Abstract
Pyrrolobenzodiazepine-diethylphosphonate conjugates have been designed and synthesized that link through two different types of spacers that are simple alkane chain and also a piperazine moiety side-armed with the alkane chains. These pyrrolobenzodiazepine conjugates have exhibited remarkable DNA-binding affinity and improved solubility in water, a representative compound 7d showing promising in vitro cytotoxicity.
Original language | English (US) |
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Pages (from-to) | 3895-3906 |
Number of pages | 12 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 16 |
Issue number | 7 |
DOIs | |
State | Published - Apr 1 2008 |
Bibliographical note
Funding Information:The authors P.P.K., B.N.S., O.S and M.S.K. thank CSIR, New Delhi for the award of research fellowships. We are also thankful to the Department of Biotechnology (BT/PR/7037/Med/14/933/2006), New Delhi for financial assistance.
Keywords
- Cytotoxicity
- DNA-binding affinity
- Diethylphosphonate
- Pyrrolobenzodiazepine