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A New Type of Cytotoxic Immunosuppressive Agent: 3-Acetyl-5-(4-fluorobenzylidene)4-hydroxy-2-oxo-2:5-dihydrothiophen

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Abstract

DURING the past 3 years we have been investigating the biological properties of a series of thiophens of tho following general formula (I): in which R is an alkyl or alkoxy group and the substituent X is an electron-withdrawing group such as halogen or nitro. These investigations resulted from the observation that the compound I.C.I. 45,514 (I, R = ethoxy, X = H) prevented the development of secondary inflamed lesions in rats injected into the foot-pad with a fine suspension of dead tubercle bacilli in liquid paraffin. The use of this syndrome for evaluating chemotherapeutic agents has already been described1,2.

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References

  1. Newbould, B. B., Brit. J. Pharmacol., 21, 127 (1963).

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  2. Newbould, B. B., Brit. J. Pharmacol., 24, 632 (1965).

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  3. O'Mant, D. M., and Stacey, G. J., U.K. patent application Nos. 8965/63 and 27696/63 (Belg. Pat. No. 661, 255).

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Authors and Affiliations

  1. Imperial Chemical Industries, Ltd., Pharmaceuticals Division, Alderley Park, Macclesfield, Cheshire

    T. J. FRANKLIN, B. B. NEWBOULD, D. M. O'MANT, A. I. SCOTT, G. J. STACEY & G. E. DAVIES

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  1. T. J. FRANKLIN
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  2. B. B. NEWBOULD
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  3. D. M. O'MANT
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  4. A. I. SCOTT
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  5. G. J. STACEY
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  6. G. E. DAVIES
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FRANKLIN, T., NEWBOULD, B., O'MANT, D. et al. A New Type of Cytotoxic Immunosuppressive Agent: 3-Acetyl-5-(4-fluorobenzylidene)4-hydroxy-2-oxo-2:5-dihydrothiophen. Nature 210, 638–639 (1966). https://doi.org/10.1038/210638a0

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  • DOI: https://doi.org/10.1038/210638a0

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