- Design and synthesis of new mitochondrial cytotoxin N-thiadiazolylanilines that inhibit tumor cell growth
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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.
- Hori, Hitoshi,Noguchi, Naoto,Yokoyama, Hideakira,Ise, Hirohiko,Jin, Cheng-Zhe,Kasai, Soko,Goto, Takatsugu,Taira, Zenei
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- Preparation method of 2, 4-dichloro-3, 5-dinitrobenzotrifluoride
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The invention discloses a preparation method of 2, 4-dichloro-3, 5-dinitrobenzotrifluoride, and the method comprises the following steps: carrying out first-step nitration reaction by using 2, 4-dichlorobenzotrifluoride as a raw material, and carrying out phase separation to obtain waste acid and a nitration intermediate after the reaction; mixing fuming nitric acid and fuming sulfuric acid to form mixed acid, carrying out a second-step nitration reaction on the mixed acid and the nitration intermediate, and carrying out phase separation after the reaction to obtain semi-waste acid and the target compound 2, 4-dichloro-3, 5-dinitrobenzotrifluoride, wherein the semi-waste acid separated from the nitration reaction in the second step can be directly recycled in the nitration reaction in thefirst step, and is mixed with the 2, 4-dichlorobenzotrifluoride to perform a new round of nitration reaction. According to the preparation method of the 2, 4-dichloro-3, 5-dinitrobenzotrifluoride, disclosed by the invention, two-step reaction is carried out under normal pressure, the operation is simple, and the purity of the finished product is high; the semi-waste acid generated in the second step of nitrification can be directly used in the first step of nitrification reaction, so that the circular economy is realized, and the waste acid discharge is reduced.
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Paragraph 0025-0026; 0029-0031
(2020/08/25)
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- Synthesis and evaluation of oryzalin analogs against Toxoplasma gondii
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The synthesis and evaluation of 20 dinitroanilines and related compounds against the obligate intracellular parasite Toxoplasma gondii is reported. Using in vitro cultures of parasites in human fibroblasts, we determined that most of these compounds selectively disrupted Toxoplasma microtubules, and several displayed sub-micromolar potency against the parasite. The most potent compound was N1,N1-dipropyl-2,6-dinitro-4-(trifluoromethyl)-1,3- benzenediamine (18b), which displayed an IC50 value of 36 nM against intracellular T. gondii. Based on these data and another recent report [Ma, C.; Tran, J.; Gu, F.; Ochoa, R.; Li, C.; Sept, D.; Werbovetz, K.; Morrissette, N. Antimicrob. Agents Chemother. 2010, 54, 1453], an antimitotic structure-activity relationship for dinitroanilines versus Toxoplasma is presented.
- Endeshaw, Molla M.,Li, Catherine,Leon, Jessica De,Yao, Ni,Latibeaudiere, Kirk,Premalatha, Kokku,Morrissette, Naomi,Werbovetz, Karl A.
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scheme or table
p. 5179 - 5183
(2010/10/03)
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- N3 -(Cycloalkyl)alkyl-2,4-dinitro-6-trifluoromethyl-1,3-phenylenediamine compounds
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N3 -(Cycloalkyl)alkyl-2,4-dinitro-6-trifluoromethyl-1,3-phenylenediamine compounds of the formula STR1 wherein R1 is selected from the group consisting of H--, C1 -C6 straight and branched chain alkyl, haloalkyl and hydroxyalkyl, C2 -C6 straight and branched chain alkenyl, alkynyl and alkoxyalkyl and C 3 -C6 cycloalkyl; R2 is selected from the group consisting of C3 -C5 cycloalkyl groups and C3 -C5 cycloalkyl groups substituted with C1 -C6 straight and branched chain alkyl; and n is 1, 2 or 3. The compounds are useful in herbicidal compositions.
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- One step process for preparing 2,6-dinitro-4-trifluoromethylchlorobenzene by nitration of 4-trifluoromethylchlorobenzene
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There is disclosed a one-step process for dinitrating 4-trifluoromethylchlorobenzene to obtain the 2,6-dinitro-derivative.
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