Antitumor activities of newly synthesized 5-carbamoyl-1 H-imidazol-4yl 1-adamantanecarboxylate and 5-carbamoyl-1H-imidazol-4yl piperonylate.
In synthetic studies on the chemical modification of the nucleoside antibiotic bredinin, two new derivatives, 5-carbamoyl-1H-imidazol-4-yl 1-adamantanecarboxylate and 5-carbamoyl-1H-imidazol-4-yl piperonylate, were found to possess a potent antitumor activity in several experimental tumor systems, even though bredinin itself shows only in vitro cytotoxicity and thus lacks therapeutic effectiveness. These two derivatives of bredinin exhibited antitumor activity against a wide variety of tumors, including leukemias L1210 and P388, Lewis lung carcinoma, B16 melanoma, Colon 26 and 38 adenocarcinomas. Ehrlich carcinoma, and Sarcoma 180. It is noteworthy that these agents showed good therapeutic effects not only against ascitic types of tumors but also against a number of slow-growing solid tumor lines, particularly the ascitic and solid forms of Ehrlich carcinoma. At their optimal doses, both compounds effected a complete cure of all or most of the mice treated. Although the mechanisms of action of these compounds remain unknown, they are able to suppress in vivo tumor growth, presumably by being slowly anabolized in vivo to an active form and inhibiting purine de novo synthesis as bredinin does.
Use of adamantanecarboxylic acid for the modification of drugs and biologically active compounds (review)
The discovery of 1964 of the antiviral activity (AA) of l-aminoadamantane and a number of its derivatives [149] led to intensive development of adamantane chemistry [131, 153]. Although a number of surveys have been devoted to the biological study of aminoadamantane derivatives [53, 202], the activity of other adamantane derivatives is barely mentioned in the general reviews and monographs [55, 153, 171, 179, 9
LAND DEGRADATION IN THE DEVELOPING WORLD: ISSUES AND POLICY OPTIONS FOR 2020
Land degradation takes a number of forms, including depletion of soil nutrients, salinization, agrochemical pollution, soil erosion, vegetative degradation as a result of overgrazing, and the cutting of forests for farmland. All of these types of degradation cause a decline in the productive capacity of the land, reducing potential yields. Farmers may need to use more inputs such as fertilizer or manure in order to maintain yields, or they may temporarily or permanently abandon some plots. Degradation may also induce farmers to convert land to lower-value uses. For example, farmers may plant cassava, which demands few nutrients, instead of maize, or convert cropland to grazing land.