By R T Blickenstaff
Antitumor Steroids examines using steroids, in addition to nonsteroidal antiestrogens and a few benzo[a]carbazoles, within the therapy of melanoma. It explains the mechanism through which steroids and their receptors interact to impact their physiological services in most cases and their antitumor task specifically. It additionally describes the systematic screening of antitumor compounds remoted from typical assets.
Organized into 9 chapters, this ebook starts with an summary of the position of steroids in melanoma remedy. It then discusses the estrogens, antiestrogens, and compounds (all containing an fragrant A-ring). the subsequent chapters examine androgens, a few antiandrogens, derivatives in keeping with C-19 steroids, progestins and corticoids, bile acids, and compounds with a side-chain carboxyl team. The e-book explains the biogenesis and metabolism of androgens; the pharmacology of medroxyprogesterone acetate; the antitumor houses of obviously happening corticosteroids; sterols and cucurbitacins; diet D and its metabolites; and cardenolides, bufadienolides, and withanolides. The e-book concludes with a bankruptcy on bile acids, sapogenins and its analogs, and miscellaneous steroids.
This ebook is a priceless source for natural and medicinal chemists biochemists, and pharmacologists attracted to using steroids in treating melanoma.
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Additional info for Antitumor Steroids
This compound is inactive against the Dunning leukemia . It was condensed with ethyl formate to give a 76% yield of the hydroxymethylene derivative 293 . The corresponding diacetate reacted with diethylamine to give the tertiary amine 294, which was hydrogenated to amine 295 (Pt0 2 , glacial acetic acid). Elimination was accomplished by heating the amine in glacial acetic acid in the presence of sodium acetate to give a mixture of α-methylene lactone 296 0*° n° — \ X ^CHR ^ r H 292 293, R = O H 294, R = N(Cj>Η5>2 296, R = H CHART XXXVL Ring-D lactones.
REFERENCES 51 2,10-16 2-Methanesulfonoxyestrone The 2-mesylate (299) of 2-hydroxyestrone was reported to bind irreversibly to the ER . Interestingly, it produced a very strong inhibition of growth of the (ER-positive) MCF-7 cell line, whereas it was totally ineffective against a control (ER-negative) line. Further studies are required to establish its potential value. 2-11 SUMMARY Two of the most valuable antitumor compounds come from this group: tamoxifen (6, Chart I) and estracyt (or its hydrolysis product estramustine, 16, Chart IV), used against breast and prostate cancers, respectively.
12. T. Nogrady, K. M. Vagi, and V. W. Adamkiewicz (1962). N-Mustard derivatives of estrogens. Can. ]. Chem. 40, 2126-2129. 13. R. Catane, S. Bruno, and F. M. Muggia (1980). Prospects for compounds utilizing estrogens as carriers of cytotoxic molecules in cancer treatment. In "Cytotoxic Estrogens in Hormone Receptive Tumors' 7 (J. Raus, H. Matens, and G. ), pp. 263-270. Academic Press, New York. 14. A. A. Sandberg (1980). The fate and biochemical effects of estracyt in the human and baboon. In "Cytotoxic Estrogens in Hormone Receptive Tumors" (J.