Design, synthesis of DNA-interactive 4-thiazolidinone-based indolo-/pyrroloazepinone conjugates as potential cytotoxic and topoisomerase I inhibitors

Synthesis, Characterization, Molecular Docking and in vitro Biological Studies of Thiazolidin‐4‐one Derivatives as Anti‐Breast‐Cancer Agents

“…[23,24] Finally, the imine group pf arylidenehydrazide derivatives was converted to thiazolidin-4-one derivatives using thioglycolic acid in toluene at 100 °C and thiazolidine-4-ones 5(a-h) were synthesized. [19] The study utilized a selection of aldehyde compounds including benzaldehyde, 4-chlorobenzaldehyde, 4methylbenzaldehyde, 4-methoxybenzaldehyde, 4-nitrobenzal-Scheme 1. Synthesis of the target compounds.…”

“…[11] Thiazolidin-4-one and its derivatives have a wide range of pharmacological activities such as anticancer [12][13][14][15][16][17] anti-inflammatory, analgesic, anticonvulsant, antimicrobial, local and spinal anesthetics, central nervous system stimulants, hypnotics, anti-HIV, antidiabetic, follicle-stimulating hormone receptor antagonist. [18][19][20][21][22] The aim of this study is to develop new and effective anticancer agents through the synthesis of thiazolidin-4-one derivatives of 4-furfuryloxy-benzohydrazide. To achieve this, 16 new compounds were synthesized and their cytotoxic effects were tested in vitro against both MCF7 human breast cancer cells and MCF10A human healthy breast tissue.…”

“…Thiazolidin‐4‐one and its derivatives have a wide range of pharmacological activities such as anticancer [12–17] anti‐inflammatory, analgesic, anticonvulsant, antimicrobial, local and spinal anesthetics, central nervous system stimulants, hypnotics, anti‐HIV, antidiabetic, follicle‐stimulating hormone receptor antagonist [18–22] …”

Design, synthesis andin vitrocytotoxicity evaluation of indolo–pyrazoles grafted with thiazolidinone as tubulin polymerization inhibitors

“…1). 24 In our consistent efforts in the development of molecular leads towards cancer chemotherapy, 25 herein, we report the thiazolidinone-grafted indolo-pyrazole conjugates as cytotoxic agents. These molecules adjoin two different pharmacophores, and may thereby help in achieving synergetic potency toward cancer therapeutics.…”

Design, Synthesis, and Antifungal Activities of Novel Pyrazole-4-carboxamide Derivatives Containing an Ether Group as Potential Succinate Dehydrogenase Inhibitors

“…Incorporation of two or more pharmacophores of bioactive scaffolds based on molecular hybridization has been one of the most successful strategies for the discovery of new pesticides and drugs. − For example, flubeneteram, a novel commercial SDHI fungicide approved recently (Figure ), was discovered through pharmacophore-linked fragment virtual screening (PFVS) by the Yang group, − which could be considered as a combination of pyrazole-4-carboxamide and diphenyl ether bioactive scaffolds based on the molecular hybridization strategy. Scaffold hopping, another widely exploited design approach, offers the opportunity to modify known lead compounds to afford novel structures with high potency, low toxicity, and enhanced physicochemical properties. − In this work, in search of novel SDHIs, flubeneteram was used as lead compounds, and we attempted to replace the diphenyl ether scaffold of flubeneteram with extended phenyl diether and aliphatic ether by scaffold hopping (Figure ).…”