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Synthesis, Characterization and Biological Evaluation of Novel (S,E)-11-[2-(Arylmethylene) Hydrazono] Pyrrolo [2,1-c] [1,4] Benzodiazepine DerivativesMingle, David 01 August 2019 (has links)
Pyrrolo [2,1-c] [1,4] benzodiazepine (PBD) is a class of natural products obtained from various actinomycetes which have both anti-tumor and antibiotic activities and can bind to specific sequences of DNA. PBD-dilactam was initially produced using isatoic anhydride and (L)-proline which was then converted to the PBD-thiolactam using Lawesson's reagent. Reaction of thiolactam with hydrazine in ethanol afforded PBD-11-hydrazinyl. Condensation of 11-hydrazinyl PBD with aldehydes possessing various substitutions was performed to obtain (S,E)-11-[2-(arylmethylene) hydrazono] pyrrolo [2,1-c] [1,4] benzodiazepine derivatives. 1HNMR, 13C-NMR, DEPT, IR, GC-MS and X-ray crystallography were used for the characterization. Inhibition activity of the products were carried out using TEM-1, AmpC and P99 β-lactamases. A minimal inhibition growth of 25% was observed for one of the selected PBDs on cancer cell line. A promising result was observed on preliminary cannabinoid binding activity test on one of the compounds.
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Synthèse et caractérisations de nouvelles sondes fluorescentes et réactifs chimiques pour l'étude structurale de l'ARN / Synthesis and characterization of new fluorescent probes and chemical reagents for structural analysis of RNABarhoum, Patrick 30 September 2013 (has links)
L’étude de la structure de l’ARN est reconnue un sujet d’actualité qui permet de connaître sa fonction. Il existe différentes techniques enzymatiques ou chimiques classiques et récentes couplées au séquençage à haut débit pour étudier la structure de l’ARN. Le projet de thèse vise l’optimisation de deux techniques de cartographie déjà existantes et se divise en deux parties. La première partie concerne l’optimisation de la technique de hSHAPE et ceci en synthétisant de nouvelles sondes fluorescentes à transfert d’énergie capables d’étudier de faibles quantités d’ARN et adaptées au séquenceur d’ADN. Mon travail a permis la synthèse de 5 molécules fluorescentes intermédiaires et l’obtention d’une sonde finale. L’étude de cette sonde a montrée que l’interaction entre les deux fluorophores est majoritairement due à un mécanisme de couplage excitonique causé par la flexibilité et la distance entre les deux entités fluorescentes. De plus, les propriétés de la molécule sont fortement dépendantes du solvant. Dans la deuxième partie, nous cherchons à optimiser la cartographie en solution afin d’étudier le génome entier du VIH-1 in virio. Pour cela, nous avons synthétisé 4 molécules dérivées de l’anhydride isatoïque et modifiées sur la fonction amine N1 par un groupement propyn-2-yle. Nous avons aussi préparé 8 molécules de référence. De plus, des études préliminaires réalisées sur l’ARN 1-311 du VIH-1 ont montré que nos composés modifient l’ARN et qu’il est possible de fixer la biotine-PEG3-azoture par click chemistry sur les ARN ainsi modifiés. / Understanding the function of RNA involved in biological processes requires a thorough knowledge of RNA structure. Traditional chemical and enzymatic reagents and backbonebased cleavage are useful for mapping RNA secondary structure, and on going advances in nucleotide resolution RNA structure probing have made possible increasingly rigorous and quantitative analysis. Although chemical and enzymatic probes are recently coupled to high throughput sequencing, these techniques still suffer from some disadvantages. This project aims the optimization of two existing techniques and is divided into two major topics. The first part aims the optimization of “hSHAPE chemistry”. A practical method is the synthesis of energy transfer dyes from the “BigDyes” family that are useful to study small amount of RNA and are compatible with DNA sequencing. We have done the synthesis of 5 modified dyes and one BigDye. The characterization of this BigDye shows that it exists excitoncoupling mechanism due to the strong interaction between the two transition dipoles. In addition, the solvent influences strongly the photophysical properties of this BigDye. The purpose of the second part is to develop and synthesize new class of isatoic anhydride derivatives useful to map the entire genome of HIV-1 in virio. We have done the synthesis of 4 N-substituted molecules with a propyn-2-yl function and 8 reference molecules. In addition, preliminary results on HIV-1 1-311 RNA showed that these compounds are able to modify RNA and that it is possible to fix a biotin-azide by click chemistry.
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