Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole

Stefania Aiello; Rana Bazzi; Hachemi Kadri; Andrew D. Westwell; Erica L. Stone; Stefania Aiello; Tracey D. Bradshaw; Charles S. Matthews; Geoffrey Wells; Malcolm F. G. Stevens; David R. Bell

Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole

Stefania Aiello, Rana Bazzi, Hachemi Kadri, Andrew D. Westwell, Erica L. Stone, Stefania Aiello, Tracey D. Bradshaw, Charles S. Matthews, Geoffrey Wells, Malcolm F. G. Stevens, David R. Bell

Risultato della ricerca: Article › peer review

253 Citazioni (Scopus)

Abstract

New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.

Lingua originale	English
pagine (da-a)	5135-5139
Numero di pagine	5
Rivista	Journal of Medicinal Chemistry
Volume	51
Stato di pubblicazione	Published - 2008

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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Aiello, S., Bazzi, R., Kadri, H., Westwell, A. D., Stone, E. L., Aiello, S., Bradshaw, T. D., Matthews, C. S., Wells, G., Stevens, M. F. G., & Bell, D. R. (2008). Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole. Journal of Medicinal Chemistry, 51, 5135-5139.

Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole. / Aiello, Stefania; Bazzi, Rana; Kadri, Hachemi; Westwell, Andrew D.; Stone, Erica L.; Aiello, Stefania; Bradshaw, Tracey D.; Matthews, Charles S.; Wells, Geoffrey; Stevens, Malcolm F. G.; Bell, David R.

In: Journal of Medicinal Chemistry, Vol. 51, 2008, pag. 5135-5139.

Risultato della ricerca: Article › peer review

Aiello, Stefania ; Bazzi, Rana ; Kadri, Hachemi ; Westwell, Andrew D. ; Stone, Erica L. ; Aiello, Stefania ; Bradshaw, Tracey D. ; Matthews, Charles S. ; Wells, Geoffrey ; Stevens, Malcolm F. G. ; Bell, David R. / Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole. In: Journal of Medicinal Chemistry. 2008 ; Vol. 51. pagg. 5135-5139.

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abstract = "New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.",

author = "Stefania Aiello and Rana Bazzi and Hachemi Kadri and Westwell, {Andrew D.} and Stone, {Erica L.} and Stefania Aiello and Bradshaw, {Tracey D.} and Matthews, {Charles S.} and Geoffrey Wells and Stevens, {Malcolm F. G.} and Bell, {David R.}",

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T1 - Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole

AU - Aiello, Stefania

AU - Bazzi, Rana

AU - Kadri, Hachemi

AU - Westwell, Andrew D.

AU - Stone, Erica L.

AU - Aiello, Stefania

AU - Bradshaw, Tracey D.

AU - Matthews, Charles S.

AU - Wells, Geoffrey

AU - Stevens, Malcolm F. G.

AU - Bell, David R.

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N2 - New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.

AB - New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.

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