A total of 29 novel compounds bearing N1-(2-aryl-1, 3-thiazolidin-4-one)-N3-aryl ureas were designed, synthesized and evaluated for their biological activities. The structure-activity relationships (SARs) and binding modes of this series of compounds were clarified together. Compound 29b was ide...

To develop new anticancer drug candidates from 2-arylnaphthyridin-4-one (AN), we have designed and synthesized a series of 3′-hydroxy and 6-hydroxy derivatives of AN. The results of cytotoxicity screening indicated that the replacement of the 3′-methoxy moiety on the C-ring phenyl group of AN ...

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase responsible for development of various tumor types. In this study, we synthesized a series of novel 2,4-diarylaminopyrimidine derivatives possessing a unique N-(3-pyridinylmethyl)urea moiety as ALK inhibitors. The most promising anal...

Today, the problem of antimicrobial resistance is the most important cause of morbidity and mortality in the treatment of infectious diseases worldwide. Therefore, alternative treatment strategies are important for controlling infectious diseases. In the basic principle of antimicrobial photodyn...

In this study, the synthesis of non-ionic and ionic soluble axially disubstituted silicon phthalocyanines has been reported. Aggregation behavior of the silicon phthalocyanines was investigated in different solvents and concentrations. In all studied solvents and concentrations, silicon phthaloc...

In this study, the new 2-[2-(1H-naphtho[1,2-e][1,3]oxazin-2(3H)-yl)ethoxy]ethanol, 6-(1H-naphtho[1,2-e][1,3]oxazin-2(3H)-yl)hexan-1-ol have been synthesized. Then, novel axially naphthoxazin substituted two silicon(IV) phthalocyanines (SiPcs) have been synthesized and characterized. The aggregat...

Photodynamic therapy is one of the hot topics in cancer studies. Photosensitizing chemical substrates are stimulated by light having a specific wavelength to cause fatal effect on different kinds of targets.In this study, axially 4-{[(1E)-2-furylmethylene]amino}phenol, 4-{[(1E)-2-thienylmethylen...

A novel second generation benzyl ester dendrimer silicon phthalocyanine (D-SiPc) was synthesized and encapsulated into amphiphilic block copolymers to form polymeric nanoparticles ([email protected]). The cellular uptake and subcellular localization of [email protected] in U251 glioma cells were...

In this study, axially {4-[3-(9H-carbazol-9-yl)propoxy]phenyl}methoxy and ({3,5-bis[3-(9H-carbazol-9-yl)propoxy]phenyl}methoxy) substituted silicon phthalocyanines were synthesized by reaction of SiPcCl2 with {4-[3-(9H-carbazol-9-yl)propoxy]phenyl}methanol and {3,5-bis[3-(9H-carbazol-9-yl)propox...

Two bradykinin-related peptides (Protopolybiakinin-I and Protopolybiakinin-II) were isolated from the venom of the social wasp Protopolybia exigua by RP-HPLC, and sequenced by Edman degradation method. Peptide sequences of Protopolybiakinin-I and Protopolybiakinin-II were DKNKKPIRVGGRRPPGFTR-OH ...

This study describes the anti-inflammatory actions of NPC 18884, a non-peptide bradykinin B2 receptor antagonist in bradykinin and carrageenan-induced inflammation in the mouse model of pleurisy. The selectivity of NPC 18884 was assessed in the pleurisy caused by histamine, substance P and des-A...

A series of 2-(2,6-dihalophenyl)-3-(substituted pyrimidinyl)-1,3-thiazolidin-4-ones were designed on the prediction of quantitative structure–activity relationship (QSAR) studies, synthesized, and evaluated as HIV-1 reverse transcriptase inhibitors. Our attempts in correlating the identified mo...

A series of 2-oxo-3, 4-dihydropyrimido[4,5-d]-pyrimidinyl derivatives were designed and synthesized as new irreversible inhibitors of the FGFR family. One of the most promising compounds 2l potently inhibited FGFR1/2/3 with IC50 values of 1.06, 0.84 and 5.38 nM, respectively, whereas its potency...

Human Islet Amyloid Polypeptide or amylin is a neuroendocrine peptide with important endocrine and paracrine functions. Excessive production and accumulation of human amylin in the pancreas can lead to its aggregation and apoptosis of islet β-cells. Amylin has been shown to function within the ...

Nine phenolic acids were identified and quantified by HPLC–MS in leaves and 10 in seeds of kale (black cabbage). The free, ester (methanol-soluble), glycoside and ester-bound (methanol-insoluble) phenolic acid contents of the leaves were 487, 532, 4989 and 6402 ng/g fresh weight, respectively. ...

We report the synthesis of multivalent oleanolic acid (OA) protein conjugates as nonglycosylated neomucin mimic for the capture and entry inhibition of influenza viruses. Oleanolic acid derivatives bearing an amine-terminated linker were synthesized by esterification of carboxylic acid and furth...

The mechanism of the thermal polymerization (at 180°C) of glutamic acid, tyrosine, and glycine has been studied. Glutamic acid is quickly and almost completely converted into pyroglutamic acid. The only dipeptide that is formed by dimerization of the remaining two amino acids is cyclic glycyl-t...

A series of stable hemiaminals and Schiff bases containing 3,5-disubstituted 1,2,4-triazole derivatives were synthesized. The structure of the prepared compounds was confirmed by means of 1H NMR, 13C NMR, IR, MS and elemental analysis. The steric and electronic effects of the triazole ring subst...

Publisher SummaryThis chapter discusses the unusual DNA structures with known sequence dependencies such as bends, and the relatively new concept of sequence-directed structural softness or flexibility, and correlates these with protein structural motifs wherever possible. It shows that analyses...

A plant cDNA has been cloned that encodes a DNA-binding protein displaying a nucleotide (nt) sequence specificity similar to that of the mammalian cyclic AMP response element-binding protein/activating transcription factor (CREB/ATF) family of mammalian proteins. This cDNA was cloned in Escheric...