Synthesis and biological evaluation of deoxy-hematoxylin derivatives as a novel class of anti-HIV-1 agents.

SAR studies for the exploration a novel class of anti-human immunodeficiency virus type 1 (HIV-1) agents based on the hematoxylin structure (1) are described. The systematic deoxygenations of 1 including asymmetric synthesis were conducted to obtain a compound showing high potencies for inhibiting the nuclear import and viral replication as anti-HIV-1 agent. Among all, C-3-deoxygenated analog 16 exhibited most promising biological activities as anti-HIV-1 agent such as lower cytotoxicity (16:1; >80:40 µM), stronger inhibition of nuclear import (0.5:1.3 µM), and viral replication in HIV-1-infected TZM-bl cells (24.6:100 µM), human peripheral blood mononuclear cells (PMBCs) (30.1 µM: toxic). Different spectra of inhibitory activities against infected three healthy humans macrophages with high (donor A) and low (donor B and C) amounts of virus were also observed. Thus 16 showed 10-times stronger activity than 1 (16:1; 0.1:<1.0 µM) in the case of A, while 16 and 1 showed comparable activities in the cases of B and C (>0.01 and >0.00 1µM). The comparison of the inhibition of viral p24 antigen production was clearly indicated that compound 16 is at least twofold more potent anti-viral activity than 1. Thus, structures and actions of deoxy analogs particularly 16 could provide valuable information for the development of a novel class of anti-HIV-1 agents.

Diagnóstico del carcinoma escamoso de la mucosa bucal: reporte de 5 casos / Diagnosis of the squamous carcinoma of the bucal mucous: report of 5 cases

Es indudable que el cáncer bucal causa un importante número de muertes a nivel mundial. El cáncer invasivo puede permanecer largo tiempo bajo cambios macroscópicos inespecíficos, sólo la biopsia permite su diagnóstico. La técnica más utilizada es la rutina con hematoxilina - eosina, actualmente se agrega a la misma otras que contribuyen a clarificar el diagnóstico, por ejemplo la inmunohistoquímica, que en muchos casos determinará la estirpe de una neoplasia (AU)

It is certain that the cancer buccal cause an important number of deaths at world level. The cancer invasivo can remain long time low changes macroscopic unspecific, the biopsy only allows its diagnosis. The more used technique is the routine with hematoxylin - eosin, at the moment is added to the same others that contribute to clarify the diagnosis, for example the inmunohistoquímica that will determine the stock of a neoplasia in many cases (AU)