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)
Stefania AielloWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,Geoffrey WellsWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,Erica L. StoneWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,Hachemi KadriWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,Rana BazziWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,David BellWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,Malcolm F. G. StevensWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,Charles S. MatthewsWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,Tracey D. BradshawWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,Andrew D. WestwellWelsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff, CF10 3NB, U.K., Dipartimento Farmacochimico Tossicologico e Biologico, Facoltà di Farmacia, Università degli Studi di Palermo, 90123 Palermo, Italy, Pharminox Ltd., BioCity, Pennyfoot Street, Nottingham NG1 1GF, U.K., Centre for Biomolecular Sciences, School of Pharmacy, University of Nottingham, University Park, Nottingham NG7 2RD, U.K., and School of Biology, University of Nottingham, University Park,
2008en
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Annotatsiya
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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