2. Academic Validation
  3. Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648)

Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648)

  • J Med Chem. 2008 Aug 28;51(16):5135-9. doi: 10.1021/jm800418z.
Stefania Aiello 1,  Geoffrey Wells,  Erica L Stone,  Hachemi Kadri,  Rana Bazzi,  David R Bell,  Malcolm F G Stevens,  Charles S Matthews,  Tracey D Bradshaw,  Andrew D Westwell
Affiliations

Affiliation

  • 1 Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, UK.
PMID: 18666770 DOI: 10.1021/jm800418z
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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-118474
    99.78%, Antitumor Agent