Anthracyclinone glycoside antibiotics including the known antibiotics daunomycin and adriamycin, as well as other, novel glycoside antibiotics of the formula (VIII): ##STR1## wherein WHEN R.sub.1 is hydrogen, R.sub.2 and R.sub.3 are each independently hydrogen, methyl, methoxy, chloro, or bromo; and when R.sub.2 and R.sub.3 are hydrogen, R.sub.1 is methyl, chloro, or bromo and R.sub.4 and R.sub.5 are each independently hydrogen or hydroxy are prepared by an acid catalyzed addition reaction between (a) an anthracyclinone compound of the formula ##STR2## or a dioxolanyl protected derivative thereof (VI) having the formula: ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, and R.sub.6, R.sub.7 and R.sub.8 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl; or R.sub.7 and R.sub.8, together with the carbon atom to which they are bound may form a saturated or unsaturated ring of 3-8 carbon atoms and (b) a novel reactive, protected 1,2-unsaturated pyranoid sugar, preferably, 1,2,3,6-tetradeoxy-3-trifluoroacetamido-4-trifluoroacetoxy-L-lyxo-hex-1-en opyranose which forms protected derivatives of said glycoside antibiotics and then removing the protecting groups from said glycoside antibiotics. These antibiotics are useful in the treatment of various human cancers and leukemia such as sarcomas, breast cancer, bronchogenic carcinoma, malignant lymphomas, neuroblastomas, acute leukemia and bladder cancer.

Societa' Farmaceutici Italia S.p.A.

L-lyxohex-1-enopyranose derivative

Esters of C.sub.4 -C.sub.10 saturated fatty acids with N-trifluoroacetyladriamycin are novel compounds. These compounds have the following structure: ##STR1## in which A is alkanoate having from 4 to 10 carbon atoms. Therapeutic compositions containing these compounds or the acetate or propionate of N-trifluoroacetyladriamycin are more effective than adriamycin in antitumor activity against murine P 388 and L 1210 leukemias and Ridgway osteogenic sarcoma in mice and at the same time significantly less toxic than adriamycin.

adriamycin/сарком

L-lyxohex-1-enopyranose derivative

N-trifluoroacetyladriamycin-14-alkanoates and therapeutic compositions containing same

Най-пълната база данни за лечебни билки, подкрепена от науката