Design, synthesis and biological evaluation of pyrido[2,3-d] pyrimidine derivatives as potential anticancer agents
Background: CDK2 shows a fundamental role as a controller of cell growing, which makes it as one of the goals of anticancer inhibitors. Methods: The current study participated in design (docking and binding energy), which used to select the promising prop
Al-Otaibi, Jamelah S.,Ibrahim, Diaa A.,El Gogary, Tarek M.
p. 1240 - 1251
(2018/11/01)
Polycarbosilane-supported titanium(IV) catalyst for Knoevenagel condensation reaction
Polycarbosilane (PCS) was synthesized by the polycondensation of trichloromethylsilane and trimethoxyvinylsilane in the presence of sodium metal. PCS has a highly crosslinked structure, high ceramic yield and high surface area. Titanium metal ion was attached to the polycarbosilane and its catalytic activity was investigated. The Knoevenagel condensation reaction catalysed by titanium-incorporated polycarbosilane is reported. The titanium-incorporated PCS catalysed the reaction well and with a diverse set of substrates the reaction proceeded with good yield. PCS-supported transition metal catalysts have been prepared for the first time and used successfully in the Knoevenagel condensation reaction. Copyright
Mangala, Kunniyur,Sreekumar, Krishnapillai
p. 73 - 78
(2013/03/29)
Cosmetic composition
A composition suitable for topical application to mammalian skin and hair for inducing, maintaining or increasing hair growth comprises a hair growth promoter chosen from glutamine derivatives and salts thereof. The composition preferably also comprises an activity enhancer which may be chosen from hair growth stimulants, penetration enhancers and cationic polymers.
-
(2008/06/13)
Cosmetic composition containing DOPA derivatives
A composition for topical application to human hair or skin contains a chemical analogue of dihydroxyphenyl alanine (DOPA). This chemical analogue can be absorbed by skin or by a hair follicle and metabolised in-vivo, thus leading to the formation of melanin in skin or to the growth of melanin-pigmented hair. Consequently the composition can give controlled skin darkening to mimic sun-induced tanning or can bring about the growth of dar hair in place of the grey or white hair.
-
(2008/06/13)
Mechanistic and stereochemical study of phenylpyruvate tautomerase
A variety of substrates and potential enol/enolate mimics for the product/transition state of the enzyme phenylpyruvate tautomerase (E.C. 5.3.2.1) have been prepared and studied. Their stereostructures have been secured by a combination of NMR spectroscopy based on vicinal H-F and H-C coupling constants and X-ray crystallography. On the basis of the inhibition by stereoisomeric substituted cinnamates, it has been concluded that the enzyme produces the thermodynamically less stable (E) enol via a syn tautomerization transition state. Free energy profiles for the reaction suggest that vinyl fluorides act as product analogues. Because amide and dicarboxylate enolate mimics are relatively poor inhibitors of the enzyme, it is believed that an enolate is not involved in the tautomerization process.
Pirrung, Michael C.,Chen, Jrlung,Rowley, Elizabeth G.,McPhail, Andrew T.
p. 7103 - 7110
(2007/10/02)
Cosmestic composition
A composition suitable for topical application to mammalian skin and hair for inducing, maintaining or increasing hair growth comprises a hair growth promoter chosen from glutamic acid derivatives and salts thereof. The composition preferably also comprises an activity enhancer which may be chosen from hair growth stimulants, penetration enhancers and cationic polymers.
-
(2008/06/13)
Tyrphostins I: Synthesis and Biological Activity of Protein Tyrosine Kinase Inhibitors
A novel class of low molecular weight proteine kinase inhibitors is described.These compounds consitute a systematic series of molecules with a progressive increase in affinity toward the substrate site of the EGF receptor kinase domain.These competitive inhibitors also effectively block the EGF-dependent autophosphorylation of the receptor.The potent EGF receptor kinase blockers examined were found to competitively inhibit the homologous insulin receptor kinase at 102-103 higher inhibitor concentrations in spite of the significant homology between these protein tyrosine kinases.These results demonstrate the ability to synthesize selective tyrosine kinase inhibitors.The most potent EGF receptor kinase inhibitors also inhibit the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on EGF independent cell growth.These results demonstrate the potential use of protein tyrosine kinase inhibitors as selective antiproliferative agents for proliferative diseases caused by the hyperactivity of protein tyrosine kinases.We have suggested the name "tyrphostins" for this class of antiproliferative compounds which act as protein tyrosine kinase blockers.
Gazit, Aviv,Yaish, Pnina,Gilon, Chaim,Levitzki, Alexander
p. 2344 - 2352
(2007/10/02)
More Articles about upstream products of 17449-03-5