Boronic analogues of (R)-6-O-desmethylantofine as anticancer agents.

@article{Omran2019BoronicAO,
  title={Boronic analogues of (R)-6-O-desmethylantofine as anticancer agents.},
  author={Ziad Omran and Ashraf N. Abdalla and Munjed M. Ibrahim and Mohammad Akbar Hossain and Mohamed Alarja and Linwei Chen and Yuxiu Liu and Qingmin Wang},
  journal={Chemical \& pharmaceutical bulletin},
  year={2019}
}
Phenanthroindolizidines are naturally occurring alkaloids mainly isolated from different species of Asclepiadaceae. These alkaloids are characterized by an excellent anticancer activity against a very wide range of cancerous cell lines including those who are multi drug resistant. Nevertheless, phenanthroindolizidines are associated with sever neurotoxicity that prevented any candidate from this family to pass the clinical trials. A number of boron-based analogues of (R)-6-O-desmethylantofine… 

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The developed quaternary ammonium salts of phenanthroindolizidines showed high chemical and metabolic stability and are predicted to have no penetration through the blood–brain barrier, and the designed prodrugs displayed decreased cytotoxicity when tested under normoxic conditions, however, their cytotoxic activity considerably increased when testing under hypoxic conditions.

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