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3'-Deamino-3'-(3-cyano-4-morpholinyl)doxorubicin is a new analogue that is 100 to 1000 times more potent than doxorubicin against tumors in cell culture or in mice, that is active by intraperitoneal, intravenous, or oral dosing, and that does not produce chronic myocardial lesions in mice. This analogue was encountered in studies on the reductive alkylation… (More)
Previously we reported that reductive alkylation of doxorubicin with 2,2'-oxybis[acetaldehyde] and NaBH3CN to form the 4''-morpholinyl derivative also gave the intensely potent 3''-cyano-4''-morpholinyl as a byproduct, by addition of CN- to an iminium intermediate in place of hydride. We now find that sugar 4'-OH is a third nucleophile that can add to the… (More)
After cellular injury many endogenous toxins are released from injured cells and result in secondary injury. To elucidate mechanisms of such injury many of these toxins have been studied individually. However, the data obtained is only useful for reference and does not accurately represent the multifactorial situation under pathophysiological conditions.… (More)
Reaction of daunorubicin (1) and adriamycin (2) with aldehydes and ketones in the presence of NaCNBH3 afforded N-alkyl- and N,N-dialkylanthracyclines along with their 13-dihydro derivatives. Product ratios depended upon the nature of the carbonyl reagent and the starting drug. The majority of these analogues retained in vivo antitumor activity comparable to… (More)
Treatment of daunorubicin with methanolic ammonia affords 5-iminodaunorubicin, the first quinone-modified analogue of either daunorubicin or adriamycin. This product retains antileukemic activity in mice, is less cardiotoxic by electrocardiographic measurements in rats, and is nonmutagenic in Salmonella typhimurium (Ames test).
The decay J/psi-->NNpi provides an effective isospin 1/2 filter for the piN system due to isospin conservation. Using 58x10(6) J/psi decays collected with the Beijing Electromagnetic Spectrometer at the Beijing Electron Positron Collider, more than 100 thousand J/psi-->ppi-n+c.c. events are obtained. Besides the two well-known N* peaks at around 1500 MeV/c2… (More)
A series of rubidazone analogues (4-14) with varying phenyl group substituents was prepared. The effect of these compounds on inhibition of nucleic acid synthesis in cultured cells, on in vivo antitumor properties, and on cardiotoxicity was examined. Substituent effects on drug-DNA binding as indicated by DNA melting temperature measurements were also… (More)