Musa Musiliyu A, Khan M Omar F, Cooperwood John S
Florida A and M University, College of Arts and Sciences, Department of Chemistry, 219 Jones Halls, Tallahassee, FL 32307, USA; Tel: (1)-850-599-3509.
Lett Drug Des Discov. 2009 Mar;6(2):133-138. doi: 10.2174/157018009787582624.
The syntheses and cytotoxic activity of coumarin-estrogen conjugates are described. In vitro results indicated that conjugates 10, 11 and 13 show growth inhibitory activities at 5-dose concentration (100, 10, 1, 0.1, 0.01 muM) against the following NCI-7- human breast cancer cell lines: BT-549, HS 578T, MCF 7, MDA-MB-231/ATCC, MDA-MB-435, NCI/ADR-RES, and thus serve as new leads for further development of antibreast cancer agent.
描述了香豆素 - 雌激素缀合物的合成及细胞毒性活性。体外实验结果表明,缀合物10、11和13在5个剂量浓度(100、10、1、0.1、0.01 μM)下对以下NCI - 7种人乳腺癌细胞系显示出生长抑制活性:BT - 549、HS 578T、MCF 7、MDA - MB - 231/ATCC、MDA - MB - 435、NCI/ADR - RES,因此可作为进一步开发抗乳腺癌药物的新先导物。