Discovery of novel serine palmitoyltransferase inhibitors as cancer therapeutic agents

[Display omitted] We pursued serine palmitoyltransferase (SPT) inhibitors as novel cancer therapeutic agents based on a correlation between SPT inhibition and growth suppression of cancer cells. High-throughput screening and medicinal chemistry efforts led to the identification of structurally diver...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2018-05, Vol.26 (9), p.2452-2465
Hauptverfasser:	Kojima, Takuto, Asano, Yasutomi, Kurasawa, Osamu, Hirata, Yasuhiro, Iwamura, Naoki, Wong, Tzu-Tshin, Saito, Bunnai, Tanaka, Yuta, Arai, Ryosuke, Yonemori, Kazuko, Miyamoto, Yasufumi, Sagiya, Yoji, Yaguchi, Masahiro, Shibata, Sachio, Mizutani, Akio, Sano, Osamu, Adachi, Ryutaro, Satomi, Yoshinori, Hirayama, Megumi, Aoyama, Kazunobu, Hiura, Yuto, Kiba, Atsushi, Kitamura, Shuji, Imamura, Shinichi
Format:	Artikel
Sprache:	eng
Schlagworte:	3-KDS Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Antitumor efficacy Cell Line, Tumor Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology High-Throughput Screening Assays Humans Mice Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacokinetics Piperidines - pharmacology Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacokinetics Pyrazoles - pharmacology Serine C-Palmitoyltransferase - antagonists & inhibitors SPT Stereoisomerism Structure-Activity Relationship Xenograft Model Antitumor Assays
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