Synthesis and biological activity of N-alkoxybenzenesulfonyl-5-halouracils

Kaldrikyan, M. A.; Geboyan, V. A.; Ter-Zakharyan, Yu. Z.; Paronikyan, R. V.; Garibdzhanyan, B. T.; Stepanyan, G. M.; Paronikyan, G. M.; Akopyan, L. G.

doi:10.1007/bf00757632

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“…Martirosyan et al [20] isolated 1-(p-toluenesulfonyl)uracil as an unwanted product in the transformation of C-4 keto group of uracil, and Kaldrikyn et al [21] examined the synthesis of 1-p-alkoxybenzenesulfonyl-5-bromouracil derivatives possessing antibacterial activity. According to Tada [22], benzoyl and arenylsulfonyl-5-fluorouracil derivatives are more active and less toxic than 1-(2-tetrahydrofuryl)uracil in the leukemia L/1210 system.…”

Section: Resultsmentioning

confidence: 99%

Atypical cytostatic mechanism of N-1-sulfonylcytosine derivatives determined by in vitro screening and computational analysis

et al. 2007

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We have previously shown that N-1-sulfonylpyrimidine derivatives have strong antiproliferative activity on human tumor cell lines, whereby 1-(p-toluenesulfonyl)cytosine showed good selectivity with regard to normal cells and was easily synthesized on a large scale. In the present work we have used an interdisciplinary approach to elucidate the compounds' mechanistic class. An augmented number of cell lines (11) has allowed a computational search for compounds with similar activity profiles and/or mechanistic class by integrating our data with the comprehensive DTP-NCI database. We applied supervised machine learning methodology (Random Forest classifier), which offers information complementary to unsupervised algorithms commonly used for analysis of cytostatic activity profiles, such as self-organizing maps. The computational results taken together with cell cycle perturbation and apoptosis analysis of the cell lines point to an unusual mechanism of cytostatic action, possibly a combination of nucleic acid antimetabolite activity and a novel molecular mechanism.

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Section: Resultsmentioning

confidence: 99%