Optimization of gefitinib analogues with potent anticancer activity
The interactions of gefitinib (Iressa) in EGFR are hydrogen bonding and van der Waals forces through quinazoline and aniline rings. However the morpholino group of gefitinib is poorly ordered due to its weak electron density. A series of novel piperazino analogues of gefitinib where morpholino group substituted with various piperazino groups were designed and synthesized. Most of them indicated significant anti-cancer activities against human cancer cell lines. In particular, compounds 52-54 showed excellent potency against cancer cells. Convergent synthetic approach has been developed for the synthesis of gefitinib intermediate which can lead to gefitinib as well as numerous analogues.
Langmuir-Blodgett film formation of succinic acid half-esters containing double long alkoxy chains
Two types of half-esters of succinic acid have been prepared. One contains a 1,2-dialkylated glyceryl group, while the other has a normal alkyl group as the hydrophobic group. The mono-molecular films of the half-esters developed at the air-water interface were evaluated by π-A curves. Multilayer Langmuir-Blodgett (L-B) films deposited on the substrate are discussed in terms of pinhole defects. Influences of the surface pressure on accumulation, the number of layers, and the chain length of the lipophilic group are analysed. The L-B film made from the double-chained homologues possessed fewer pinhole defects compared with that composed of the single-chained one.
Preparation and characteristics of silica-based packings for high-performance liquid chromatography modified with amino and carboxyl groups
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Nomura,Yamada,Tsunoda
p. 2509 - 2512
(2007/10/02)
A NOVEL PREPARATION OF HEMISUCCINATES
Hemisuccinates are prepared by condensation of succinic acid mono-2-(trimethylsilyl)ethyl ester with alcohols and subsequent aprotic removal of the protective group.
Pouzar, Vladimir,Drasar, Pavel,Cerny, Ivan,Havel, Miroslav
p. 501 - 507
(2007/10/02)
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