Synthesis and in vitro evaluation of analogues of avocado-produced toxin (+)-(R)-persin in human breast cancer cells

A structure–activity study of several new synthetic analogues of the avocado-produced toxin persin has been conducted, with compounds being evaluated for their cytostatic and pro-apoptotic effects in human breast cancer cells. A 4-pyridinyl derivative demonstrated activity comparable to that of the...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2011-12, Vol.19 (23), p.7033-7043
Hauptverfasser:	Brooke, Darby G., Shelley, Elizabeth J., Roberts, Caroline G., Denny, William A., Sutherland, Robert L., Butt, Alison J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-cancer agent Antineoplastic agents Antineoplastic Agents, Phytogenic - chemical synthesis Antineoplastic Agents, Phytogenic - chemistry Antineoplastic Agents, Phytogenic - pharmacology apoptosis Avocado Biological and medical sciences Breast cancer breast neoplasms Breast Neoplasms - drug therapy Breast Neoplasms - pathology Cell Line, Tumor Estrogen receptor Fatty Alcohols - chemical synthesis Fatty Alcohols - chemistry Fatty Alcohols - pharmacology Female General aspects General pharmacology Humans in vitro studies Medical sciences Persea - chemistry Persin Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Plant Extracts - chemical synthesis Plant Extracts - chemistry Plant Extracts - pharmacology Structure-Activity Relationship structure-activity relationships β-Hydroxyketone
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Beschreibung
Zusammenfassung:	A structure–activity study of several new synthetic analogues of the avocado-produced toxin persin has been conducted, with compounds being evaluated for their cytostatic and pro-apoptotic effects in human breast cancer cells. A 4-pyridinyl derivative demonstrated activity comparable to that of the natural product, suggesting future directions for exploration of structure–activity relationships.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2011.10.006