Synthesis, characterization and biological evaluation of bile acid-aromatic/heteroaromatic amides linked via amino acids as anti-cancer agents
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- 作者：Devesh S. Agarwala ; Hasitha Shilpa Anantarajub ; Dharmarajan Sriramb ; Perumal Yogeeswarib ; Shankara H. Nanjegowdac ; P. Malluc ; Rajeev Sakhujaa ; sakhuja.rajeev@gmail.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Cancer ; Cholic acid ; Coupling ; Cytotoxicity ; Amino acid ; Heteroaryl amines
- 刊名：Steroids
- 出版年：2016
- 出版时间：March 2016
- 年：2016
- 卷：107
- 期：Complete
- 页码：87-97
- 全文大小：803 K
文摘
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Series of bile acid aryl/heteroaryl amides linked via α-amino acid were synthesized.
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Cytotoxic behavior against HT29, MDAMB231, U87MG were tested.
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Three conjugates showed good in vitro activity (GI50 = 1.35, 1.41, 4.52 μM) against MDAMB231.
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Another three conjugates showed good in vitro activity (GI50 = 2.49, 2.46, 1.62 μM) against U87MG.
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Greater than 65% of the synthesized compounds were found to be safer on human normal cell line (HEK293T).