Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines

Upendar Reddy Chamakura; E. Sailaja; Balakrishna Dulla; Arunasree M. Kalle; S. Bhavani; D. Rambabu; Ravikumar Kapavarapu; M. V.Basaveswara Rao; Manojit Pal

doi:10.1016/j.bmcl.2014.01.044

Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines

Upendar Reddy Chamakura, E. Sailaja, Balakrishna Dulla, Arunasree M. Kalle, S. Bhavani, D. Rambabu, Ravikumar Kapavarapu, M. V.Basaveswara Rao, Manojit Pal

Department of Chemistry

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

14 Scopus citations

Abstract

A series of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl) methyl]pyridine derivatives were designed as potential anticancer agents. These compounds were conveniently prepared by using Pd/C-Cu mediated Sonogashira type coupling as a key step. Many of these compounds were found to be promising when tested for their in vitro anti-proliferative properties against six cancer cell lines. All these compounds were found to be selective towards the growth inhibition of cancer cells with IC₅₀ values in the range of 0.9-1.7 μM (against MDA-MB 231 and MCF7 cells), comparable to the known anticancer drug doxorubicin.

Original language	English
Pages (from-to)	1366-1372
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2014.01.044
State	Published - 1 Mar 2014

Keywords

Alkyne
Anti-proliferation
Cancer
Coupling
Pd/C

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

UN SDGs

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

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10.1016/j.bmcl.2014.01.044

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Reddy Chamakura, U., Sailaja, E., Dulla, B., Kalle, A. M., Bhavani, S., Rambabu, D., Kapavarapu, R., Rao, M. V. B., & Pal, M. (2014). Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines. Bioorganic and Medicinal Chemistry Letters, 24(5), 1366-1372. https://doi.org/10.1016/j.bmcl.2014.01.044

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title = "Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines",

abstract = "A series of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl) methyl]pyridine derivatives were designed as potential anticancer agents. These compounds were conveniently prepared by using Pd/C-Cu mediated Sonogashira type coupling as a key step. Many of these compounds were found to be promising when tested for their in vitro anti-proliferative properties against six cancer cell lines. All these compounds were found to be selective towards the growth inhibition of cancer cells with IC50 values in the range of 0.9-1.7 μM (against MDA-MB 231 and MCF7 cells), comparable to the known anticancer drug doxorubicin.",

keywords = "Alkyne, Anti-proliferation, Cancer, Coupling, Pd/C",

author = "{Reddy Chamakura}, Upendar and E. Sailaja and Balakrishna Dulla and Kalle, {Arunasree M.} and S. Bhavani and D. Rambabu and Ravikumar Kapavarapu and Rao, {M. V.Basaveswara} and Manojit Pal",

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doi = "10.1016/j.bmcl.2014.01.044",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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Reddy Chamakura, U, Sailaja, E, Dulla, B, Kalle, AM, Bhavani, S, Rambabu, D, Kapavarapu, R, Rao, MVB & Pal, M 2014, 'Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines', Bioorganic and Medicinal Chemistry Letters, vol. 24, no. 5, pp. 1366-1372. https://doi.org/10.1016/j.bmcl.2014.01.044

Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines. / Reddy Chamakura, Upendar; Sailaja, E.; Dulla, Balakrishna et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 24, No. 5, 01.03.2014, p. 1366-1372.

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

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AU - Reddy Chamakura, Upendar

AU - Sailaja, E.

AU - Dulla, Balakrishna

AU - Kalle, Arunasree M.

AU - Bhavani, S.

AU - Rambabu, D.

AU - Kapavarapu, Ravikumar

AU - Rao, M. V.Basaveswara

AU - Pal, Manojit

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Synthesis and in vitro anti-proliferative effects of 3-(hetero)aryl substituted 3-[(prop-2-ynyloxy)(thiophen-2-yl)methyl]pyridine derivatives on various cancer cell lines

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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