under progress.

Original language	English
Pages (from-to)	3160-3169
Number of pages	10
Journal	Medicinal Chemistry Research
Volume	22
Issue number	7
DOIs	https://doi.org/10.1007/s00044-012-0312-7
Publication status	Published - Jul 1 2013
Externally published	Yes

Keywords

Cancer
Cell lines
Cytotoxicity
Molecular hybrids
Resistance

ASJC Scopus subject areas

Pharmacology, Toxicology and Pharmaceutics(all)
Organic Chemistry

UN SDGs

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

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10.1007/s00044-012-0312-7

Cite this

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title = "Synthesis of 1,2,3-triazole tethered bifunctional hybrids by click chemistry and their cytotoxic studies",

abstract = "In view of the drug resistance with most of the currently used anticancer drugs, molecular hybrids of pyrazolyl chalcones and p-nitro benzyl functionalities tethered by triazole ring have been synthesised and evaluated for cytotoxic studies against three human cancer cell lines (THP, COLO-205, A-549). The results of the preliminary investigation exhibited marked dependence of the cytotoxic activity on the electronic factors. Placement of naphthyl (JGPT-11) and trimethoxy phenyl ring (JGPT-6) as ring A proved to be extremely beneficial in enhancing the cytotoxic potential. Thus we herein report the synthesis and cytotoxic studies of a new class of molecular hybrids. Detailed investigation on the biological mechanistic insights of JGPT-11 and 6 is under progress.",

keywords = "Cancer, Cell lines, Cytotoxicity, Molecular hybrids, Resistance",

author = "Jagjeet Singh and Sahil Sharma and Saxena, {A. K.} and Kunal Nepali and Bedi, {Preet Mohinder Singh}",

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T1 - Synthesis of 1,2,3-triazole tethered bifunctional hybrids by click chemistry and their cytotoxic studies

AU - Singh, Jagjeet

AU - Sharma, Sahil

AU - Saxena, A. K.

AU - Nepali, Kunal

AU - Bedi, Preet Mohinder Singh

PY - 2013/7/1

Y1 - 2013/7/1

N2 - In view of the drug resistance with most of the currently used anticancer drugs, molecular hybrids of pyrazolyl chalcones and p-nitro benzyl functionalities tethered by triazole ring have been synthesised and evaluated for cytotoxic studies against three human cancer cell lines (THP, COLO-205, A-549). The results of the preliminary investigation exhibited marked dependence of the cytotoxic activity on the electronic factors. Placement of naphthyl (JGPT-11) and trimethoxy phenyl ring (JGPT-6) as ring A proved to be extremely beneficial in enhancing the cytotoxic potential. Thus we herein report the synthesis and cytotoxic studies of a new class of molecular hybrids. Detailed investigation on the biological mechanistic insights of JGPT-11 and 6 is under progress.

AB - In view of the drug resistance with most of the currently used anticancer drugs, molecular hybrids of pyrazolyl chalcones and p-nitro benzyl functionalities tethered by triazole ring have been synthesised and evaluated for cytotoxic studies against three human cancer cell lines (THP, COLO-205, A-549). The results of the preliminary investigation exhibited marked dependence of the cytotoxic activity on the electronic factors. Placement of naphthyl (JGPT-11) and trimethoxy phenyl ring (JGPT-6) as ring A proved to be extremely beneficial in enhancing the cytotoxic potential. Thus we herein report the synthesis and cytotoxic studies of a new class of molecular hybrids. Detailed investigation on the biological mechanistic insights of JGPT-11 and 6 is under progress.

KW - Cancer

KW - Cell lines

KW - Cytotoxicity

KW - Molecular hybrids

KW - Resistance

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Synthesis of 1,2,3-triazole tethered bifunctional hybrids by click chemistry and their cytotoxic studies

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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