Can I read Water Soluble Prodrugs of the Antitumor Agent 3-[(3-Amino-4-methoxy)phenyl]-2-(3,4,5-trimethoxyphenyl)cyclopent-2-ene-1-one on EtoBox?

Water Soluble Prodrugs of the Antitumor Agent 3-[(3-Amino-4-methoxy)phenyl]-2-(3,4,5-trimethoxyphenyl)cyclopent-2-ene-1-one by Nguyen-Hai Nam; Yong Kim; Young-Jae You; Dong-Ho Hong; Hwan-Mook Kim; Byung-Zun Ahn is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Water Soluble Prodrugs of the Antitumor Agent 3-[(3-Amino-4-methoxy)phenyl]-2-(3,4,5-trimethoxyphenyl)cyclopent-2-ene-1-one about?

Fourteen prodrugs of the antitumor agent 3-[(3-amino-4-methoxy)phenyl]-2-(3,4,5-trimethoxyphenyl)cyclopent-2-ene-1-one (1) were prepared to improve its water solubility and potency. These prodrugs include alpha-amino acid (1a-1h), aliphatic amino acid (1i-1l), phosphoramidate (1m), and phosphate (1n) derivatives. All of the prodrugs showed improved water solubility. A number of the amino acid prodrugs (1a, 1b, 1d-1f, 1h, 1j, and 1k) exhibited more potent antitumor activity compared to the parent compound (1). The phosphate prodrug 1n also offered a potent antitumor activity, but the phosphoramidate 1m did not show any antitumor activity in vivo. None of the prodrugs exhibited significant toxicities in mice. These results indicate that the design and preparation of the amino acid prodrugs (1a, 1b, 1d-1f, 1h, 1j, and 1k) and phosphate prodrug (1n) are beneficial for enhancing the antitumor activity of 1. The similar approaches may be used to improve water solubility and bioactivity of other poorly soluble aromatic amines.

Who reads Water Soluble Prodrugs of the Antitumor Agent 3-[(3-Amino-4-methoxy)phenyl]-2-(3,4,5-trimethoxyphenyl)cyclopent-2-ene-1-one?

Author

Nguyen-Hai Nam; Yong Kim; Young-Jae You; Dong-Ho Hong; Hwan-Mook Kim; Byung-Zun Ahn

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2003

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)