Design and synthesis of chlorinated and fluorinated 7-azaindenoisoquinolines as potent cytotoxic anticancer agents that inhibit topoisomerase I
MSA Elsayed, Y Su, P Wang, T Sethi… - Journal of medicinal …, 2017 - ACS Publications
The 7-azaindenoisoquinolines are cytotoxic topoisomerase I (Top1) inhibitors. Previously
reported representatives bear a 3-nitro group. The present report documents the
replacement of the potentially genotoxic 3-nitro group by 3-chloro and 3-fluoro substituents,
resulting in compounds with high Top1 inhibitory activities and potent cytotoxicities in human
cancer cell cultures and reduced lethality in an animal model. Some of the new Top1
inhibitors also possess moderate inhibitory activities against tyrosyl-DNA …
reported representatives bear a 3-nitro group. The present report documents the
replacement of the potentially genotoxic 3-nitro group by 3-chloro and 3-fluoro substituents,
resulting in compounds with high Top1 inhibitory activities and potent cytotoxicities in human
cancer cell cultures and reduced lethality in an animal model. Some of the new Top1
inhibitors also possess moderate inhibitory activities against tyrosyl-DNA …
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