Synthesis and biological evaluation of cinnamido linked pyrrolo[2,1-c][1,4]benzodiazepines as antimitotic agents

European Journal of Medicinal Chemistry
Ahmed KamalShasi V Kalivendi


A series of new cinnamido-pyrrolo[2,1-c][1,4]benzodiazepine conjugates (4a-d and 5a-d) and their dimers (6a-d) have been designed, synthesized and evaluated for their biological activity. The anticancer screening of compound 4a by the NCI exhibited significant GI50 values ranging from 68 to 732 nM against 53 of 59 human cancer cell lines tested. Compounds 5a-d and 6a-d have also shown remarkable cytotoxic activity with GI50 values <0.1 microM concentrations in a large number of cell lines. Interestingly, compounds 5b and 6b have been identified as a new class of inhibitors of tubulin polymerization and their action has been rationalized by the cell cycle arrest in G0 and G2/M phase.


Dec 21, 2010·Chemical Reviews·Dyeison Antonow, David E Thurston
Aug 20, 2011·Journal of Medicinal Chemistry·M Amarnath ReddyB Sreedhar
Aug 19, 2014·PloS One·Khondaker M RahmanDavid E Thurston
Apr 13, 2017·Bioorganic & Medicinal Chemistry Letters·Thokhir B ShaikAhmed Kamal
Oct 4, 2014·Colloids and Surfaces. B, Biointerfaces·C Ganesh KumarSuman Kumar Mamidyala
Feb 10, 2017·Zeitschrift Für Naturforschung. C, a Journal of Biosciences·Patel NavinGildardo Rivera

Related Concepts

Cell Cycle
Cell Nucleus
TUBE1 gene
Apoptosis, Intrinsic Pathway
Inhibitory Concentration 50
Protein Structure, Quaternary
Cell Line, Tumor
Antimitotic Agents
Protein Multimerization

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