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This work demonstrates the optimization of an efficient, mild, and environmentally friendly synthetic approach to access a diverse library of N-naphthoyl thioureas. These derivatives could be exploited as precursor scaffolds for designing valuable heterocycles with anticipated biological activities. Additionally, the utilization of a copper complex derived from the newly synthesized N-naphthoyl thiourea ligand in the photodegradation of methyl orange (MO) dye was explored. The antiproliferative effect of the synthesized derivatives was examined against MCF-7, HCT116, and A549 cancer cell lines. Most of the assembled derivatives revealed a significant cytotoxic effect, in some cases, greater than doxorubicin. Of these, the copper complex demonstrated significant antitumor activities (IC50 < 1.3 μM) and lesser cytotoxic impact (IC50 > 76 μM), indicating its possibility as a pioneering candidate for future carcinogenic pharmaceutics. Relations between the structure and activity also have been addressed.

I N this present work, synthesized a novel derivatives of bis-chalcones via condensation of 1,4-diacetylbenzene with different aldehydes in basic media. The reaction of chalcone derivatives 3a,b with thioglycolic acid gave compounds 4a,b. That was reacted with ethyl cyanoacetate in presence of ammonium acetate to give the corresponding cyanopyridine derivatives 5a,b. Furthermore, bis-chalcone 3a,b was cyclization to pyrazole analogs by using 2,4-dinitrophenylhydrazine to give compounds 7a,b in good yields. All products were characterized by IR spectrum, 1 HNMR, 13 CNMR, and elemental analysis. The new compounds have been screened as anti-bacterial activity

A new series of hydroquinolines derivatives (1, 2) have been achieved by the cyclo condensation of 2 (4-methoxybenzylidenemalonitrile), aniline and dimedone in the presence of piperidene. Cyclization of 5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7,7-dimethyl-5-oxo-2-(phenylamino) quinoline-3-carbonitrile (2) sulphuric acid at room temperature afforded 7,8-dihydro-4-(4methoxyphenyl)-7,7-dimethylquinolin-5(6H)-one[2,3-b]2,3-dihydroquinolin-4 (1H)-one (3). Several substituted pyrimido [4,5-b]quinoline derivatives (4, 5, 6 and 7) were synthesized from 2-amino-1,4,5,6,7,8-hexahydro-4-(4-methoxphenyl)-7,7,-dimethyl-5-oxo-1-phenylquinoline-3carbonitrile (1) via cyclization with thiourea, chloroacetyl chloride, phenyl isothiocynate and formamide, respectively. The condensation of dimedone, with 4-methoxybenzylidene malononitrile in the presence of trimethylamine afforded 11-amino-3,4,8,9-tetrahydro-12-(4-methoxyphenyl)-3,3,8,8-tetramethyl-2H-chromeno [2,3-b]quinoline-1, 10(7H,12H)-dione (8) but in ammonium acetate afforded 7,8-dihydro-4-(4-methoxyphenyl)-7,7-dimethylquinolin-5(1H,4H,6H)-one[2,3-b]4-amino-7,8dihydro-7,7-dimethylquinolin-5(6H)-one (9). The structures of the synthesized compounds were elucidated by elemental analyses and spectral data.

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The present work is mainly dedicated to heterocyclic compounds as well as S-glycoside. 1,4dihydroquinoxaline derivatives 3 were obtained from the reaction 2 with carbon disulfide in presence of potassium hydroxide. S-glycoside 4 was prepared from the reaction of compound 3 with 2,3,4,6-tetra-O-acetyl-α-D-glucopyranosyl bromide. Several heterocyclic derivatives containing thioxobenzo[g]pteridine ring systems were obtained starting from ethyl 3-amino-1,4dihydroquinoxaline-2-carboxylate 1. These newly synthesized compounds were docked within the active site of cyclooxygenase-2 (COX-2). The results of this docking study revealed that the new compounds might exhibit good anti-inflammatory activity. The structure of new compounds was demonstrated by elemental analysis, IR, 1 H NMR spectra and mass spectra.

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