Synthesis and Biological Activity of C-8 Fluoroaryl Substituted Pyrimidine Linked-Pyrrolobenzodiazepine Conjugates

Title: Synthesis and Biological Activity of C-8 Fluoroaryl Substituted Pyrimidine Linked-Pyrrolobenzodiazepine Conjugates

Volume: 2 Issue: 1

Author(s): Ahmed Kamal, K. Laxma Reddy, V. Devaiah, N. Shankaraiah, M. Shiva Kumar and G. Suresh Kumar Reddy

Affiliation:

Keywords: pyrrolobenzodiazepines, pyrimidines, cytotoxicity, antitumour activity

Abstract: Synthesis of C-8 fluoroaryl substituted pyrimidine linked-PBD conjugates are described. The compounds are prepared with varying degrees of linker length in order to probe the structural requirements for optimal in vitro antitumour activity. These compounds have been tested against a panel of 60 human cancer cell lines, and it is demonstrated that compound 5b with four carbon spacer exhibited promising in vitro anticancer activity in comparison to the other analogues (5a and 5c).

Cite this article as:

Kamal Ahmed, Reddy Laxma K., Devaiah V., Shankaraiah N., Kumar Shiva M. and Reddy Suresh Kumar G., Synthesis and Biological Activity of C-8 Fluoroaryl Substituted Pyrimidine Linked-Pyrrolobenzodiazepine Conjugates, Letters in Drug Design & Discovery 2005; 2 (1) . https://dx.doi.org/10.2174/1570180053398343

DOI https://dx.doi.org/10.2174/1570180053398343	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X