Refernces
10.1016/j.bmc.2016.12.010
The study focuses on the synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids, which are designed to inhibit tubulin polymerization and induce apoptosis in cancer cells. These compounds were synthesized by modifying the combretastatin pharmacophore, replacing ring B with benzothiazole scaffolds and incorporating triazole and tetrazole rings to restrict the cis configuration of the olefinic bond. The synthesized compounds were evaluated for their antiproliferative activity on selected cancer cell lines, and the structure-activity relationship was developed. The most potent compounds demonstrated effects comparable to combretastatin A-4 (CA-4), a known tubulin-binding ligand. The study aimed to develop new molecules with improved properties, such as better aqueous solubility and reduced toxicity, to target microtubules and disrupt cancer cell division. The chemicals used in the study include various substituted anilines, p-nitrobenzoylchlorides, Lawesson's reagent, and other reagents for the synthesis of the target compounds, as well as CA-4 as a reference compound for biological evaluation. The purpose of these chemicals was to create a series of novel tubulin inhibitors that could potentially be developed into anticancer drugs.
10.1007/BF00475641
The research investigates a method for synthesizing aryl- and heteroarylacetylenes using acyl derivatives of the Fischer base. The study aims to develop a convenient and efficient route for introducing an ethynyl group into organic compounds. The key chemicals used include 1,3,3-trimethyl-2-methylene-indoline (the Fischer base), various acylating agents (such as p-nitrobenzoyl chloride), phosphorus oxychloride, and aqueous alkali (e.g., NaOH or KOH). The method involves heating acyl derivatives of the Fischer base with phosphorus oxychloride to form indolenium salts, which are then treated with aqueous alkali to yield monosubstituted acetylenes and 1,3,3-trimethyl-2-oxindole. The researchers synthesized a series of aryl- and heteroarylacetylenes and demonstrated the versatility of the method by using various acyl groups from aliphatic, aromatic, and heterocyclic acids. The study concludes that this method is effective for synthesizing aryl- and heteroarylacetylenes, but not for alkylacetylenes, which tend to undergo resinification under the reaction conditions. The findings provide a valuable synthetic route for preparing acetylenes, which are important in the synthesis of various organic compounds, including dyes and thermochromic materials.
10.3184/174751912X13460810792101
The research focuses on developing a green and efficient method for the acylation of amines and phenols using hydrotalcite as a catalyst in water at room temperature. The study aimed to overcome the disadvantages of traditional methods, such as the use of toxic solvents and complicated reaction conditions, by following the principles of green chemistry. The experiments involved the reaction of various amines and phenols with carboxylic acid anhydrides and chlorides, using different amounts of water and catalyst to optimize the reaction conditions. The reactants included 4-methoxyaniline, 4-nitrobenzoyl chloride, and other substituted amines and phenols, along with acetylating agents like acetic anhydride and benzoic anhydride. The analyses used to characterize the products included Fourier-transform infrared spectroscopy (FT-IR), proton (1H) and carbon (13C) nuclear magnetic resonance (NMR) spectroscopy. The results showed that the method was effective, yielding moderate to high yields of amides and esters with good purity, and the catalyst could be reused without significant loss of activity.
10.1007/s10847-010-9813-5
The study presents the development of a new colorimetric anion sensor 1, synthesized using Fat Brown RR dye and a nitrophenyl group as signaling components, and an amide moiety as the binding site. The receptor 1 is designed to selectively recognize fluoride and acetate ions through color changes observable both via spectroscopic methods and to the naked eye. The receptor was synthesized by reacting Fat Brown RR with 4-nitrobenzoyl chloride, yielding a red solid in 76.3% yield. In DMSO, the receptor displayed strong absorption at 412 nm, which shifted upon addition of tetrabutylammonium fluoride, indicating complex formation. Excess fluoride ions led to deprotonation, evidenced by a new absorption band at 531 nm. Similar behavior was observed with acetate ions. The receptor did not bind to other anions like chloride, bromide, iodide, perchlorate, hydrogensulfate, or nitrate. The association constants for fluoride and acetate were determined through UV–vis and 1H NMR titrations, confirming the receptor's selectivity and efficiency as a naked-eye detector for these anions.