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Runt-related transcription factor 1 (RUNX1) is generally considered to function as a tumor suppressor in the development of leukemia, but a growing body of evidence suggests that it has pro-oncogenic properties in acute myeloid leukemia (AML). Here we have demonstrated that the antileukemic effect mediated by RUNX1 depletion is highly dependent on a functional p53-mediated cell death pathway. Increased expression of other RUNX family members, including RUNX2 and RUNX3, compensated for the antitumor effect elicited by RUNX1 silencing, and simultaneous attenuation of all RUNX family members as a cluster led to a much stronger antitumor effect relative to suppression of individual RUNX members. Switching off the RUNX cluster using alkylating agent–conjugated pyrrole-imidazole (PI) polyamides, which were designed to specifically bind to consensus RUNX-binding sequences, was highly effective against AML cells and against several poor-prognosis solid tumors in a xenograft mouse model of AML without notable adverse events. Taken together, these results identify a crucial role for the RUNX cluster in the maintenance and progression of cancer cells and suggest that modulation of the RUNX cluster using the PI polyamide gene-switch technology is a potential strategy to control malignancies.

We investigated photoinduced electron accumulation in a colloidal system of layered hexaniobate that is known as a photocatalytically active wide band-gap semiconductor, and attempted to control the photoresponse by introducing additives into the colloid. The inorganic nanosheets were obtained by exfoliation of the layered oxide. UV-irradiation of the colloids led to electron accumulation in the nanosheets to generate reduced niobate species. Propylammonium ions introduced as the exfoliating reagent and present as the counter ions of niobate nanosheets were indicated as the electron donor that stabilized the electron-accumulating state. Yield and half-life of the reduced niobate species greatly increased by adding an appropriate amount of photochemically inert clay nanosheets, while they increased only a little by the addition of molecular electron donors such as EDTA and triethanolamine. Moreover, the molecular species diminished the enhancement effect of the clay nanosheets. The results suggested that the photochemical event was not explained by direct interactions between the semiconductor nanosheets and the additives at molecular level but governed by indirect interactions between the colloid components regulated by the colloid structure.

Performance of photoresist stripping using steam-water mixed spray is quantitatively investigated with water flow rate as the operating parameter. The most striking and the most important finding is that air-water mixed spray turns out hardly effective. This result shows the peculiar superiority of the proposed technique. As we found that the prominently excessive long time of spraying of steam-water mixture on metal surface results in surface abrasion, this result strongly suggests that both the resist strippping and metal surface abrasion are dominated by essentially the same mechanism. We speculate that our proposing technique is categorized in the physical force cleaning. We discuss the role of the water flow rate in this cleaning technique and the validity of the assumption of physical force cleaning.

Architectural space is composed by the interrelationship of three elements; relationship between interior space and exterior space which created the space by putting the wall, relationship between interior space and interior space which is based on arrangement and expanse of room and wall and human being who enjoy two relationships and move in it. So to speak, the architectural design is pursuit of the interrelationship of three elements, and what were created by behavior are the outline, zone, and path. On this research, we define three kind of factor, outline which means expanse to exterior space, zone which means continuity of rooms and path which means positioning to the main rooms. Furthermore, we analyze by comparison of those factors and consider the interrelationship of three elements.

Condensation of O,O-diethyl phosphorochloridothioate with N-methoxyacetamide in the presence of a base gave selectively the geometrical isomers of O,O-diethyl O-1-(N-methoxyimino)ethylphosphorothioate which on heating rearranged to the corresponding thiolo isomers having P–S–C=N linkage.

Condensation of O,O-diethyl phosphorochloridothioate with N-methoxyacetamide in the presence of a base gave selectively the geometrical isomers of O,O-diethyl O-1-(N-methoxyimino)ethylphosphorothioate which on heating rearranged to the corresponding thiolo isomers having P–S–C=N linkage.

We investigated photoinduced charge separation occurring in a multicomponent colloidal system composed of oxide nanosheets of photocatalytically active niobate and photochemically inert clay and electron accepting methylviologen dications (MV2+). The inorganic nanosheets were obtained by exfoliation of layered hexaniobate and hectorite clay. The niobate and clay nanosheets were spatially separated in the colloidally dispersed state, and the MV2+ molecules were selectively adsorbed on the clay platelets. UV irradiation of the colloids led to electron transfer from the niobate nanosheets to the MV2+ molecules adsorbed on clay. The photoinduced electron transfer produced methylviologen radical cations (MV*+), which was characterized by high yield and long lifetime. The yield and stability of the MV*+ species were found to depend strongly on the clay content of the colloid: from a few mol % to approximately 70 mol % of the yield and several tens of minutes to more than 40 h of the lifetime. The contents of the niobate nanosheets and MV2+ molecules and the aging of the colloid also affected the photoinduced charge separation. In the absence of MV2+ molecules in the colloid, UV irradiation induced electron accumulation in the niobate nanosheets. The stability of the electron-accumulated state also depended on the clay content. The variation in the photochemical behavior is discussed in relation to the viscosity of the colloid.

