Boronic Analogues of (R)-6-O-Desmethylantofine as Anticancer Agents

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, phen...

Full description

Saved in:

Bibliographic Details
Published in:	Chemical and Pharmaceutical Bulletin Vol. 67; no. 12; pp. 1324 - 1327
Main Authors:	Ziad Omrana, Ashraf N.Abdallaa, Munjed M.Ibrahima, Mohammad A.Hossaina, Mohamed Alarjaa, Linwei Chenb, Yuxiu Liub, Qingmin Wangb
Format:	Journal Article
Language:	Japanese
Published:	Pharmaceutical Society of Japan 01-12-2019
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	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 have been synthesised. Their physochemical properties were evaluated, same as their in-vitro antiproliferative activity. The pinacol boronate ester derivative (3) showed interesting cytotoxicity against a panel of cancerous cell lines attested by a cancer cell growth-inhibitory potency (GI50) as low as 30nM.
ISSN:	0009-2363