Anti-breast cancer activity of some novel 1,2-dihydropyridine, thiophene and thiazole derivatives

Novel quinolines carrying pyridine, thienopyridine, isoquinoline, thiazolidine, thiazole and thiophene moieties as potential anticancer agents

“…The ). The quinoline derivative carrying dihydrothiazole with 4-nitrophenyl and thioxo moiety (27), dihydrothiazole with 4fluorophenyl and thioxo moiety (25), tetrahydrobenzothiophene (34), dihydroisoquinoline with 4-methylphenyl and carbonitrile moiety (7), tetrahydro-4-H-cycloheptathiophene (35), dihydroisoquinoline with unsubstituted phenyl moiety (6), acrylamide moiety (21), dihydroisoquinoline with 2-chlorophenyl moiety (11), dihydroisoquinoline with 4-hydroxyphenyl moiety (8) with exhibited good cytotoxic activity better than doxorubicin as reference drug (IC 50 26.7 to 44.7 μmol L -1 ). A closer look into the structure activity relationship indicates that addition of dihydrothiazole with thioxo group at 2-position, 4-nitrophenyl at 3-position, free amino group at 4-position, dihydrothiazole with thioxo group at 2position, 4fluorophenyl at 3position, free amino group at 4position and tetrahydrobenzo[b]thiophene with free amino group at 2-position was proven to be successful in the case of compounds 27, 25 and 34, which showed an increase in activity.…”

“…It is well known that many 2-pyridone derivatives revealed diverse biological activities such as anticancer (19), cardiotonic (20), and potential HIV1 specific reverse transcriptase inhibiting (21). In view of the above mentioned findings and as a part of our research efforts to explore novel anticancer heterocyclic compounds (22)(23)(24)(25)(26)(27)(28), we have synthesized a new series of quinoline derivatives carrying a number of biologically active moieties as analogues to compounds I-V (Fig. 1).…”

“…It has been reported that designing a single molecule with more than one pharmacophore with different modes of action could be beneficial for the treatment of cancer (4), as well as for reducing unwanted side effects (5). Many quinolines, dihydropyridines, thienopyridines, isoquinolines, acrylamides, thiazolidines, thiazoles and thiophenes were found to possess antineoplastic activity (6)(7)(8)(9)(10)(11). Although the antineoplastic activity of these quinolines was attributed to intercalating binding to DNA, there were additional advantages of quinolines that interact with DNA, with a low association constant.…”

Study of reactivity of cyanoacetohydrazonoethyl-N-ethyl-N-methyl benzenesulfonamide: preparation of novel anticancer and antimicrobial active heterocyclic benzenesulfonamide derivatives and their molecular docking against dihydrofolate reductase

“…On the other hand, the presence of cyanoacetylhydrazono moiety (C¼NÀNÀC(O)ÀCH 2 ÀCN) in a structure, makes it a versatile and convenient intermediate for the synthesis of a wide variety of heterocyclic compounds. The b-functional nitrile [1][2][3][4] moiety of the molecule is a favorable unit for addition followed by cyclization or via cycloaddition with numerous reagents providing heterocyclic compounds of different ring sizes with one or several heteroatoms that are interesting as pharmaceuticals agents [24][25][26][27][28][29][30] . Considering this background, some novel heterocyclic sulfonamides as thiophenes 3, 4, 5 and 6, thiazole 7, chromenes 8 and 9, piperidine 10, pyrrolidine 11, tetrahydropyridine 12, pyridine 13, pyrazole 14 and hydrazono 15 derivatives were prepared and tested in terms of anticancer and antimicrobial activity with the purpose of revealing possible leading compounds for development of new anticancer and antimicrobial agents.…”

2-(2-(2-Hydroxybenzyliden) Hydrazinyl)-2-Oxo-N-(Pyridine-2-Yl) Acetamide Complexes: Synthesis, Characterization and Biological Studies

“…Hydrazones and their coordination compounds play important roles in treatment of different diseases. Hydrazones considered as an significant class of compounds with wide importance due to their various biological applications such as anticonvulsant, analgesic, anti-inflammatory, antidepressant, antimalarial, antiplatelet, antimycobacterial, antimicrobial, antiviral, anticancer, antidiabetic, vasodilator, anti-HIV, anthelmintic, and trypanocidal activities [6][7][8][9][10][11][12][13][14]. This work targets the synthesize and characterization Co(II) and Ni(II) complexes of 2-(2-(2-hydroxybenzyliden) hydrazinyl)-2-oxo-N-(pyridine-2-yl) acetamid (H 2 L).…”