Design, synthesis and biological evaluation of estradiol-chlorambucil hybrids as anticancer agents

作者：Gupta Atul; Saha Pijus; Descoteaux Caroline; Leblanc Valerie; Asselin Eric; Berube Gervais^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(5): 1614-1618.

DOI：10.1016/j.bmcl.2010.01.053

• Estradiol-chlorambucil hybrids
• Anticancer agents
• Estrogen receptor
• Breast cancer

A series of estradiol-chlorambucil hybrids was synthesized as anticancer drugs for site-directed chemotherapy of breast cancer. The novel compounds were synthesized in good yields through efficient modifications of estrone at position 16 alpha of the steroid nucleus. The newly synthesized compounds were evaluated for their anticancer efficacy in different hormone-dependent and hormone-independent breast cancer cell lines. The novel hybrids showed significant in vitro anticancer activity when compared to chlorambucil. Structure-activity relationship (SAR) reveals the influence of the length of the spacer chain between carrier and drug molecule.

• 出版日期2010-3-1