Synthesis of compound libraries and their concurrent assessment as selective reagents for probing and modulating biological function continues to be an active area of chemical biology. Microwave-assisted solid-phase Dötz benzannulation reactions have been used to inexpensively synthesize 2, 3-disubstituted-1, 4-naphthoquinone derivatives. Herein, we report the biological testing of a small libr...

Phagocytes mediate their innate immunological response by releasing products that damage invading microorganisms. These products include proteins such as lysozyme, peroxidases, and elastase as well as reactive oxygen species such as superoxide, hydrogen peroxide, hypohalous acid, and hydroxyl radical. Although it is clear that many phagocytic secretory products have direct cytotoxic potential, ...

Cytotoxic drugs have a lower therapeutic index than most other drugs. As cytotoxic drugs kill dividing cells, the normal tissues adversely affected by these drugs are those which are rapidly dividing: the bone marrow and the gastrointestinal tract. Some agents have other organ specific toxicities. Additionally, some drugs are associated with immediate adverse reactions which are a result of the...

Cardiotoxicity is an important side effect of cytotoxic drugs and may be a risk factor of long-term morbidity for both patients during therapy and also for staff exposed during the phases of manipulation of antiblastic drugs. The mechanism of cardiotoxicity studied in vitro and in vivo essentially concerns the formation of free radicals leading to oxidative stress, with apoptosis of cardiac cel...

cranesbill (geranium species) are used traditionally as tonic, antidiabetic, antidiarrheal, antihemorrhoidal, diuretic and for the treatment of cough, fever, tonsillitis, urticaria, kidney pain and gastrointestinal ailments. the leaves of some geranium species are consumed in traditional turkish cousin as salad or added to pastry. in the present study, different extracts from g. psilostemon and...

a series of 2-amino-4-aryl-3-cyano-7-(dimethylamino)-4 h -chromenes was synthesized by condensation of 3-(dimethylamino)phenol, an aromatic aldehyde and malonitrile in ethanol containing piperidine. the assignments of the structure of all synthesized compounds were based on spectral data (ir, mass and 1 h nmr). the cytotoxic activities of the synthesized compounds against six human tumor cell l...

Synthesis of biaryl-containing macrocycles has been carried out through a four-step approach comprising two Ugi four component reactions and a Suzuki-Miyaura macrocyclization. This protocol allowed the synthesis of 12- and 14-membered macrocycles. Cytotoxic activity evaluation showed that some of the molecules were effective against leukemia, glioblastoma and lung cancer cell lines (IC50 = 4.0,...

Toxic epidermal necrolysis is the most severe form of drug-induced skin reaction and includes denudation of >30% of total body surface area. The mechanism of disease is not completely understood, but immunologic mechanisms, cytotoxic reactions, and delayed hypersensitivity seem to be involved. We report a case of cephazolin-induced toxic epidermal necrolysis treated with intravenous immunoglobu...