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Nilutamide (1) of the NO2 group can be converted to NH2 by addition of triethyl silane and Wilkinson's catalyst to give amino compound (2) via reduction. It is further treated with t_BuONO by TMSN3 in RB flask containing CH3CN to give 3-(4-(4-azido-3-(trifluoromethyl) phenyl)-5-5-dimmethylimidazolidine-2,4-dione (3). Azide furthermore reacted with different terminal alkynes in the presence of Sharpless catalyst to form 5,5-dimethyl-3-(4-(4-phenyl-1H-1,2,3-triazol-1-yl)-3-trifluoromethyl imidazolidine-2,4-diones(4a-4j) with favorable yields depicted (scheme-I) in this manuscript. All the compounds were screened for in vitro anti-cancer activity, among them compound 4h containing the 4-CN group showed highest anticancer activity PC3=-1.94±1.16µM and DU-145=1.54±0.32 and MCF-7=1.43±0.92 µM. Compound 4d NO2 group resulting compound 4d exhibited PC3 3.38±2.07 and DU-145 =3.58±1.57 µM. Compound 4C containing Ome group PC3=2.10±1.38, DU-145=1.57±0.32 and MCF-7=2.08±1.64 µM as IC50 in µM, Etoposide is used as a reference. [ABSTRACT FROM AUTHOR]

Synthesis of new series of chromen-2-one-1,2,3-Triazoles (6a-6j) was reported using the help of key methods such as [3+2]-cycloaddition and ultrasound. All compounds were further evaluated for their in vitro anticancer activity profile in three human cancer cell lines MCF-7(breast), A-549 (lungs), and HeLa (cervical). Among all, three compounds namely 6c, 6f, and 6j showed the most promising activity against three lines, when compared with the etoposide. [ABSTRACT FROM AUTHOR]

In this context, we describe the efficiency of this catalyst towards green organic synthesis has been studied by carrying out a mixture of 1-fluoro-4-isocyanobenzene (1), 6-aminonicotinic acid (2)and substituted 1H-indole-3-carbaldehyde (3a-i) in distilled water, porous Au/TiO2nanospheres were added at room temperature in H2O. It proceeds yielding the corresponding isubstituted-3-((4-fluorophenyl) amino)-2-(1H-indol-3-yl)imidazo [1,2-a]pyridine-6-carboxylic acid derivative in good to excellent yield viz one-pot multi-component reaction. All the title compounds were also screened for Anti- proliferation activity screened for their in vitro anticancer activity against four human cancer cell lines MCF-7, HeLa, HEK 293T and IMR 32. Among them 4a (having 4-OCH3 substituent) has shown promising activity with IC50 (µM) 16.74±1.86 (MCF-7), 40.68 ± 1.25(HeLa), 50.61±4.64 (HEK 293T) and 26.58±1.68 (IMR32) has shown IC50 (µM) and these results are close to that of standard drug Doxorubicin. [ABSTRACT FROM AUTHOR]

Herein, we depict the reaction subbed with a blending bar originate the alkyne (III) and azide was added CuSO4/sodium ascorbate of 1.2 eq K2CO3 and the response combination was mixed at RT for 16-18 h. After work up to bear the preferred 1-((1-aryl) - 1H-1,2,3-triazol-4-yl) methyl) quinoxalin-2(1H)- ones (IV a-IV j) item. This large number of mixtures were evaluated for their hostile to disease action against human malignant growth cell lines by means of MCF-7,A-549 and HeLa. In vitro against malignant growth movement uncovers that a couple of mixtures displayed strong inhibitory in an assortment of disease cell lines. Among them 1-((1-(2,4- dimethoxyphenyl)- 1H-1,2,3-triazol-4-yl)methyl)pyrido[2,3-b]pyrazin-2(1H)- one (IV j) with 2,4-OCH3C6H3 MCF- 7 (3.64 ± 0.92), HeLa (4.62 ± 0.29), A-549 (8.02 ± 0.94) promising enemy of multiply movement .1-((1-(4- nitrophenyl)- 1H-1,2,3-triazol-4-yl)methyl)pyrido[2,3-b]pyrazin-2(1H)- one(IVi) with p-NO2C6H4 MCF-7 (4.15 ± 1.02), HeLa (6.43 ± 1.67), A-549 (10.74 ± 1.88) potent.1-((1-(2,4-dichlorophenyl)- 1H-1,2,3-triazol-4- yl)methyl)pyrido[2,3-b]pyrazin-2(1H)- one (IV h) with 2,4-ClC6H3 MCF-7 (5.02 ± 1.38), HeLa (8.84 ± 2.01), A-549 (12.18 ± 2.82) great action. Etoposide utilized as a positive control. [ABSTRACT FROM AUTHOR]

Herein we described the synthesis of indazole derivatives through C-N cyclization and evaluated for their anticancer activities against three human cancer cell lines such as HeLa, MCF-7, and SKOV3 using MTT assay. The synthesized indazole hybrids are characterized based on 1H NMR, 13C NMR spectral data, and elemental analysis. The results indicated that the most potent molecule in this series is compound 3b against MCF-7, compound 3h against HeLa, and compound 3d against SKOV3, which showed the highest activity with an IC50 value of 32.92 μg/ml, 12.08 μg/ml, and 29.06 µg/ml respectively. [ABSTRACT FROM AUTHOR]