Design and synthesis of new mitochondrial cytotoxin N-thiadiazolylanilines that inhibit tumor cell growth

…, N Noguchi, H Yokoyama, H Ise, CZ Jin, S Kasai…

Index: Hori, Hitoshi; Noguchi, Naoto; Yokoyama, Hideakira; Ise, Hirohiko; Jin, Cheng-Zhe; Kasai, Soko; Goto, Takatsugu; Taira, Zenei Bioorganic and Medicinal Chemistry, 1996 , vol. 4, # 2 p. 247 - 253

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Abstract

New N-thiadiazolylanilines were designed and synthesized to develop mitochondrial cytotoxins superior to SF 6847. The mitochondrial cytotoxin N-thiadiazolylanilines, TX-108 and TX-109, inhibited EMT6/KU mammary sarcoma cell growth at a low micromolar concentration. Their inhibitory activities were parallel to their mitochondrial cytotoxicity, such as uncoupling oxidative phosphorylation and inhibiting ATP synthesis. This report also ...