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With the upsurging cases of type II diabetic patients, the demand for safe and effective oral antidiabetic drugs is also increasing. Coordination complexes have proven their mettle as efficient oral drug candidates, which thereby motivated us in this work to design new transition metal complexes as plausible candidates for the treatment of diabetes. A reduced salen ligand, {H2(hpdbal)2‐an} (1) derived vanadium (IV) and iron (III) complexes, namely, [VIVO{(hpdbal)2‐an}] (2) and [{FeIII (OH2)((hpdbal)2‐an)}2 μ2‐SO4] (3) were synthesized in this study. The newly obtained ligand and complexes were characterized using usual analytical and spectroscopic techniques. The potential of these compounds in inducing increased glucose uptake by diabetic cells were studied by using insulin resistant HepG2 cells as model diabetic cells and 2‐NBDG molecule as a D‐glucose analogue and fluorescent tracker. The cells added with the vanadium (IV) complex 3 induced significant NBDG uptake of 95.4% which was higher than that induced by metformin, the standard antidiabetic drug. To elucidate the behavior of the complexes in biological media, model solution studies were conducted with a wide range of pH conditions and protein bovine serum albumin (BSA). The complexes demonstrated effective binding with BSA which was concluded through spectroscopic titration studies and were also found to be sufficiently stable over physiological pH conditions. The study can thus prove to be beneficial in the quest for new antidiabetic drugs.

In our continuing efforts to develop therapeutically active coumarin‐based compounds, a series of new C4–C4′ biscoumarin–pyrimidine conjugates (1a–l) was synthesized via SN2 reaction of substituted 4‐bromomethyl coumarin with thymine. All compounds were characterized using spectroscopic techniques, that is, attenuated total reflection infrared (ATR‐IR), CHN elemental analysis, and 1H and 13C NMR (nuclear magnetic resonance). In addition, the structure of compound 1d (1,3‐bis[(7‐chloro‐2‐oxo‐2H‐chromen‐4‐yl)methyl]‐5‐methylpyrimidine‐2,4(1H,3H)‐dione) was established through X‐ray crystallography. Compounds 1a–l were screened for in vitro anticancer activity against C6 rat glioma cells. Among the screened compounds, 1,3‐bis[(6‐chloro‐2‐oxo‐2H‐chromen‐4‐yl)methyl]‐5‐methylpyrimidine‐2,4(1H,3H)‐dione (1c) was identified as the best antiproliferative candidate, exhibiting an IC50 value of 4.85 μM. All the compounds (1a–l) were found to be nontoxic toward healthy human embryonic kidney cells (HEK293), indicating their selective nature. In addition, the most active compound (1c) displayed strong binding interactions with the drug carrier protein, human serum albumin, and exhibited good solution stability at biological pH conditions. Fluorescence, UV–visible spectrophotometry and molecular modeling methodologies were employed for studying the interaction mechanism of compound 1c with protein.