Synthesis of some coumarinyl chalcones and their antiproliferative activity against breast cancer cell lines

Kuldeep Patel; Chandrabose Karthikeyan; Viswas Raja Solomon; N. S Hari Narayana Moorthy; Hoyun Lee; Kapendra Sahu; Girdhar Singh Deora; Piyush Trivedi

doi:10.2174/157018011794839475

Synthesis of some coumarinyl chalcones and their antiproliferative activity against breast cancer cell lines

Kuldeep Patel, Chandrabose Karthikeyan, Viswas Raja Solomon, N. S Hari Narayana Moorthy, Hoyun Lee, Kapendra Sahu, Girdhar Singh Deora, Piyush Trivedi

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

44 Citations (Scopus)

Abstract

A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R₁; R₂ and R₃ positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

Original language	English
Pages (from-to)	308-311
Number of pages	4
Journal	Letters in Drug Design and Discovery
Volume	8
Issue number	4
DOIs	https://doi.org/10.2174/157018011794839475
Publication status	Published - May 2011
Externally published	Yes

Keywords

184B5
Antiproliferative activity
Breast cancer cell lines
Coumarinyl chalcones

UN SDGs

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

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10.2174/157018011794839475

Cite this

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title = "Synthesis of some coumarinyl chalcones and their antiproliferative activity against breast cancer cell lines",

abstract = "A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1; R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells. ",

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author = "Kuldeep Patel and Chandrabose Karthikeyan and Solomon, {Viswas Raja} and Moorthy, {N. S Hari Narayana} and Hoyun Lee and Kapendra Sahu and Deora, {Girdhar Singh} and Piyush Trivedi",

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doi = "10.2174/157018011794839475",

language = "English",

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pages = "308--311",

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T1 - Synthesis of some coumarinyl chalcones and their antiproliferative activity against breast cancer cell lines

AU - Patel, Kuldeep

AU - Karthikeyan, Chandrabose

AU - Solomon, Viswas Raja

AU - Moorthy, N. S Hari Narayana

AU - Lee, Hoyun

AU - Sahu, Kapendra

AU - Deora, Girdhar Singh

AU - Trivedi, Piyush

PY - 2011/5

Y1 - 2011/5

N2 - A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1; R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

AB - A series of coumarinyl chalcones derivatives were synthesized and evaluated for their antiproliferative activities on three different breast cancer cell lines (MDA-MB231, MDA-MB468, MCF7) and one non-cancer breast epithelial cell line (184B5). The coumarinyl derivatives exhibited anticancer activity against breast cancer cell lines at a micromolar range. A structure-activity relationship (SAR) analysis was performed by studying the effect of substituents on their antiproliferative activities. One of the compound 3i bearing methoxy substitutions at the R1; R2 and R3 positions of the phenyl ring showed comparable potency to the reference drug cisplatin as well as a two-fold higher selectivity for the breast cancer cell lines than 184B5 cells.

KW - 184B5

KW - Antiproliferative activity

KW - Breast cancer cell lines

KW - Coumarinyl chalcones

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DO - 10.2174/157018011794839475

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SP - 308

EP - 311

JO - Letters in Drug Design and Discovery

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Synthesis of some coumarinyl chalcones and their antiproliferative activity against breast cancer cell lines

Abstract

Keywords

UN SDGs

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