The four diastereomers of 2-cyano-N-[1-(2,4-dichlorophenyl)ethyl]-3,3-dimethyl-butyramide were prepared by a direct HPLC separation with chiral columns. The [(S)acid, (R)amine]-isomer was the most antifungal among the diastereomers tested. Because of the lability of the clinical group in the acid moiety, the (RS)-(R)-isomer is being developed as a rice blasticide. (S-2900, proposed common name diclocymet).

Palladium(II) effectively catalyzes the [3,3]-sigmatropic type rearrangement of propargyl thionophosphates to provide allenyl thiolophosphates specifically.

Aryl alkyl (or benzyl) ketones are selectively prepared by the reaction of aryl iodides and alkyl iodides (or benzyl chlorides) in the presence of a stoichiometric amount of zinc-copper couple and a catalytic amount of palladium(0) complex under an atmospheric pressure of carbon monoxide.

Palladium acetate catalyzed the reaction of 4-bromo-2,6-lutidine with allylic alcohols to give 4-(3′ -oxo-alkyl)-2,6-lutidines selectively together with small amounts of 4-(2′ -oxo-alkyl)-2,6-lutidines. Under the same conditions, 4-chloro- and 2-bromopyridines react to give 4,4′- and 2,2′-bipyridyls, respectively.

Pd catalyzed reaction of allylic alcohols with 2-bromothiophene provides 3-(2'-thienyl)aldehydes or ketones selectively together with the small amounts of 2-(2'-thienyl)aldehydes and ketones. Similarly 3-(3'-thienyl)-aldehydes or ketones were obtained selectively from allylic alcohols and 3-bromothiophene. The reactivity and regioselectivity largely depend on the solvents, additives, and the structure of allylic alcohols. Generally aprotic dipolar solvent such as HMPA and DMF gave the most satisfactory results. 2-Thienyl iodide showed somewhat higher reactivity than 2-thienyl bromide. 2-Thienyl chloride was unreactive. Sodium iodide and/or triphenyl-phosphine were very effective as the cocatalysts especially for the reactions to give aldehydes. This thienylation reaction was also applicable to 2-bromothiophenes with a wide variety of substituents at 5-position. The synthetic utility of this catalytic reaction has been illustrated by the synthesis of 9-oxo-trans-2-decenoic acid (Queen substance).

Hydrosulfonylation de diene-1,3 acyclique et de vinyl-1 cycloalcenes par l'intermediaire de complexes π-allyl-Pd

1-ヒドロキシエチルホスフィン酸, その無機または有機塩基との塩類, およびそのエステル類が, キュウリのべと病に対して, 茎葉処理・土壌処理のいずれにおいても高い防除活性を示すことが見いだされた. これらの化合物は, 予防効果だけでなく治療効果をも有することが明らかになった. またこれらの化合物は, ジャガイモの疫病およびキュウリの灰色疫病に対しても防除活性を示した. 供試化合物中, 1-ヒドロキシエチルホスフィン酸の Ca (II) または Al (III) の塩が最も高い活性を示し, かつキュウリに対する薬害も軽微であった. なお, これらの化合物は, in vitro では抗菌活性を示さなかった.

A new thiono-thiolo allylic rearrangement of phosphoro- and phosphono-thionates with Pd(PPh3)4 catalyst is described, where a variety of thionates are converted to the corresponding thiolates in excellent yields.

N-Substituted 1-(alkoxyamino)alkylphosphonates were obtained by a new addition reaction of trialkyl phosphite and alkyl halide to nitrone. A push-pull type mechanism was suggested for the addition reaction.

There have been reported a few devices to overcome this difficulty by making use of relatively easily available 3-bromothiophene2 as a key compound. Among them, the reaction with 3-thienyllithium3 has been widely applied to prepare 3-substituted thiophenes. However, this reagent is unstable over -70°C and does not react with the less reactive electrophiles such as alkyl iodide, but decomposes at higher temperature to give a ring-opening product. 4

Palladium acetate catalyzed the reaction of 4-bromo-2,6-lutidine with allylic alcohols to give 4-(3′ -oxo-alkyl)-2,6-lutidines selectively together with small amounts of 4-(2′ -oxo-alkyl)-2,6-lutidines. Under the same conditions, 4-chloro- and 2-bromopyridines react to give 4,4′- and 2,2′-bipyridyls, respectively.

Alkyl 5-bromo-2-furoate reacts with allylic alcohols in the presence of 1 mol% of palladium acetate to give 1-(5′-alkoxycarbonyl-2′-furyl)-3-oxoalkanes (3) selectively, together with small amounts of 1- (5′-alkoxycarbonyl-2′-furyl)-2-oxoalkanes (4). The reaction (regio-selectivity and reactivity) largely depends on the structure of allylic alcohols.

Die Umsetzung von 3-Bromthiophen mit Allylalkoholen in Hexametapol in Gegenwart von Palladiumacetat ergibt 3-(3′-Thienyl)-aldehyde und -ketone.

3-(2-Thienyl)-aldehydes and ketones were prepared by catalytic reaction with palladium acetate from 2-bromothiophene and five kinds of allylic alcohols.

Palladium (0.6~3 mol%) catalyses the oxidation of Δ2, Δ3, and Δ4 -unsaturated aloohols to the copresponding ketones in good yields, where bromomesitylene or bromobenzene ie used as an oxidant.