Abstract
| - Three different types of 1,4-disubstituted anthraceneswere synthesized, and their cytotoxicityin a panel of tumor cells was compared with that of the corresponding9,10-disubstitutedanthracenes. The panel contained human myeloma, melanoma, colon,and lung cancer cellsand sensitive and multidrug-resistant murine L1210 leukemia cells.These compounds had[[(dimethylamino)ethyl]amino]methyl,N-[(dimethylamino)ethyl]carbamoyl, andcarboxaldehyde(4,5-dihydro-1H-imidazol-2-yl)hydrazone side chains.The 1,4-diamide was more potent acrossthe tumor panel than the corresponding 9,10-isomer, but the1,4-diamine and the 1,4-hydrazonewere less potent than their 9,10-isomers. Although the1,4-hydrazone was active against P388leukemia in mice, it was inactive against L1210 leukemia. Withineach pair of compounds,the one with greater average potency against tumor cells gave a greaterincrease in thetransition melt temperature of DNA.
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