Synthesis and Characterization of Some Substituted 3, 4-dihydronaphthalene Derivatives through Different Enaminones as Potent Cytotoxic Agents

Abstract

A new series of novel substituted 3,4-dihydronaphthalene incorporated to benzo[h]quinoline, benzo[g]indazole, thiazolidin-4-one, pyrazolo[3,4-d]thiazol and thiazolo[4,5-b]pyridine ring systems were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. Some of the tested compounds exhibited promising carcinoma growth inhibition. The detailed synthesis, spectroscopic data and biological activities of the tested compounds were reported.

Inhibitory activity of benzo[h]quinoline and benzo[h]chromene in human glioblastoma cells

“…The combination of different ring systems in one compound is one of the major tools implemented in this study to produce more biologically active products in the field of drug development, aiming to obtain more active and less toxic products. Based on the above knowledge and in continuation of our previous work [17][18][19], the present study provides an evidence for the high efficient biological activity of the synthesized benzo[h]quinoline and benzo[h]chromene derivatives as anticancer compounds.…”

Novel Pyrazolines and Benzothiazepines as Tubulin Polymerization Inhibitors: Synthesis, Biological Evaluation, and Molecular Docking

“…[11][12][13] In addition, promising compounds D-F were synthesised to inhibit tubuline polymerization (Figure 2). [14][15][16] As a part of our research on bioactive heterocyclic and pharmaceutical compounds, [17][18][19][20][21] in this work, we developed anti-tubulin agents, based on chalcones as important precursors with novel backbone compounds for the synthesis of a variety of heterocyclic compounds using benzothiazepine and pyrazoline rings to act as linkers between essential rings based upon reported structures, in a trial to test a new ideas in both structural evolution and therapeutic approaches. .…”

Biological Validation of Novel Polysubstituted Pyrazole Candidates with in Vitro Anticancer Activities

“…On the other hand, compounds containing pyrazole derivatives represent an advantageous choice for the synthesis of compounds with a broad spectrum of pharmacological activities, including anti-inflammatory [13], antibacterial, antifungal [14], inhibition of cyclooxygenase-2 [15], antiangiogenic [16], antipyretic [17], antihypertensive [18], antiplatelet [19], nitric oxide synthase (NOS) inhibitors [20] and anticancer activities [21]. Based on these observations and in continuation of our research on biologically active heterocycles [22,23,24,25], it was of interest to incorporate the 1,2,4-polysubstituted pyrazole ring system into different heteroaryl ring systems in one molecule in an attempt to obtain a new target anticancer agents.…”