Synthesis,characterization, and anti-cancer activity of chalcone derivatives as-potent anaplastic lymphoma kinase inhibitors

Structural Chemistry - Chalcone derivatives (7a–k) have been synthesized and characterized by 1H-NMR, 13C-NMR, mass, and elemental analysis. The synthesized compounds 7a, 7d, and 7g have been...     

A facile synthesis of novel 5‐substituted pyridine 2 carboxamide derivatives and their biological evaluation and 3D QSAR studies

A variety of novel 5‐substituted pyridine 2 carboxamides were designed and synthesized using both normal and solvent‐free microwave (MW) irradiation techniques. The results revealed that MW protocol proceeded smoothly under mild reaction conditions in short reaction times, thus avoiding the use of toxic organic solvents. Structural elucidation of the synthesized compounds was carried out on the basis of various spectroscopic methods, such as ¹H NMR, ¹³C NMR, LCMS, and IR. The synthesized compounds were evaluated for their in vitro antimicrobial activity (MIC) using the agar disk diffusion method. Among the various synthetic compounds, compound 3b showed higher potential activity against Escherichia coli than the other compounds. The order of activity against E. coli of the studied compounds is 3b > 3e > 3g > 3h > 3d > 3c > 3a > 3f . Additionally, 2D and 3D structural features of the synthesized derivatives were recognized by the 3D‐QSAR model. This validated model exhibited good internal (r², 0.924) and external prediction (r²pred, 0.851) correlation. The results of QSAR studies concluded that Alog P, the number of hydrogen bond acceptors, and the number of rotatable bonds were necessary features for the activity of the pyridine carboxamide derivatives.     

Cytotoxicity assessment of palbociclib-loaded chitosan-polypropylene glycol nano vehicles for cancer chemotherapy

The delivery of drugs in nanosized carriers arises as a very attractive solution. This study reports the in vitro cytotoxic effect of palbociclib loaded chitosan cross-linked polypropylene glycol nanocarriers. The nanocarriers were prepared by ion gelation using calcium chloride, calcium oxalate, and sodium tripolyphosphate as cross-linking agents. The influence of the cross-linking agent on the size and morphology of the chitosan- polypropylene glycol nanocarriers was studied by Dynamic Light Scattering (DLS), Scanning Electron Microscope (SEM), and Atomic Fluorescence Microscope (AFM). Tripolyphosphate assisted carriers was found higher amount palbociclib encapsulation capacity compared with other two carriers. The drug releasing behavior was studied at pH 6.8 which was based on the bulk erosion principal of the carriers. Palbociclib loaded chitosan-polypropylene glycol carriers were found to show excellent drug releasing kinetics and biocompatibility in in-vitro analysis. The unloaded chitosan-polypropylene glycol carrier was identified to have less inherent cytotoxicity, whereas the loaded carriers are as active as equal to pure palbociclib against the MCF-7 cancer cell line. The palbociclib loaded nanocarriers were studied to determine their potential anticancer activity against the MCF-7 cell line. The IC₅₀ values of three carriers chitosan-polypropylene glycol -I, chitosan-polypropylene glycol -II and chitosan-polypropylene glycol -III was observed 55.4, 51.0 and 38.7 mg/μL respectively. The effect of palbociclib uptake was evaluated by confocal microscopy using acridine orange/ethidium bromide and 4, 6-diamidino-2-phenylindole staining. Palbociclib loaded chitosan-polypropylene glycol nanocarriers show promise as potential candidates for cancer therapeutic applications.     

A novel and faster route for the synthesis of polyether-polycarbonate from carbon dioxide and epoxide through microwave irradiation

The purpose of this study was to investigate the utilization of CO₂ in order to obtain polyether-polycarbonate by the co-polymerization of epoxide with CO₂ using microwave irradiation. Double metal cyanide containing Zn with Co, Fe(II), Fe(III) and Ni has been utilized as a catalyst for the co-polymerization reaction. The effect of microwave power, catalyst amount and types of catalysts has been studied. The microwaves were found to be successful in the synthesis of polyether-polycarbonate in a shorter reaction time with higher turnover numbers than those in conventional methods.