By R T Blickenstaff
Antitumor Steroids examines using steroids, besides nonsteroidal antiestrogens and a few benzo[a]carbazoles, within the remedy of melanoma. It explains the mechanism through which steroids and their receptors interact to impact their physiological features more often than not and their antitumor job particularly. It additionally describes the systematic screening of antitumor compounds remoted from common resources.
Organized into 9 chapters, this booklet 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 think about androgens, a few antiandrogens, derivatives according to C-19 steroids, progestins and corticoids, bile acids, and compounds with a side-chain carboxyl crew. The publication explains the biogenesis and metabolism of androgens; the pharmacology of medroxyprogesterone acetate; the antitumor homes of certainly happening corticosteroids; sterols and cucurbitacins; nutrition D and its metabolites; and cardenolides, bufadienolides, and withanolides. The ebook concludes with a bankruptcy on bile acids, sapogenins and its analogs, and miscellaneous steroids.
This e-book is a worthwhile source for natural and medicinal chemists biochemists, and pharmacologists attracted to using steroids in treating melanoma.
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Extra info for Antitumor Steroids
On the other hand, Gibson et al. synthesized 17a-[ 77 Br]bromoethynylestradiol (282), a compound that significantly accumulated in the uterus when administered to immature rats . More convincing imaging studies were recently reported by Mintun et al. , who tested 16a-[ 18 F]fluoroestradiol (283) by positron emission tomography. This radiopharmaceutical, synthesized by Katzenellenbogen, concentrated in primary and metastatic lesions of a small number of patients. There was an excellent correlation between uptake and ER concentration measured in the lesions after their excition.
Acylation of the amino group with 2-chloroethylnitrosocarbamoyl azide gave a 70% yield of the N-nitrosourea 95. Reaction of the amino alcohol 94 with methylnitrosocarbamoyl chloride gave a 60% yield of the N-nitrosourea 96. 17ß-Amino-l,3,5(10)-estratrien-3-ol (prepared by reduction of estrone oxime with sodium and 1-propanol) reacted with 28 2 B ESTROGENS, ANTIESTROGENS, AND OTHER ESTRANE COMPOUNDS 93, R = C7H7, R' = N3 94, R = H, R8 = NH2 CH 2 NHCNR NO 97, R = CH2CH2CI 98, R = CH3 CHART XIV» 95 96 R = CH2CH2CI R = Ch , 3 Nitrosourea of estradiol.
W. Hartmann, J. Engel, M. R. Schneider, and H. Schonenberger (1990). Cytotoxic ester derivatives of the mammary tumor inhibiting antiestrogen 2,3-bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane. Arch. Pharm. (Weinheim) 323, 121-124. 65. J. S. Pento, R. A. Magarian, and M. M. King (1982). A comparison of the efficacy for antitumor activity of the non-steroidal antiestrogens analog II and tamoxifen in 7,12dimethylbenz[(fl)]anthracene-induced rat mammary tumors. Cancer Lett. 15, 261-269. 66. R. W.
Antitumor Steroids by R T Blickenstaff