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 wherein steroids and their receptors interact to impact their physiological capabilities commonly and their antitumor task particularly. It additionally describes the systematic screening of antitumor compounds remoted from traditional assets.
Organized into 9 chapters, this ebook starts off with an summary of the function of steroids in melanoma remedy. It then discusses the estrogens, antiestrogens, and compounds (all containing an fragrant A-ring). the following chapters reflect on androgens, a few antiandrogens, derivatives according to C-19 steroids, progestins and corticoids, bile acids, and compounds with a side-chain carboxyl team. The publication explains the biogenesis and metabolism of androgens; the pharmacology of medroxyprogesterone acetate; the antitumor homes of certainly taking place corticosteroids; sterols and cucurbitacins; nutrition D and its metabolites; and cardenolides, bufadienolides, and withanolides. The booklet concludes with a bankruptcy on bile acids, sapogenins and its analogs, and miscellaneous steroids.
This booklet is a priceless source for natural and medicinal chemists biochemists, and pharmacologists drawn to using steroids in treating melanoma.
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17, respectively . Berger et al. prepared N-(2-chloroethylnitrosocarbamoyl)alanine (104, Chart XVI) by the action of 2-chloroethylnitrosocarbamoyl azide on alanine . The intermediate 104 was converted to the dipeptide 105 by way of its N-hydroxysuccinimide ester. Estradiol reacted with intermediate 104 in the presence of Ν,Ν-carbonyldiimidazole to give the 3-ester 106, and with an excess of intermediate 104 to give the 3,17-diester 107. KCN,NH3 NH4CI H N R ^U-^"«CN 100, R = H O 101, R = CNHCH2CH2CI O NO Γ" HNC-NCH2CH2CI CN 103 CHART XV.
Oncol. 24, 413-415. M. E. Stearns, D. P. Jenkins, and K. D. Tew (1985). Dansylated estramustine, a fluorescent probe for studies of estramustine uptake and identification of intracellular targets. Proc. Natl. Acad. Sei. A. 82, 8483-8487. K. D. Tew and M. E. Stearns (1986). Interaction of estramustine with high molecular weight microtubule associated proteins (HMW MAPs) in human prostatic DU145 carcinoma cells. Proc. Amer. Assoc. Cancer Res. 27, 307. K. D. Tew and M. E. Stearns (1987). Hormone-independent, non-alkylating mechanism of cytotoxicity for estramustine.
For example, methylmagnesium bromide reacted with the 17-ethylene ketal (134, Chart XIX) of 3-methoxy-l,3,5(10)estratriene-ll,17-dione to give the corresponding l l a - h y d r o x y - l l ß methyl derivative [128,129]. This derivative was dehydrated in refluxing benzene to give the A9(11)-derivative 135, which was hydrogenated in the presence of palladium on charcoal to give the 9a-hydrogen-ll/3-methyl product 136, along with a minor amount of the 9/3-hydrogen-lla-methyl isomer. Reduction of the intermediate with sodium borohydride gave the 17/3-hydroxy derivative 137.
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