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41.
Tatsuro Ouchi Toshio Banba Hiroshi Masuda Tatsuji Matsumoto Shigeo Suzuki Masuko Suzuki 《高分子科学杂志,A辑:纯化学与应用化学》2013,50(10):959-975
In order to provide a macromolecular prodrug of 5-fluorouracil (5FU) reducing the side effects, having an affinity for tumor cells, and exhibiting strong antitumor activity, the covalent attachments of 5FUs to chitosan and chitosamino-oligosaccharide (COS) through hexamethylene spacer groups via urea, urea bonds were carried out. The effect of prolongation of life was tested in vivo against p388 lyrnphocytic leukemia in female CDF, mice by intra-peritoneal (i.p.) transplantation/i.p. injection and the growth-inhibitory effect on Meth-A fibrosarcoma or MH-134Y heputoma was evaluated in vivo in SPF-C3H/He scl male or Balb/c male mice by subcutaneous (s.c.) implantation/intravenous (i.v.) injection. The effects of the degree of polymerization of chitosan and 相似文献
42.
This article reviews recent topics on the polymerization of substituted acetylenes, focusing on the synthesis of poly(diphenylacetylenes) and the living polymerization of phenylacetylenes. Diphenylacetylene (DPA) polymerizes with TaCls-n-Bu4Sn to give a polymer which is thermally very stable but insoluble in any solvents. DPAs with various groups (e.g.,p-Me3Si,m-Me3Ge, p-t-Bu,and_p-PhO) polymerize similarly. These polymers are soluble and their M¯w's reach 1 × 106 to 3 × 106. Some of them are more gas-permeable than poly(dimethylsiloxane). Several acetylenes (e.g., ClC -n-C6H13 and HCUC-t-Bu) have been found to undergo living polymerization with MoOCl4-n-Bu4Sn-EtOH. Whereas phenylacetylene (PA) does not polymerize in a living fashion, ortho-substituents in PA more or less suppress termination and chain transfer. PAs with bulky ortho groups (e.g., CF3 and Me3Ge) especially undergo virtually ideal living polymerization. 相似文献
43.
O. Takahashi Y. Masuda A. Muroya T. Furuya 《SAR and QSAR in environmental research》2013,24(5-6):547-558
In general, the docking scoring tends to have a size dependence related to the ranking of compounds. In this paper, we describe a novel method of parameter optimization for docking scores which reduce the size dependence and can efficiently discriminate active compounds from chemical databases. This method is based on a simplified theoretical model of docking scores which enables us to utilize large amounts of data of known active and inactive compounds for a particular target without requiring large computational resources or a complicated procedure. This method is useful for making scoring functions for the identification of novel scaffolds using the knowledge of active compounds for a particular target or a customized scoring function for an interesting family of drug targets. 相似文献
44.
Naoyuki Masuda Osamu Yamamoto Masahiro Fujii Tetsuro Ohgami Ayako Moritomo Toru Kontani 《合成通讯》2013,43(17):2305-2316
Various N‐3‐alkylated thiazolidenesulfonamide derivatives were efficiently prepared by the direct endo‐selective alkylation of thiazolylsulfonamides. The effects of different bases and solvents were investigated, and the NaH–THF combination was found to be the most effective at conferring high yields and endo‐selectivity. 相似文献
45.
Daisuke Saeki Takeshi Yamada Yasuko In Tetsuya Kajimoto Reiko Tanaka Yota Iizuka Takahisa Nakane Akihito Takano Kazuo Masuda 《Tetrahedron》2013,69(5):1583-1589
Novel 5 lupane-type of triterpenois, i.e., 3β-acetoxy-18α,19α-epoxylupan-21β-ol (1), 18α,19α-epoxy-21β-hydroxylupan-3-one (2), lup-18-ene-3,21-dione (3), lupa-18,21-dien-3β-yl acetate (4), and (17S)-17,18-seco-lup-19(21)-ene-3,18,22-trione (5), named officinatrione, as well as 16 known compounds from the roots of Taraxacum officinale collected in Takatsuki city, Osaka, Japan. Of the above compounds, 5 was the first lupane-type triterpene, of which the D-ring was open to form a nine-membered ring. Compounds 2 and 5 exhibited moderate cytotoxic activities against L1210 cell line (IC50 10.5 and 10.1 μM). 相似文献
46.
In this study, 8 new spirobenzopyrans were synthesized. A novel, three-step, facile route for the synthesis of 3′-allylindoline spirobenzopyrans via 3-allyl-3H-indoles was developed. The newly synthesized spirobenzopyrans were evaluated for their photochromic properties. The presence of an allyl moiety at the 3′ position did not disturb the photochromic response. The steric effects of the diallyl groups at the 3′ position affected the interconversion between colored and colorless forms. Therefore, the allyl chain in 3′-allylindoline spirobenzopyrans can be utilized to attach these compounds to a molecular matrix. Consequently, this synthetic methodology could be readily applied to the creation of new photo-switchable materials. 相似文献
47.
Herein reported is a photo-induced production of vicinal diols from alkenes under mild reaction conditions. The present dihydroxylation method using diacetyl (= butane-2,3-dione), oxygen, and water dispenses with toxic reagents and intractable waste generation. 相似文献
48.
Direct Asymmetric Mannich‐Type Reaction of α‐Isocyanoacetates with Ketimines using Cinchona Alkaloid/Copper(II) Catalysts 下载免费PDF全文
Masashi Hayashi Masaru Iwanaga Noriyuki Shiomi Dr. Daisuke Nakane Prof. Dr. Hideki Masuda Prof. Dr. Shuichi Nakamura 《Angewandte Chemie (International ed. in English)》2014,53(32):8411-8415
The enantioselective direct Mannich‐type reaction of ketimines with α‐isocyanoacetates has been developed. Excellent yields and enantioselectivity were observed for the reaction of various ketimines and α‐isocyanoacetates using cinchona alkaloid/Cu(OTf)2 and a base. Both enantiomers of the products could be obtained by using pseudoenantiomeric chiral catalysts. This process offers an efficient route for the synthesis of α,β‐diamino acids. 相似文献
49.
50.
Hirofusa Shirai Kenji Hanabusa Toshiki Koyama Hisanaga Tsuiki Etsuko Masuda 《Macromolecular Symposia》1992,59(1):155-162
The oxidation of HO-CH2-CH2-SH (RSH) by molecular oxygen and Fe(III)- as well as Co(II)-multicarboxyphthalocyanine and the mechanism in homogeneous aqueous system were investigated. As application to enzyme-like heterogeneous catalysts, Fe(III)-as well as Co(II)-octacarboxyphthalocyanine were supported on amorphous enriched rayon staple fiber and their enzyme-like activities were estimated. These fibers were applicated to new odor-removers acting as artificial enzyme systems. 相似文献