Chemotherapeutic activity

Davila J, Harriman A, Gulliya KS (1991) Photochemistry of merocyanine 540 The mechanism of chemotherapeutic activity with cyanine dyes. Photochem Photobiol 53 1-11... 

Herbicidal and chemotherapeutic activity have also been noted in other dihydropyrimidines. Certain 5,5-dihalo-6-methoxydihydropyrimidines, especially the 3-substituted derivatives such as (LXXXIll), are reported to have herbicide activity against many grasses and broad-leaf weeds [645] (herbicidal activity of some corresponding A -substituted uracils has been discussed in the preceding section). The compounds can generally be prepared by halogenation of uracil derivatives in alcohol [646, 647]. 

Commercial selenium disulfide SeSj has been found to be very untoxic (for mice LD 50 per os 3.7 g/kg). Thus the material is 100 times less toxic than selenites. Daily oral administration of 5, 25, or 125 mg/kg of SeS2 for seven and a half weeks was tolerated by mice without signs of intoxication. As SeSj is used as a constituent of shampoos several investigations on the effects of the sulfide on the eyes, skin, and hair have been published chemotherapeutic activity... 

Mendeleyev J, Kirsten E, Hakam A et al (1995) Potential chemotherapeutic activity of 4-iodo-3-nitrobenzamide metabolic reduction to the 3-nitroso derivative and induction of cell death in tumor cells in culture. Biochem Pharmacol 50 705-714... 

Levulinic acid is fairly easily converted into thiazole derivatives by the intermediate formation of an a-halogenated ketone such as the /3-bromo derivative (XL) or /3-chloro derivative, which reacts with thiourea to form 2-amino-4-methyl-5-thiazoleacetic acid (XLI) or with thioformamide to give 4-methyl-5-thiazoleacetic acid (XLII). The aminothiazole (XLI) and its ethyl ester (XLIII) have been converted into their corresponding sulfanilamide derivatives, (XLIV) and (XLV). These sulfanilamides, particularly the acid XLIV, have considerable chemotherapeutic activity moreover the acid possesses distinct solubility advantages over sulfathiazole itself. 

The commercial availability of basic pyridine derivatives has encouraged a tremendous amount of research into pharmaceutically active compounds. Two reviews in particular list a large number of medicinal compounds (B-80MI20900,77CZ389) based on the pyridine ring. Likewise, the occurrence of benzopyridine natural products with chemotherapeutic activity has stimulated the production of synthetic materials from aromatic amine precursors. Some important examples are presented below. 

Structures of cytotoxic compounds with potential cancer chemotherapeutic activity. 

In view of the high chemotherapeutic activity of Cinchona alkaloids, of which quinine is the most important as an antimalarial medicine, scientists of many countries have spent much time investigating syntheses of quinine and its analogs. 

Chemiluminescence, of firefly lanterns, 421 Chemotherapeutic activity, 152 Chichibabin reaction. 12 in synthesis of 2-aminothiazole. 12 a-Chloracetamide, with acetamidothiazoles. 

Potential, chemotherapeutic activity of this class of compounds stimulated the synthesis313,337,352 of a series of benzimidazole-, pyrimidine-, and purine-substituted nucleosides of D-glucuronic acid derivatives, using, as the starting sugar-component, bromide 1 and methyl (2,3,4-tri-0-acetyl-D-glucopyranosylamine)uronate, respectively. 

Surface active poly(ethylene glycol) ethers have been found to exert a aippressive effect on tuberculosis The greatest activity is observed wdien the number of ethylene oxide urtits is IS to 20 and the activity is completely abolished in those polymers where the number of imits ranges between 25 and 30. Conforth and coworkers have also found that when the number of ethylene oxide units was 45—70 the polymers, instead of displaying chemotherapeutic activity, significantly enhanced the infection, the so-caUed protuberculous effect. Thus, as the lipophflic to hydro-phflic ratio decreases, activity passes from antituberculosis to inactive protuberculous. These observations demonstrate the importance of two physical parameters in chemotherapy, namely surface activity and molecular size. 

Paul Ehrlich, the father of immunology and chemotherapy, discovered Salvarsan, an arsenical magic bullet (a favorite phrase of his) used to treat syphilis. He hypothesized at the beginning of this century that it might be possible to find a dye that would selectively stain, or dye, a bacterial cell and thus destroy it. In 19321.G. Farbenindustrie patented a new azo dye, Prontosil, which they put through routine testing for chemotherapeutic activity when it was noted it had particular affinity for protein fibers like silk. 

Miyakawa, S, Suzuki, K, Noto, T, Harada, Y, Okazaki, H, Thiolactomycin, a new antibiotic. IV. Biological properties and chemotherapeutic activity in mice, J. Antibiot., 35, 411-419,... 

The sulfonamides are a group of organic compounds with chemotherapeutic activity they are antimicrobial agents and not antibiotics. They have a common chemical nucleus that is closely related to PABA, an essential component in the folic acid pathway of nucleic acid synthesis. The sulfonamides are synergistic with the diaminopyrim-idines, which inhibit an essential step further along the folate pathway. The combination of a sulfonamide and a diaminopyrimidine is advantageous because it is relatively non-toxic to mammalian cells (less sulfonamide is administered) and is less likely to select for resistant bacteria. Only these so-called potentiated sulfonamides are used in equine medicine. These drugs are formulated in a ratio of one part diaminopyrimidine to five parts sulfonamide, but the optimal antimicrobial ratio at the tissue level is 1 20, which is achieved because the diaminopyrimidines are excreted more rapidly than the sulfonamides. 

Suifonamides (phthaiyisuifathiazoie [920], suifacetamide [921], suifaquinoxaiine [922], etc.) with chemotherapeutic activity are without exception 4-aminobenzene suifonamides (suifaniiamides). Their UV absorption is thus mainiy determined by the aromatic amino group. Suifaniiamides have one major band, usuaiiy at about 270 nm. 

Domagk s (7) discovery that Prontosil protected mice against lethal infections with streptococci and the findings of Foumeau and his group (8) that sulfanilamide was the chemotherapeutically active moiety of Prontosil initiated a... 

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