Four 2,6-di-tert-butyl-1,4-benzoquinone hydrazones have been synthesized viz. A1, A2, A3 and A4. The purity was checked using HPLC. These compounds were characterized by FTIR and H 1-NMR and they shows a prominent absorption of-(C=N-) in FTIR. It also shows a common peak of oleifinic proton at 6.50 Hz. These hydrazones were tested for their antimicrobial activity against Gram +ve and Gram-ve bacteria. A3 was found to be active at a minimum concentration of 50 μg•mL-1 where as A2 was inactive.

A new series of Schiff's bases, SB1, SB2 and SB3 were synthesized from 3-acetylcoumarin and different acid hydrazides. The 3-acetyl coumarin was synthesized starting from salicylaldehyde and ethylacetoacetate. The structures of the synthesized compounds have been established on the basis of physical and spectral data. They shows a prominent absorption of-(C=N-) in FTIR. A survey of existing literature revealed that there are no reports describing the synthesis of such hydrazones.

We report the synthesis, structural characterization and pharmaceutical activity of four coumarin-quinone hybrids. The compounds were significantly active against Staphylococcus aureus, Pseudomonas aeoginosa and Candida albicans. Promising antioxidant activity was observed when compared to ascorbic acid. Two compounds, DTBSB and DTBSN, also showed commendable in vitro antiproliferative activities against the cells of human cancer cell lines MCF-7, MDA-MB-231, COLO-205, HT-29 and A549 along with appreciable tumor selectivity with distinct selectivity index. Molecular docking studies using cyclooxygenase-2 (PDB ID: 6COX) revealed strong binding affinities for the COX-2 active site. Moreover, ADMET properties of the synthesized compounds were determined using the pKCSM and SwissADME online tools and all the compounds had accurate pharmacokinetic profiles. Hence, the new coumarin-quinone hybrids DTBSB and DTBSN can be considered for optimization and lead development.

Under solvent free conditions and in presence of a base 3-(2-(subsituted-(trifluoromethyl)phenylamino)acetyl)-2H-chromen-2-one derivatives were synthesized by grinding technique. Structural investigations were carried out with IR studies, HRMS, 1HNMR and 13CNMR. The compounds were checked for their in vitro anticancer activities against three different human cancer cell lines viz human breast cancer cell line (MCF-7), human cervical cancer cell line (HeLa) and human oral squamous cell carcinoma (SCC-40) using SRB method. All the title compounds showed low toxicity towards non-malignant PBMC cells indicating their tumour selectivity. The compounds exhibited good in vitro anti-proliferative potency at lower concentrations against HeLa and MCF-7 cell lines and remain moderately active against SCC-40.

3-acetylcoumarin hydrazone scaffolds, synthesized from 3-acetylcoumarin and substituted benzoic acid hydrazides are reported with structural characterization using IR, HRMS, 1H and 13C-NMR. The In vitro anticancer activities against three human cancer cell lines viz. MCF-7 (human breast cancer cell line), HeLa (human cervical cancer cell line) and SCC-40 (human oral squamous cell carcinoma) are carried out while the tumour selectivity of compounds are tested on the normal human peripheral blood mononuclear cells (PBMCs). The compounds 3ACOH, 3ACDH and 3ACMH exhibited higher sensitivity towards HeLa with GI50 values between 20.4 - 44.1μg/ml and this range of GI50 concentration of hydrazones showed no remarkable toxicity against normal PBMCs. Molecular docking studies revealed commendable binding interactions with cyclooxygenase enzyme (PDB ID 6COX). ADMET analysis shows the hydrazones are showing drug-likeness properties. The reported observations of 3-acetylcoumarin hydrazones suggest their possible role as promising new anticancer drug candidates.