الفهرس 
ChemistryOnly 14 pages are availabe for public view
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Abstract
The present study investigates the content of the leaves and barks of Melaleuca ericifolia Smith, growing in Egypt and reports from the leaves the isolation of eleven pentacyclic triterpenes three of them are new, along with other eight known compounds most of them are isolated for the first time from this species. The effect of the isolated triterpenes of on the highly malignant +SA mouse mammary epithelial cell proliferation was studied. The tested compounds showed different positive results in term of antiproliferative activities. Betulinic acid, the major lupane type pentacyclic triterpene of M. ericifolia leaves, was used to design thirteen derivatives (eleven of them are new) based on molecular modeling studies and their virtual affinities to inhibit topoisomerases I and IIα. These derivatives were tested for their topoisomerase I and IIα inhibitory activities and for their in vitro cytotoxic activities against several cancer cell lines including colon and breast cancer cell lines. Methyleugenol, the main component of the essential oil of M. ericifolia leaves, was used to design fourteen biaryl derivatives (eleven of them are new) using molecular modeling techniques and tubulin as the molecular target. These derivatives were tested for their anti-invasive activity against the breast cancer cells MDA-MB-231 and showed high activities. The designed biaryl methyleugenol derivatives were also tested for their cytotoxic activities against MDA-MB-231 and MCF-7 breast cancer cell lines. The results showed that the new designed agents can impair the invasive potential of the cancer cells at non-cytotoxic doses (1-4M).