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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]

The one step combination of an objective particle in a similar response vessel is generally viewed as an effective methodology in manufactured natural science. Several one step synthesis of biologically active molecules, primarily employing organo catalytic methods, is discussed in this overview, along with their strengths and weaknesses. The one step economy ideas presented here are not only applicable to catalysis but also to organometallic and organic reaction techniques in general. A synthesis that requires multiple steps could instead be carried out in a single reaction flask with a one step synthesis. Envision that a union including numerous means expects that you stir up the response at each step, then decontaminate and carry on the material to the following stage. During workup and/or purification, you will, of course, lose some materials regardless of how cautiously you move chemicals from flask to flask. As a result, I believe that the fact that it is less likely to lose material during workup and purification is the most significant advantage. The use of chemicals and solvents is cost-effective, which is the second benefit. If the reaction needs to be worked up at each step, you will almost always need to use solvents that will eventually go to waste. Multiple-step one-flask synthesis would only require final workup at the final step. [ABSTRACT FROM AUTHOR]

A mixture of 2-aminonicotinaldehyde 1 (0.01 mol), various acetonitrile 2a-f and in the presence of KOH with MW irradiation at 200 W intermittently at 30 sec for 2.0 min to furnish 3a-f and cooled further more mixture of HCl and were added NaNO2 solution were added and stirred at RT for 5 min to afford 4a-f.This is mixed with POCl3 was exposed to MW irradiation at 200 W intermittently at 30 sec intervals for 5 min. The reaction mixture was cooled and poured onto a mixture of crushed ice and NaHCO3. The solid thus obtained was filtered, washed with water and purified by recrystallization from ethanol to give 5a-f. To this hydrazine hydrate in ethanol was refluxed on a water bath for 0.5 hr. resulting solid product was filtered, washed with water and purified by recrystallization from ethanol to afford 6a-f shown in Scheme- I. The products were further confirmed by spectral analysis. [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]

The synthesis of some new isoxazole-piperidine-1,2,3-triazoles (4a-4j) have been achieved using Sharpless Cu(I) catalyzed [3+2] cycloaddition as a key approach. The in vitro anticancer screening of all the compounds against four human cancer cell lines including MCF-7, HeLa, A549 and IMR32 has revealed that the compounds 4c and 4f exhibited promising activity against all the cell lines as compared to etoposide. Rest of the compounds have shown good to zero activity against specific cell line when compared with the positive control. Predominantly, the compound 4c is showing superior activity against IMR32 which posses IC50 value 3.2±0.3μM. [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]

A concise and highly efficient procedure has been described for the synthesis of 9-aryl-6-(2-naphthyl)[1,2,4] triazolo[4,3-a][1,8]naphthyridines8 by the oxidation of the corresponding aryl aldehyde1-[3-(2-naphthyl) [1,8]naphthyridin-2-yl]hydrazones 7 using silica gel supported ferric chloride (SiO2-FeCl3) in solvent-free conditions under microwave irradiation. The desired products are obtained in very good yields and in a state of high purity. The structure of compounds 3-8 have been confirmed by their spectroscopic (IR, 1H NMR and MS) and analytical data. The compounds 8a-j have been screened for their antibacterial activity. [ABSTRACT FROM AUTHOR]

In this paper we would like to discuss the efficient synthesis of pyrazin fused N-(3-Mercapto-5-Aryl-[1,2,4]triazol-4-yl)-amide (5a-m and 6a-r) from4-Amino-5-Aryl-4H-[1,2,4]triazole-3-thiols(4a-b) through N-acylaton under dry dioxane, R1COCl, reflux, 10 h by a sequential manner probably the steps are mentioned in Scheme-1, Table-1,2. The structures of the compounds were elucidated by spectral (IR,1HNMR, 13CNMR and MS) analysis. The reactions are easy to conduct, under mild conditions, and form amide substituted triazole derivatives with excellent yields. [ABSTRACT FROM AUTHOR]