Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2,1,b]-benzothiazole derivatives

Jitender K. Malik; Malleshappa N. Noolvi; Fakkirappa V. Manvi; B. K. Nanjwade; Harun M. Patel; S. N. Manjula; C. Mallikarjuna Rao; Ashutosh Barve

doi:10.2174/157018011796576015

Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2,1,b]-benzothiazole derivatives

Jitender K. Malik, Malleshappa N. Noolvi, Fakkirappa V. Manvi, B. K. Nanjwade, Harun M. Patel, S. N. Manjula, C. Mallikarjuna Rao, Ashutosh Barve

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Abstract

A novel series of substituted diaryl imidazo[2,1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted α-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, ¹H NMR, ¹³C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B₁₆F₁₀) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC₅₀ range of 0.56-27.50 μM in MCF-7 and 2.57-36.54 μM in B₁₆F₁₀ cells.

Original language	English
Pages (from-to)	717-724
Number of pages	8
Journal	Letters in Drug Design and Discovery
Volume	8
Issue number	8
DOIs	https://doi.org/10.2174/157018011796576015
Publication status	Published - 10-2011

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Molecular Medicine
Pharmaceutical Science
Drug Discovery

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10.2174/157018011796576015

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title = "Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2,1,b]-benzothiazole derivatives",

abstract = "A novel series of substituted diaryl imidazo[2,1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted α-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC50 range of 0.56-27.50 μM in MCF-7 and 2.57-36.54 μM in B16F10 cells.",

author = "Malik, {Jitender K.} and Noolvi, {Malleshappa N.} and Manvi, {Fakkirappa V.} and Nanjwade, {B. K.} and Patel, {Harun M.} and Manjula, {S. N.} and {Mallikarjuna Rao}, C. and Ashutosh Barve",

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AU - Malik, Jitender K.

AU - Noolvi, Malleshappa N.

AU - Manvi, Fakkirappa V.

AU - Nanjwade, B. K.

AU - Patel, Harun M.

AU - Manjula, S. N.

AU - Mallikarjuna Rao, C.

AU - Barve, Ashutosh

N1 - cited By 2

PY - 2011/10

Y1 - 2011/10

N2 - A novel series of substituted diaryl imidazo[2,1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted α-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC50 range of 0.56-27.50 μM in MCF-7 and 2.57-36.54 μM in B16F10 cells.

AB - A novel series of substituted diaryl imidazo[2,1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted α-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC50 range of 0.56-27.50 μM in MCF-7 and 2.57-36.54 μM in B16F10 cells.

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Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2,1,b]-benzothiazole derivatives

Abstract

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