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: Articlepeer 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 originaleEnglish
pagine (da-a)5135-5139
Numero di pagine5
RivistaJournal of Medicinal Chemistry
Volume51
Stato di pubblicazionePublished - 2008

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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