Abstrakt

Choroby nowotworowe stanowią duże zagrożenie społeczne; w 2018 roku zdiagnozowano prawie 18 milionów nowych przypadków zachorowań na nowotwory. Wybór metody leczenia uzależniony jest od typu nowotworu, a także stopnia zaawansowania choroby w chwili diagnozy. W leczeniu wykorzystuje się przede wszystkim: metody chirurgiczne, radioterapię, immunoterapię, hormonoterapię i chemioterapię. Leki cytostatyczne mogą być stosowane zarówno w monoterapii, jak i w terapii skojarzonej. W latach 2009–2018 Amerykańska Agencja ds. Żywności i Leków (FDA) dopuściła prawie 356 nowych leków w terapii przeciwnowotworowej. Należy jednak zwrócić uwagę, że mimo coraz większej dostępności nowoczesnych leków, choroba ta jest drugą główną przyczyną zgonów na świecie. Badania nad opracowaniem preparatów cytotoksycznych mają na celu zaprojektowanie struktury związku, którego działanie ukierunkowane będzie na komórki nowotworowe przy jednoczesnym braku wpływu na komórki prawidłowe. Strukturę chemiczną o potencjalnym działaniu przeciwnowotworowym mogą tworzyć pochodne triazyny, które są stosowane w terapii onkologicznej już od 1965 roku. W zależności od umiejscowienia atomów azotu w pierścieniu wyróżnia się trzy izomery: [1,2,3]triazyny, [1,2,4]triazyny, [1,3,5]triazyny. Odpowiednia modyfikacja struktury [1,2,4]triazyny ma na celu zapewnienie znacznie silniejszych właściwości cytotoksycznych i ograniczenie działań niepożądanych w porównaniu do obecnie stosowanych leków. Projektowanie nowych preparatów ma także poprawić komfort życia pacjenta. W artykule pokrótce przedstawiono w jaki sposób modyfikacja struktury chemicznej pochodnych [1,2,4]triazyny wpływa na wzrost ich aktywności cytotoksycznej i dlaczego te związki mogą być lepiej tolerowane niż obecnie stosowana terapia.

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