TY - JOUR
T1 - Design and synthesis of new mitochondrial cytotoxin N-thiadiazolylanilines that inhibit tumor cell growth
AU - Hori, Hitoshi
AU - Noguchi, Naoto
AU - Yokoyama, Hideakira
AU - Ise, Hirohiko
AU - Jin, Cheng Zhe
AU - Kasai, Soko
AU - Goto, Takatsugu
AU - Taira, Zenei
PY - 1996/1/1
Y1 - 1996/1/1
N2 - 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 supports the notion that the inhibition of tumor cell growth of inhibitor of protein tyrosine kinase AG17, which is identical to SF 6847, may be due to its mitochondrial cytotoxicity.
AB - 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 supports the notion that the inhibition of tumor cell growth of inhibitor of protein tyrosine kinase AG17, which is identical to SF 6847, may be due to its mitochondrial cytotoxicity.
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U2 - 10.1016/0968-0896(95)00182-4
DO - 10.1016/0968-0896(95)00182-4
M3 - Article
C2 - 8814882
AN - SCOPUS:0029920392
VL - 4
SP - 247
EP - 253
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 2
ER -