Resumen
Por primera vez se han analizado las relaciones estructura-función de diez derivados del 9α-cortisol substituido usando técnicas de regresión de parámetros múltiples. Se concluye que los factores electrónicos y estéricos son de mayor importancia al determinar el efecto del substituyente, y que la unión hidrofóbica también es de importante consideración. Se discute el significado de estos resultados.
References
C. M. Weeks, W. L. Duax andM. E. Wolff, J. Am. Chem. Soc.95, 2865 (1973).
P. A. Kollman, D. Giannini, W. L. Duax, S. Rothenberg andM. E. Wolff, J. Am. chem. Soc.95, 2869 (1973).
cf.C. Hansch inDrug Design (Ed. E. J. Ariens: Academic Press, New York, N.Y. 1971), p. 271.
J. Fried, Ann. N.Y. Acad. Sci.61, 573 (1955).
J. Fried andA. Borman, Vitam. Horm.16, 303 (1958).
F. Hoffman, R. E. Beyler andM. Tishler, J. Am. chem. Soc.80, 5322 (1958).
L. H. Sarrett, A. A. Patchett andS. L. Steelman inProgress in Drug Research (Ed. E. Jucker; Birkhäuser, Basel 1963) vol. 5, p. 55.
T. C. Bruice, N. Kharasch andW. J. Winzler, Arch. Biochem. Biophys.62, 305 (1956).
S. M. Free andJ. W. Wilson, J. med. Chem.7, 398 (1964).
J. Kopecky andK. Bocek, Experientia23, 125 (1957).
W. P. Purcell, J. G. Beasley, R. P. Quintana andJ. A. Singer, J. med. Chem.9, 297 (1966).
C. D. Ritchie andW. F. Sager, Progr. Phys. org. Chem.2, 323 (1966).
C. Hansch andS. M. Anderson, J. org. Chem.32, 2583 (1967).
A. Leo, C. Hansch andD. Elkins, Chem. Rev.71, 525 (1971).
N. Bauer, K. Fajans andS. Z. Lewin inPhysical Methods of Organic Chemistry, 3rd edn (Ed. A. Weissberger, Interscience, New York, N.Y., 1960), vol. 1, part II, chapter 18.
E. Kutter andC. Hansch, J. med. Chem.12, 647 (1969).
N. R. Draper andH. Smith,Applied Regression Analysis (Wiley, New York, N.Y. 1966).
C. Hansch andJ. M. Clayton, J. pharm. Sci.62, 1 (1973).
I. E. Bush, Pharmac. Rev.14, 317 (1962).
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This investigation was supported in part by Public Health Service Research Grants No. AM-14824 (to M.E.W.) and No. GM 07492 (to C.H.) from the National Institutes of Arthritis and Metabolic Diseases, and General Medical Sciences, U.S. Public Health Service.
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Wolff, M.E., Hansch, C. Correlation of physicochemical parameters and biological activity in steroids 9α-substituted cortisol derivatives. Experientia 29, 1111–1113 (1973). https://doi.org/10.1007/BF01946750
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DOI: https://doi.org/10.1007/BF01946750