Boronic Analogues of (R)-6-O-Desmethylantofine as Anticancer Agents.
Chem Pharm Bull (Tokyo)
; 67(12): 1324-1327, 2019 Dec 01.
Article
in En
| MEDLINE
| ID: mdl-31564698
ABSTRACT
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 30 nM.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Boronic Acids
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Chem Pharm Bull (Tokyo)
Year:
2019
Type:
Article