Abstract Understanding chemical reactions in bacterial cellulose (BC) films is important to control the insertion of biomolecules that can improve their biomedical properties. Diphenyltetrazole molecules are able to react with tiols under UV irradiation and has been useful for immobilize proteins on different materials. In this work, we show the functionalization of a BC film with diphenyltetrazole and subsequent attempts of conjugation of the bovine serum albumin (BSA) to it. Diphenyltetrazole was synthesized in two steps, and functionalization of it with BC was carried out under ultrasound irradiation. Spectroscopic analysis of the film by UV–Vis and FTIR confirmed the success of the reaction. Attempts to conjugate BSA to the modified cellulose film by photoclick reaction failed under these conditions. Although this methodology is important in the conjugation of biomolecules, we understand that its application in cellulosic materials in heterogeneous phase is disadvantaged due to the half-life of the unstable intermediate and the biomolecule's access to it.

We report herein the synthesis of some beta-D-galactopyranosylamine and beta-lactosylamine amides and sulfonamides. The interactions of these compounds with lectins from the seeds of Erythrina cristagalli (LEC) and Ricinus communis (RCA120) were evaluated in a hemagglutination inhibitory activity assay. D-Galactose and lactose were used as reference compounds. The beta-lactosylamine amides and sulfonamides were nearly as active as lactose in inhibiting LEC mediated hemagglutination and were less active against RCA120 agglutinin. The beta-D-galactopyranosylamine amides and sulfonamides were, with one exception, considerably less active than D-galactose in the assay with both lectins.

O câncer é, atualmente, uma das principais causas de morte no mundo. A angiogênese, formação de novos vasos capilares a partir de células endoteliais, é essencial para vários processos fisiopatológicos, tais como o desenvolvimento e a disseminação dos tumores. As integrinas são uma família de receptores de superfície que estão envolvidos na angiogênese, na qual a integrina <FONT FACE=Symbol>anb</FONT>3 exerce papel importante. Os antagonistas da integrina <FONT FACE=Symbol>anb</FONT>3 têm efeitos diretos na prevenção do crescimento, angiogênese e metástase tumorais. A avaliação in vitro frente à integrina <FONT FACE=Symbol>anb</FONT>3 de coleções de ciclopeptídeos levou a compostos muito ativos e seletivos. Antagonistas não-peptídicos da integrina <FONT FACE=Symbol>anb</FONT>3 também foram planejados e sintetizados. A partir da determinação da estrutura tridimensional da integrina <FONT FACE=Symbol>anb</FONT>3 complexada com um inibidor, tornou-se possível o planejamento racional de ligantes com alta afinidade. Além disto, estes estudos permitiram a validação e o refinamento de modelo farmacofórico para os inibidores da integrina <FONT FACE=Symbol>anb</FONT>3.

Cancer is one of the leading causes of death. Angiogenesis, the growth of new blood vessels, is essential for tumor development and spreading. Integrins are a family of surface receptors that are involved in angiogenesis. The <FONT FACE=Symbol>anb</FONT>3 integrin plays an important role in tumor angiogenesis. <FONT FACE=Symbol>anb</FONT>3 inhibitors have direct effects to prevent tumor metastases, growth and angiogenesis. In vitro screening of cyclic peptide libraries led to highly active and <FONT FACE=Symbol>anb</FONT>3-selective compounds. Non-peptidic <FONT FACE=Symbol>anb</FONT>3 antagonists were also designed and synthesized. The crystal structure of the <FONT FACE=Symbol>anb</FONT>3 integrin in complex with RGD ligant allowed structure-based rational design of ligands and validation of pharmacophore model to <FONT FACE=Symbol>anb</FONT>3 antagonists.