Author
Roman L. Wydra
Other affiliations: University of Florida
Bio: Roman L. Wydra is an academic researcher from Georgia State University. The author has contributed to research in topics: Trifluoromethyl & Lithium. The author has an hindex of 15, co-authored 35 publications receiving 634 citations. Previous affiliations of Roman L. Wydra include University of Florida.
Topics: Trifluoromethyl, Lithium, Aniline, Addition reaction, Tautomer
Papers
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TL;DR: The results of the quantitative structure-activity relationship analyses, including several classical, linear regression correlations and a Free-Wilson approach of de novo model, provide guidelines for the design of new active compounds of this class.
Abstract: Thirty-eight 2-(aryl or heteroaryl)quinolin-4-amines, N,N-disubstituted, N-monosubstituted, and without a substituent at the amino group have been synthesized with use of novel chemistries developed by us recently. Some of these derivatives show anti-HIV-1 activity at a concentration level of 1 microM and low cell toxicity in vitro. The most active and least toxic compounds are derivatives of 2-(3-pyridyl)quinoline. The results of the quantitative structure-activity relationship analyses, including several classical, linear regression correlations and a Free-Wilson approach of de novo model, provide guidelines for the design of new active compounds of this class.
157 citations
46 citations
TL;DR: It is suggested that the amplifier‐induced conformational changes of the DNA helix increase affinity of the activated bleomycin complex toward the DNA minor groove and, consequently, result in an increased efficiency of theBleomycin‐mediated degradation of the helix.
Abstract: The bleomycin-mediated degradation of DNA is stimulated (amplified) by certain DNA binding compounds, such as polyamines, that distort the double helix. Computer modelling studies suggest that putrescine (1), spermidine (2), and spermine (3) bind preferentially on the floor of the major groove of (dGdC)5.(dGdC)5. This interaction results in a bend of the oligomer helix toward the major groove and enlargement of the minor groove, both effects being in the order 1 less than 2 less than 3. These polyamine-induced distortions, as obtained from theoretical studies, parallel the experimental values of the amplification activities of 1-3 in the bleomycin-mediated degradation of poly(dGdC).poly(dGdC). The amplification mechanism of non-competitive binding of amplifier molecules in the major groove, and bleomycin in the minor groove, is proposed. It is suggested that the amplifier-induced conformational changes of the DNA helix increase affinity of the activated bleomycin complex toward the DNA minor groove and, consequently, result in an increased efficiency of the bleomycin-mediated degradation of the helix.
45 citations
TL;DR: In this article, trifluoromethyl-substituted ketimines with strong bases are suggested intermediates in a novel synthetic route to 2-arylquinolines.
Abstract: 6-(Substituted methylene)-N-(aryl-alkylidene)-2,4-cyclohexadien-1-imines are suggested intermediates in a novel synthetic route to 2-arylquinolines based on the reaction of trifluoromethyl-substituted ketimines with strong bases
41 citations
TL;DR: In this article, a practical method for the preparation of 2-chloro-4,6-di(heteroaryl)pyrimidines and their 5-methyl homologues from readily available 2chloropyrimidine and 2chloro -5-methylpyrimidine, respectively, is described.
39 citations
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TL;DR: This review concludes that Etherification without Cyclization and N-Alkylation should be considered as separate science, and the proposed treatment of Etherification with Cyclization as a separate science should be reconsidered.
Abstract: 10. Patented Literature 2616 10.1. Esterification 2616 10.2. Ether Formation 2619 10.2.1. Etherification without Cyclization 2619 10.2.2. Etherification with Cyclization 2624 10.3. N-Alkylation 2625 10.4. Other Reactions 2627 11. Summary and Outlook 2628 12. Note Added in Proof 2628 13. Abbreviations Used in This Review 2629 14. Acknowledgments 2629 15. Supporting Information Available 2630 16. References 2630
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512 citations
TL;DR: Flies of the genus Anastrepha are among the world's most devastating agricultural pests, but at the same time, they display remark able ecological and behavioral characteristics, which have served as models in the development of general theories on insect mating systems and the physiology of host marking.
Abstract: Flies of the genus Anastrepha (Diptera: Tephritidae) are among the world's most devastating agricultural pests. At the same time, they display remark able ecological and behavioral characteristics, which have served as models in the development of general theories on insect mating systems and the physiology of host marking. Anastrepha species are endemic to the New World and restricted to tropical and sUbtropical environments. The genus's range extends from the southern US to northern Argentina and includes most of the Caribbean Islands. There are 184 described Anastrepha species. The great majority of these are poorly known biologically, and knowledge is basically restricted to seven economically important species: Jraterculus, grandis, ludens, obliqua, serpentina,
424 citations
398 citations