Cancer cytotoxics

The primary objective of a Phase I trial is to assess the safety of the drug in humans. Studies are normally conducted in healthy male volunteers, although specific categories of subject may be used in certain cases. For example, to avoid the risk of low blood pressure, subjects with mild hypertension would be more appropriate for the evaluation of antihypertensive drugs, while patients are likely to be used in the case of drugs that are expected to produce significant toxic effects (e.g. anti-cancer cytotoxic drugs). Remuneration may be offered for participation in the study. The number of subjects is normally between 10 and 100 people. 

Pt(terpy)(4-Me2Npy)]2+ and [Pt (4 -BrC6H4)terpy (4-Mepy)]2+ 275< many of these compounds were more effective than carboplatin for ovarian cancer cytotoxicity.275 ... 

Oxaliplatin Antitumor agent with activity against colorectal cancer cytotoxicity follows the formation of adducts with DNA. 

Cancer Cytotoxic on skin tumoral cell lines. ... 

Trivalent gold complexes were potentially attractive as anticancer agents because of their cytotoxic effects on established human tumor cell lines. All tested Au+ complexes substantially retained their antitumor potency against platinum-resistant tumor cell lines for leukemia and ovarian cancer. Cytotoxicity of these compounds in vitro is attributed to binding with DNA and modification and subsequent impairment of replication and transcription processes. The paucity of data on Au+ complexes probably derives from their high redox potential and relatively poor stability, which makes their use problematical under physiological conditions. 

Rodrigues et al. (149) reviewed the biological activities, as well as the structure and occurrence, of the sesquiterpene lactones. The biological activities discussed were anti-cancer, cytotoxic, antibiotic, chemophylaxis (against schistosomiasis), allergic contact dermatitis, antifeedants for insects, vertebrate poisons, and phytotoxins. The structural requirements for biological activity in these compounds were elucidated. Kuksis et al. (96) used GLC to study phytosterolemia. 

C. It is a cytotoxic agent used in the treatment of neoplastic disease, e.g. breast cancer. 

Gradual diminution of 004 T-lymphocytes from the peripheral blood is the most consistent feature observed in HIV infection. Because the majority of 004 cells are T-helper lymphocytes, removal leads to deficiency of cellular immunity, which depends on T-helper cells to initiate cytotoxic T-ceU killing of vims-infected cells of cancer. The loss of immune surveillance leads to the appearance of viraHy induced tumors from unopposed clonal expansion of viraHy transformed cells. Furthermore, depletion of cellular immunity leads to exaggerated viral, fungal, and proto2oal infections. 

A principal appHcation for photomedicine is the photodynamic treatment of cancer. Photochemical and clinical aspects of this topic have been reviewed (10,11). Direct irradiation of tumors coupled with adininistration of a sensitizer is used to effect necrosis of the malignancy. In this process, an excited state sensitizer interacts with dissolved in vivo to effect conversion of the oxygen from its triplet ground state to an excited singlet state, which is highly cytotoxic. In principle, excited sensitizers in either the singlet or the triplet state can effect this conversion of molecular oxygen (8). In... 

Approaches to cytotoxic chemotherapy iaclude special emphasis on dmg targeting and toxicity alleviation. The directions ia which new dmg discovery strategies are moving and the criteria used for advanciag compounds iato clinical trials (2) are discussed hereia, as are all of the dmgs approved by the United States Food and Dmg Administration (FDA) for the treatment of cancer as of this writing and those compounds ia clinical trials. 

Mucopolysaccharide levels are increased in many cancer cells this increase is accompanied by a decreased vascular supply. Hyaluronidase [9001-54-17, obtained from bovine testis, dissolves the mucopolysaccharides surrounding a tumor, thereby allowing cytotoxic agents to penetrate the neoplasm with enhanced faciUty. In clinical studies hyaluronidase was given to patients with malignant tumors, alone or in combination with 5- uorouracil [51-21-8], significant decreases in tumormass were observed (55). 

In vitro cytotoxicity assays using isolated cells have been applied intermittently to cyanobacterial toxicity testing over several years." Cells investigated for suitability in cyanobacterial toxin assays include primary liver cells (hepatocytes) isolated from rodents and fish, established permanent mammalian cell lines, including hepatocytes, fibroblasts and cancerous cells, and erythrocytes. Earlier work suggested that extracts from toxic cyanobacteria disrupted cells of established lines and erythrocytes," but studies with purified microcystins revealed no alterations in structure or ion transport in fibroblasts or erythrocytes,... 

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