A library of imidazopyridine-propenone conjugates () were synthesized and evaluated for their antitumor activity against four human cancer cell lines, namely, prostate (DU-145), lung (A549), cervical (Hela) and breast (MCF-7) cancer cell lines. These conjugates showed good to moderate activity against the tested cell lines. Among them, two conjugates ( and ) showed significant antiproliferative activity against the human lung cancer cell line (A549) with IC values of 0.86 μM and 0.93 μM, respectively. Flow cytometry analysis revealed that these compounds arrested the cell cycle at the G/M phase in the human lung cancer cell line (A549), inhibiting tubulin polymerization leading to apoptosis. Further, Hoechst staining, decrease in mitochondrial membrane potential and Annexin V-FITC assay suggested that the cell death was due to apoptosis induction. Overall, the present investigation demonstrated that the synthesized imidazopyridine-propenone conjugates are promising tubulin inhibitors and apoptotic inducers.
The self emulsifying drug delivery system (SEDDS) is considered to be the novel technique for the delivery of lipophillic plant actives. The self emulsifying (SE) formulation significantly enhance the solubility and bioavailability of poorly aqueous soluble phytoconstituents. The self emulsifying drug delivery system (SEDDS) can be developed for such plant actives to enhance the oral bioavailability using different excipients (lipid, surfactant, co solvent etc.) and their concentration is selected on the basis of pre formulation studies like phase equilibrium studies, solvent capacity of oil for drug and mutual miscibility of excipients. The present review focuses mainly on the development of SEDDS and effect of excipients on oral bioavailability and aqueous solubility of poorly water soluble phytoconstituents/ derived products. A recent list of patents issued for self emulsifying herbal formulation has also been included. The research data for various self emulsifying herbal formulation and patents issued were reviewed using different databases such as PubMed, Google Scholar, Google patents, Scopus and Web of Science. In a nutshell, we can say that SEDDS was established as a novel drug delivery system for herbals and with the advances in this technique, lots of patents on herbal SEDDS can be translated into the commercial products.
A mild domino rearrangement strategy for the direct access to substituted quinoline‐4‐carboxamides has been developed. This copper‐catalyzed coupling reaction of O‐acyl oximes with isatins in the presence of molecular oxygen as the sole oxidizing agent proceeds through a ring expansion of the isatins through cleavage of the two C–N bonds.
An efficient one‐pot route for the construction of naphtho[1′,2′:4,5]imidazo[1,2‐a]pyridin‐5‐yl(aryl)methanones and 5‐phenylnaphtho[1′,2′:4,5]imidazo[1,2‐a]pyridines by sequential Sonogashira coupling reaction followed by trifluoroacetic acid promoted alkyne‐carbonyl metathesis (ACM) has been developed. 2‐(2‐Bromophenyl)imidazo[1,2‐a]pyridine‐3‐carbaldehyde preferentially underwent ACM with phenyl acetylenes, whereas intramolecular hydroarylation reaction was the common pathway in the absence of a carbonyl moiety at the C‐3 position under similar conditions. This protocol is compatible with a wide variety of functional groups and delivered corresponding naphtho[1′,2′:4,5]imidazo[1,2‐a]pyridines in good to excellent yields.
Bangham was first to develop these spherical-shaped nano-vesicles called liposomes in the early 1960s. Today, liposomes have emerged as crucial tools for bettering the delivery of drugs that majorly includes-antifungal drug, peptide hormones, enzymes, vaccines antimicrobial agents, drugs against cancer, and genetic materials. Following the different manufacturing practices and versatile properties liposomes can be categorized in various parameters of size, charge, poly-dispersity index, encapsulation efficiency, solubility properties, and lamellarity. Alteration in such parameters elevates the loading and bioavailability of a drug by giving more clear target specification, desired or controlled release. This bibliographic chapter provides a comprehensive overview of methods for the preparation of liposomes with other perspectives that majorly includes-physio-chemical characteristics, dosage regimen, advantages over other delivery systems, approved liposomal based drugs and other ongoing drugs in clinical trials. It will help researchers to breakthrough more structurally successful delivery vehicles depending upon their various physic-chemical properties.
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