Literature DB >> 10571162

Synthesis and antitumor activity of water-soluble duocarmycin B1 prodrugs.

A Asai1, S Nagamura, E Kobayashi, K Gomi, H Saito.   

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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Year:  1999        PMID: 10571162     DOI: 10.1016/s0960-894x(99)00518-1

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  A fundamental relationship between hydrophobic properties and biological activity for the duocarmycin class of DNA-alkylating antitumor drugs: hydrophobic-binding-driven bonding.

Authors:  Amanda L Wolfe; Katharine K Duncan; James P Lajiness; Kaicheng Zhu; Adam S Duerfeldt; Dale L Boger
Journal:  J Med Chem       Date:  2013-08-29       Impact factor: 7.446

  1 in total

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