Purine Antagonists

A comparative trial of daunorubicin, cytosine arabinoside, and thioguanine, and a combination of the three agents for the treatment of acute myelocytic leukemia

“…1). This phase of the maintenance treatment was designed to test whether the different mechanisms of action of these antipurines [8] and the enhanced activity of the two drugs in combination observed with some experimental tumor lines in vitro [9] might lead to improved results in human A M L remission duration. tion was prescribed by protocol on the basis of bone marrow aspirate and peripheral blood count suppression.…”

The development of cytotoxic chemotherapeutics in the twentieth century

“…Hücrede DNA ve RNA'daki nükleotitlerin bileşenlerinden olan pü-rin ve primidin nükleobazlarının, proliferasyon için diğer hücreler gibi kanser hücreleri tarafından da sentezlenmeleri zorunlu olduğundan, kanser tedavisinde pürin ve primidin antagonistlerinden yararlanmak fikri mantıklı görünmüştür. [56,57] Bu doğrultuda "rasyonel dizayn" ile geliştirilen ilk kemoterapötiklerden, ilk antipürin olan merkaptopurin Amerikan Gıda ve İlaç Dairesi (FDA) tarafından 1953'te, ilk antiprimidin olan fluorourasil ise 1962'de onaylanmıştır. Bu ilaçlar, 1950'lerde hücre biyokimyasına dair sınırlı bilgi birikimi göz önünde bulundurulduğunda büyük birer adımdır; bugün hala çeşitli kanserlerin tedavisinde kullanıl-maktadırlar.…”

Biosynthesis

“…Duazomycin B, also named azotomycin (RAO, 1962) is a peptide composed of two moles of DON and one mole of aminoterminal yglutamic acid. The clinical usefulness of these antibiotics which act as glutamine antagonists in cancer chemotherapy has been reviewed (LEPAGE and Loo, 1973). The clinical usefulness of these antibiotics which act as glutamine antagonists in cancer chemotherapy has been reviewed (LEPAGE and Loo, 1973).…”