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Machine translation
1. (WO1981000410) CYTOTOXIC NUCLEOSIDE-CORTICOSTEROID PHOSPHODIESTERS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1981/000410    International Application No.:    PCT/US1980/000938
Publication Date: 19.02.1981 International Filing Date: 28.07.1980
IPC:
C07H 19/10 (2006.01), C07J 51/00 (2006.01)
Applicants:
Inventors:
Priority Data:
63753 06.08.1979 US
Title (EN) CYTOTOXIC NUCLEOSIDE-CORTICOSTEROID PHOSPHODIESTERS
(FR) PHOSPHODIESTER NUCLEOSIDE-CORTICOSTEROIDES CYTOTOXIQUES
Abstract: front page image
(EN)Nucleotides of nucleosides or bases having known cytotoxic activity are reacted with steroids, preferably corticosteroids, to form corresponding cytotoxic nucleoside-corticosteroid phosphodiester analogues of the formula: (FORMULA) wherein: steroid is the residue formed by removal of a hydrocyl hydrogen atom from a natural or synthetic adrenal corticosteroid containing the characteristic cyclopentanophenanthrene nucleus which is esterified to the phosphate moiety at the 21-position; sugar is a naturally occuring pentose or deoxypentose in the furanose form, preferably ribose, deoxyribose, lyxose, xylose or arabinose and especially ribose, deoxyribose or arabinose, which is esterified to the phosphate moiety at the 5"-position and covalently bonded to the heterocycle moiety at the 1"-position to form a nucleoside; and heterocycle is a purine, pyrimidine, hydrogenated pyrimidine, triazolopurine or similar nucleoside base. The conjugates exhibit an enhanced therapeutic index as compared to the parent nucleoside or base compounds, and are thus useful cytotoxic, antiviral and antineoplastic agents.
(FR)On fait reagir des nucleotides de nucleosides ou bases ayant une activite cytotoxique connue avec des steroides, de preference des corticosteroides, pour former des produits analogues aux phosphodiesters de nucleosides-corticosteroides cytotoxiques de formule: steroide-O-P-O-sucre-heterocycle (FORMULE) ou le steroide est le residu forme par extraction d"un atome d"hydrogene hydroxyle a partir d"un corticosteroide adrenal naturel ou synthetique contenant le noyau caracteristique cyclopentanophenanthrene qui est esterifie a la moitie de phosphate en position 21; le sucre est un pentose ou deoxypentose se produisant naturellement sous la forme de furanose, de preference ribose, desoxyribose, lyxose, xylose ou arabinose et specialement ribose, desoxyribose ou arabinose, qui est esterifie a la moitie de phosphate en position (5") et lie par covalence a la moitie de l"etherocycle en position (1") pour former un nucleoside; et l"heterocycle est une purine, pyrimidine, pyrimidine hydrogenee, triazolopurine ou base nucleoside similaire. Les conjugues ont un meilleur index therapeutique en comparaison des composes nucleosides ou bases de la meme famille, et sont donc utiles comme agents cytotoxiques, antiviraux et antineoplastes.
Designated States:
Publication Language: English (EN)
Filing Language: English (EN)