Anti-tumor substances

Sarkomycin, an anti-tumor substance produced by streptomyces, H. Umezawa, T. Takeuchi, K. Nitta, T. Yamamoto, and S. Yamaoka, J. Anti-biot A6(1953) 101. 

Natural and synthetic substances related to human health (anti-tumor substances, antibiotics, antihistamins, dioxines) 02PAC1959. 

Effects of Sesquiterpene Lactones on Seed Germination. Sesquiterpene lactones are common constituents of the Asteraceae but are also found in other angiosperm families and in certain liverworts (31,32). These highly bitter substances exhibit a wide spectrum of biological activities (J 3) which include cytotoxicity, anti-tumor, anti-microbial, insecticidal (34) and molluscicidal (35) properties. Furthermore, they are known causes for livestock poisoning and contact dermatitis in humans (33). Structure-activity relationship studies on sesquiterpene lactones have demonstrated that biological activity frequently depend on the presence of the cr... 

Enantiomerically pure trifluoromethyl- and trifluoroethylcyclopropylcarbi-nols 132 and derivatives (R=Ci 2 fluoroalkyl, alkyl, aryl) appeared useful as intermediates for enzyme inhibitors, physiological active substances and anti-tumoral agents, Eq. (53), [183]. 

Nishino, H. Okuyama, T. Takata, M. Shibata, S. Tokuda, H. Takayasu, J. Hasegawa, T. Nishino, A. Ueyama, H. Iwashima, A. Studies on the anti-tumor-promoting activity of naturally occurring substances IV. Pd-H [(+)anomalin, (- -)praeruptorin B], a seselin-type coumarin, inhibits the promotion of skin tumor formation by 12-O-tetradecanoyl-phorbol-13-acetate in 7,12-dimethylbenz[a]anthracene-initiated mice. Carcinogenesis (London), 1990, 11 1557-1561. 

The effect of adriamycin, an anti-tumor chemical, on cardiolipin (CL), a phospholipid specific to the inner mitochondrial membrane, was studied by ATR-IR spectroscopy. It was shown that in the very stable complex the structures of both adriamycin and cardiolipin are different from those of the pure substances (Goormaghtigh et al., 1987). 

This polyene cyclization is the first reported example that employs the /S -keto ester unit as initiator. Substances related to 3 exhibit anti-tumor properties. 

The ideal cytotoxic dmg is a small molecule that is stiU very potent. A promising class of cytotoxic agents is a group of radiomimetic substances called ene-diyenes these are secondary metaboHtes from Streptomyces that are minor groove DNA-binders and introduce double-strand breaks that may lead to apoptosis [112-114] (Fig. 1.8). Their anti-tumor potential has been investigated in a number of experimental studies [115-117]. 

Surh, Y.-J., Anti-tumor-promo ting activities of selected pungent phenolic substance present in ginger, J. Environ. Pathol. Toxicol. Oncol, 18, 131, 1999. 

C52H76O24, Mr 1085.16, yellow cryst., mp. 180-183 °C. A. belongs to the substance class of the chromomycins which exhibit anti-tumor activity. It is isolated from Streptomyces argillaceus and S. tana-shiensis. It cannot be used clinically on account of its toxicity. 

Unlike other biological agents, T2 is quite toxic when applied to unprotected skin. But like other biologically derived toxins, related substances have been investigated for possible medical uses, including the treatment of some cancerous tumors. A mycotoxin from Fusarium equiseti (diacetoxyscirpenol, or DAS) was considered for an anti-tumor drug formulation called Anguidine, but it was found to be far too toxic for therapeutic use. 

Currently, there has been no study of the secondary metabolites of Cephalochordata. Studies of Urochordata have been considerable but have focused on the class Ascidiacea (ascidians or sea squirts), which contain entire series of alkaloids, often with antiviral and anti-tumor properties. The ascidians share with sharks, which are primitive cartilaginous fish, the absence of liability to tumor development. In many species there is no epibio-sis, which often indicates the presence of cytotoxic and/or antibacterial substances, but antiviral substances were discovered among ascidians with epibionts (Eudistoma sp. and eudistomins (see below). 

With more than 350 original structures, almost all of which contain nitrogen, Didemnidae may be regarded as the richest family of the class Ascidiacea, with several molecules that are undergoing clinical trials for their antiviral and anti-tumor activity. Most of the structures isolated from Didemnidae derive from only three genera, Didemnum, Trididemnum and Lissoclinum, which each contain families of active substances (didemnins, eudis-tomins, lamellarins, lissoclinamides and Hssodimides). Table 28.3 shows the main types of structure encountered in the main genera of the order. 

A comprehensive website summarizing the status of tumor antiangiogenic compounds in various stages of clinical trial is maintained by the National Cancer Institute at www.cancer.gov/clinicaltrials/developments/ anti-angio-table. Following is a survey of the most important substances currently in clinical development. 

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