- 2′-Deoxy-2′-azidonucleoside analogs: synthesis and evaluation of antitumor and antimicrobial activity
-
Abstract: A series of ten pyrimidine nucleosides modified in 2′ position with azide or amine group was tested for the antibacterial, antifungal and cytotoxic activity. The cytotoxic effect was determined on three cancer (CCRF-CEM, MCF7, HeLa) and one norm
- Mieczkowski, Adam,Wińska, Patrycja,Kaczmarek, Marta,Mroczkowska, Magdalena,Garbicz, Damian,Pil?ys, Tomasz,Marcinkowski, Micha?,Piwowarski, Jan,Grzesiuk, El?bieta
-
-
Read Online
- Cu(I)-catalyzed efficient synthesis of 2'-triazolo-nucleoside conjugates
-
A small library of thirty-two 2'-triazolyl uridine and 2'-triazolyl-5-methyluridine has been synthesized by Cu(I)-catalyzed condensation of 2'-azido-2'-deoxyuridine and 2'-azido-2'-deoxy-5-methyluridine with different alkynes and aryl propargyl ethers in almost quantitative yields. Triazolo-nucleoside conjugates, which can be evaluated for different biological activity for suitable drug development, were unambiguously identified on the basis of 1H NMR, 13C NMR, IR, and HRMS data analysis. These compounds have been synthesized for the first time and have not been reported in the literature earlier.
- Mathur,Rana,Olsen,Parmar,Prasad
-
p. 701 - 710
(2015/05/13)
-
- Synthesis and evaluation of thymidine-5′-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase
-
A number of 2′- and 3′-modified thymidine 5′-O-monophosphate analogues were synthesized as potential leads for new anti-mycobacterial drugs. Evaluation of their affinity for Mycobacterium tuberculosis thymidine monophosphate kinase showed that a 2′-halogeno substituent and a 3′-azido function are the most favorable leads for further development of potent inhibitors of this enzyme.
- Vanheusden, Veerle,Munier-Lehmann, Helene,Pochet, Sylvie,Herdewijn, Piet,Van Calenbergh, Serge
-
p. 2695 - 2698
(2007/10/03)
-