New ferrocene modified lawsone Mannich bases with anti-proliferative activity against tumor cells

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• 作者：Aamir Ahmad^a ; Katharina Mahal^b ; Subhash Padhye^c ; Fazlul H. Sarkar^a ; Rainer Schobert^b ; Bernhard Biersack^b ; ^{bernhard.biersack@yahoo.com}
• 关键词：Ferrocene ; Lawsone ; Mannich base ; Anticancer drugs ; Multi-drug resistance ; Prostate cancer
• 刊名：Journal of Saudi Chemical Society
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：21
• 期：1
• 页码：105-110
• 全文大小：1538 K
• 卷排序：21

文摘

Lawsone (1a) is a known naphthoquinone dye from the Henna plant Lawsonia inermis. Out of a series of four new ferrocene modified Mannich bases of 1a, the 2-pyridyl derivative 2a was distinctly more active than its analogs 2b–d in breast, prostate and pancreatic cancer cells. 2a also exhibited greater antiproliferative effects when compared with the known anticancer active Mannich bases 1b and 1c in the androgen-receptor negative PC-3 prostate and Pgp-expressing KB-V1/Vbl cervix carcinoma cell lines. Compound 2a reached sub-micromolar activities in these aggressive cancer cells and, thus, features a promising drug candidate for the efficient treatment of hormone- or multidrug-resistant cancer types.