This project has been designed to study the molecular basis of action of the benzophenanthridinum alkaloid of known antitumor activity, fagaronine and nitidine. A series of analogues has been synthesized to determine the active centre of these molecules in order to correlate the biological effect with the molecular structure. In view of our success in the design and synthesis of a potentially useful antitumor agent, based on the structural features present in known drugs displaying this property, we plan to continue and expand our research program directed towards the synthesis of new NBQ, fagaronine, and nitidine analogues. This will provide the basis for the design of more effective antitumor drugs. In our studies we have found that fagaronine and related analogues interfere with the DNA template function as a direct consequence of the intercalation process to double-stranded DNA. NBQ, the most active of these analogues, has been shown to induce differentiation of HL-60 promyelocytic leukemia at lower-than-chemotherapeutic doses. Our findings with NBQ as differentiation inducer raises the question: By what mechanism(s) does this drug expresses its differentiation effect? The understanding of how much of the biologic activity of these drugs can be attributed to cytocydal effect in contrast to differentiation induction will give us an insight of a potentially new mode of cancer chemotherapy.
| Ramírez-Camejo, Luis A; Maldonado-Morales, Génesis; Bayman, Paul (2017) Differential Microbial Diversity in Drosophila melanogaster: Are Fruit Flies Potential Vectors of Opportunistic Pathogens? Int J Microbiol 2017:8526385 |
| Morales-Rivera, Keyla F; Piñero Cruz, Dalice M; Prieto, Jose A (2017) Crystal structure of (-)-(S)-4-[(2S,3S,4S,Z)-3-hydroxy-4-methyl-hept-5-en-2-yl]-1,3-dioxolan-2-one. Acta Crystallogr E Crystallogr Commun 73:1070-1072 |
| García-Arriaga, Marilyn; Acosta-Santiago, Maxier; Cruz, Antony et al. (2017) Probing the Limits of Supramolecular G-Quadruplexes Using Atomistic Molecular Dynamics Simulations. Inorganica Chim Acta 468:209-222 |
| Huang, Qing; Quiñones, Edwin (2016) A spectroscopic method to determine the activity of the restriction endonuclease EcoRV that involves a single reaction. Anal Biochem 497:103-5 |
| Mège, Pascal; Schizas, Nikolaos V; Reyes, Joselyd García et al. (2015) Genetic seascape of the threatened Caribbean elkhorn coral, Acropora palmata, on the Puerto Rico Shelf. Mar Ecol (Berl) 36:195-209 |
| Morales-Rivera, Amarilys; Hernández-Burgos, Mayté M; Martínez-Rivera, Arlene et al. (2014) Anxiolytic effects of oxytocin in cue-induced cocaine seeking behavior in rats. Psychopharmacology (Berl) 231:4145-55 |
| Ramírez-Camejo, Luis A; Torres-Ocampo, Ana P; Agosto-Rivera, José L et al. (2014) An opportunistic human pathogen on the fly: strains of Aspergillus flavus vary in virulence in Drosophila melanogaster. Med Mycol 52:211-9 |
| Galindo-Cardona, Alberto; Acevedo-Gonzalez, Jenny P; Rivera-Marchand, Bert et al. (2013) Genetic structure of the gentle Africanized honey bee population (gAHB) in Puerto Rico. BMC Genet 14:65 |
| Santiago-Rodriguez, Tasha M; Rivera, Jessica I; Coradin, Mariel et al. (2013) Antibiotic-resistance and virulence genes in Enterococcus isolated from tropical recreational waters. J Water Health 11:387-96 |
| Pantoja-Feliciano, Ida Gisela; Clemente, Jose C; Costello, Elizabeth K et al. (2013) Biphasic assembly of the murine intestinal microbiota during early development. ISME J 7:1112-5 |
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