Synthesis of d- and l-tyrosine-chlorambucil analogs active against breast cancer cell lines
| Autor: | Eric Asselin, Caroline Descôteaux, Valérie Leblanc, Kevin Brasseur, Atul Gupta, Gervais Bérubé |
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| Rok vydání: | 2010 |
| Předmět: |
Receptor
ErbB-2 Stereochemistry Clinical Biochemistry Pharmaceutical Science Estrogen receptor Antineoplastic Agents Breast Neoplasms Biochemistry Chemical synthesis Structure-Activity Relationship Breast cancer Cell Line Tumor Drug Discovery medicine Humans Structure–activity relationship Moiety Tyrosine skin and connective tissue diseases Molecular Biology Chlorambucil Chemistry Organic Chemistry Stereoisomerism medicine.disease Cell culture Molecular Medicine Female medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:7388-7392 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2010.10.039 |
| Popis: | A series of D- and L-tyrosine-chlorambucil analogs was synthesized as anticancer drugs for chemotherapy of breast cancer. The novel compounds were synthesized in good yields through efficient modifications of D- and L-tyrosine. The newly synthesized compounds were evaluated for their anticancer efficacy in different hormone-dependent and hormone-independent (ER+ and ER-) breast cancer cell lines. The novel analogs showed significant in vitro anticancer activity when compared to chlorambucil. Structure-activity relationship (SAR) reveals both, the influence of the length of the spacer chain and the stereochemistry of the tyrosine moiety. Interestingly, the D- and L-tyrosinol-chlorambucil derivatives with 10 carbon atoms spacer are selective towards MCF-7 (ER+) breast cancer cell line. |
| Databáze: | OpenAIRE |
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