Discovery, Optimization, and Pharmacophore Modeling of Oleanolic Acid and Analogues as Breast Cancer Cell Migration and Invasion Inhibitors Through Targeting Brk/Paxillin/Rac1 Axis

Bioassay‐guided fractionation of Terminalia bentzoe L. leaves methanol extract identified the known triterpene oleanolic acid (1) as its major breast cancer cell migration inhibitor. Further chemical optimization afforded five new (9–12 and 15) and seven known (4–8, 13, and 14) semisynthetic analogu...

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Veröffentlicht in:	Chemical biology & drug design 2015-02, Vol.85 (2), p.231-243
Hauptverfasser:	Elsayed, Heba E., Akl, Mohamed R., Ebrahim, Hassan Y., Sallam, Asmaa A., Haggag, Eman G., Kamal, Amel M., El Sayed, Khalid A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents, Phytogenic - chemistry Antineoplastic Agents, Phytogenic - pharmacology bioassay-guided Breast - drug effects Breast - metabolism Breast - pathology breast cancer Breast Neoplasms - drug therapy Breast Neoplasms - metabolism Breast Neoplasms - pathology Brk/Paxillin/Rac1 axis Cell Line, Tumor Cell Movement - drug effects Combretaceae Drug Discovery Female Humans Models, Molecular Neoplasm Invasiveness - pathology Neoplasm Invasiveness - prevention & control Neoplasm Proteins - metabolism oleanolic acid Oleanolic Acid - chemistry Oleanolic Acid - pharmacology Paxillin - metabolism Protein-Tyrosine Kinases - metabolism rac1 GTP-Binding Protein - metabolism Signal Transduction - drug effects Terminalia - chemistry Terminalia bentzoe L
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