A series of novel hydrazide-hydrazone derivatives were synthesized and evaluated for their larvicidal and adult topical activity against Aedes aegypti. The proposed structures of all the synthesized compounds were confirmed using elemental analysis, UV, IR, 1 H-NMR, 13 C-NMR and mass spectroscopy. Compounds 4a-h were screened in larval bioassays at concentrations of 100, 50 and 25 ppm in a dose dependent manner and data for their mortality was recorded. Among the tested compounds, 1-(4-nitrophenyl)-3-(4-{2-oxo-2-[2-(2-oxo-1,2-dihydro-3H-ylidene)hydrazinyl] ethyl} phenyl)urea (4b) showed noteworthy larvacidal activity against Aedes aegypti. Dose-response data of compound 4b showed LC 50 and LC 90 values of 30.5 (15.4 -22.7) and 95.9 (73.8 -139.4) ppm, respectively. Screening of compounds 4a-h at four doses by topical bioassay indicated a range of activity between 10000 and 1000 ppm.

In this study, a series of hydrazide-hydrazone derivatives (3a-3u) were synthesized and evaluated for their anticancer activitiesagainst prostate cancer cell line (PC-3), breast cancer cell line (MCF-7), colon cancer cell line (HT-29) and human umbilical vein endothelial cells (HUVEC) using MTT assay. In particular, compound 3h having a pyrrole ring was found to be the most potent derivative with IC50 = 1.32, 2.99, 1.71 μM against PC-3, MCF-7, HT-29 cancer cell lines respectively using paclitaxel as a standard compound. Furthermore, compound 3h was subjected to further biological studies such as caspase-3 activity and Annexin-V assay to evaluate their inhibitory potentials. The activity results displayed that compound 3h increased caspase-3 activation and the number of cells to early apoptosis. The additional studies like pharmacokinetics, bioavailability scores and drug-likeness properties were also evaluated. The in silico pharmacokinetics predictions displayed that the bioavailability of these compounds may be high.

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