Phosphonate-linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: Synthesis, DNA-binding affinity and cytotoxicity
| Autor: | Aarti Juvekar, P. Praveen Kumar, Ahmed Kamal, O. Srinivas, B. N. Seshadri, M. Shiva Kumar, Nisha Kurian, Subrata Sen, Surekha M. Zingde |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
Cell Survival
Stereochemistry Clinical Biochemistry Organophosphonates Pharmaceutical Science Pyrrolobenzodiazepine Nucleic Acid Denaturation Biochemistry Chemical synthesis Benzodiazepines Structure-Activity Relationship chemistry.chemical_compound Cell Line Tumor Drug Discovery Animals Humans Moiety Structure–activity relationship Pyrroles Cytotoxicity Molecular Biology Amination Molecular Structure Organic Chemistry Temperature DNA Phosphonate Piperazine chemistry Lactam Molecular Medicine Cattle Dimerization |
| Zdroj: | Bioorganic & Medicinal Chemistry. 16:3895-3906 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2008.01.040 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect