2. Academic Validation
  3. Phosphonate-linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: synthesis, DNA-binding affinity and cytotoxicity

Phosphonate-linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: synthesis, DNA-binding affinity and cytotoxicity

  • Bioorg Med Chem. 2008 Apr 1;16(7):3895-906. doi: 10.1016/j.bmc.2008.01.040.
Ahmed Kamal 1,  P Praveen Kumar,  B N Seshadri,  O Srinivas,  M Shiva Kumar,  Subrata Sen,  Nisha Kurian,  Aarti S Juvekar,  Surekha M Zingde
Affiliations

Affiliation

  • 1 Biotransformation Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad, Andhra Pradesh 500 007, India. ahmedkamal@iict.res.in
PMID: 18262426 DOI: 10.1016/j.bmc.2008.01.040
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.

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