Synthesis and antitumor activity of water-soluble duocarmycin B1 prodrugs |
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| Authors: | Asai A Nagamura S Kobayashi E Gomi K Saito H |
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| Affiliation: | Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Japan. |
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| Abstract: | The water-soluble duocarmycin B1 prodrugs such as glycoside 3, phosphate 4 and carbamate 5 were synthesized for improving biological and pharmaceutical profiles of duocarmycin. Among these prodrugs, N-methylpiperazinylcarbamoyl derivative 5 exhibited potent antitumor activity against several human tumors in vivo. |
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