Synthesis and DNA-binding ability of C2R-fluoro substituted DC-81 and its dimers

Ahmed Kamal; D Rajasekhar Reddy; P S Murali Mohan Reddy

doi:10.1016/j.bmcl.2006.10.070

Synthesis and DNA-binding ability of C2R-fluoro substituted DC-81 and its dimers

Bioorg Med Chem Lett. 2007 Feb 1;17(3):803-6. doi: 10.1016/j.bmcl.2006.10.070. Epub 2006 Oct 27.

Authors

Ahmed Kamal¹, D Rajasekhar Reddy, P S Murali Mohan Reddy

Affiliation

¹ Biotransformation Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500007, India. ahmedkamal@iict.res.in

PMID: 17113291
DOI: 10.1016/j.bmcl.2006.10.070

Abstract

C2R-Fluoro substituted DC-81 and its dimers have been synthesized that exhibit significant DNA-binding ability, particularly the five carbon alkane spacer compound (6c) showed the helix melting temperature (DeltaTm) of 18.8 degrees C after incubation of 36 h at 37 degrees C.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzodiazepines / chemical synthesis*
Benzodiazepines / pharmacology*
DNA / metabolism*
Hot Temperature
Indicators and Reagents
Protein Denaturation
Pyrroles / chemical synthesis*
Pyrroles / pharmacology*
Structure-Activity Relationship

Substances

Indicators and Reagents
Pyrroles
pyrrolo(2,1-c)(1,4)benzodiazepine
Benzodiazepines
DNA