3-deazauridine and Lung-Neoplasms

Cyclopentenylcytosine (CPE-C, 2), a pyrimidine analogue of the fermentation derived carbocyclic nucleoside neplanocin A, has been synthesized from the optically active cyclopentenylamine 3b by two synthetic routes. CPE-C demonstrates significant antitumor activity against both the sensitive and ara-C resistant lines of L1210 leukemia in vivo. Multiple long term survivors are produced in both tumor models. The compound also gives 100% growth inhibition of the solid human A549 lung and MX-1 mammary tumor xenografts grown in athymic mice. Good activity is also observed against a third human tumor xenograft model, metastatic LOX melanoma. CPE-C has significant activity against both DNA and RNA viruses in vitro. Potent activity is observed against HSV-1 (TK+ and TK-), HSV-2, vaccinia, cytomegalovirus, and varicella-zoster virus. Good activity is also found against a strain of influenza virus (Hong Kong flu), vesicular stomatitis virus, Japanese encephalitis virus, and Punta Toro virus.

Topics: 3-Deazauridine; Animals; Antineoplastic Agents; Antiviral Agents; Chemical Phenomena; Chemistry; Cytidine; DNA Viruses; Humans; Leukemia L1210; Leukemia P388; Lung Neoplasms; Mammary Neoplasms, Experimental; Melanoma; Mice; Mice, Nude; Neoplasm Transplantation; Neoplasms, Experimental; Orthomyxoviridae; RNA Viruses; Sarcoma, Experimental; Viruses