- Synthesis, characterization and anticancer screening of some novel piperonyl-tetrazole derivatives
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A series of new 1,2-substituted tetrazole derivatives were synthesized and evaluated on MCF-7 (ER positive), MDA-MB-231 and ZR-75 (ER negative) breast cancer cell lines. Out of the fourteen compounds, three compounds 10, 12 and 14 showed higher inhibitory effects on MCF-7 cells. Whereas, compound 8 exhibited higher inhibition in MDA-MB-231 and ZR-75 cells at 10-5 M concentration. Total RNA was extracted and effect of compounds on different marker genes was studied. The gene expression of CD44, BRAC and BAX were significantly affected. The compounds were screened against the HepG2 cell line, to know if they are selectively targeting specific cancers and only 1-10 percent inhibition was found at 10-5 M concentration.
- Arshad, Mohammad,Bhat, Abdul Roouf,Pokharel, Smritee,Kim, Ji-Eun,Lee, Eun Ju,Athar, Fareeda,Choi, Inho
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- Facile one-pot preparation of 5-aryltetrazoles and 3-arylisoxazoles from aryl bromides
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The successive treatment of aryl bromides with n-BuLi, DMF, hydroxylamine hydrochloride, and finally diphenylphosphoryl azide provided efficiently the corresponding 5-aryltetrazoles in good to moderate yields. Similarly, the successive treatment of aryl bromides with n-BuLi, DMF, hydroxylamine hydrochloride, and finally diethyl acetylenedicarboxylate and Oxone provided efficiently the corresponding diethyl 3-arylisoxazole-4,5-dicarboxylates in good to moderate yields. Aromatic aldoximes are the key intermediates in both reactions, and 5-aryltetrazoles and 3-arylisoxazoles could be obtained from aryl bromides in one pot under transition-metal-free conditions.
- Kobayashi, Eiji,Togo, Hideo
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p. 4226 - 4235
(2018/07/06)
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- Discovery of bisamide-heterocycles as inhibitors of scavenger receptor BI (SR-BI)-mediated lipid uptake
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Abstract A new series of potent inhibitors of cellular lipid uptake from HDL particles mediated by scavenger receptor, class B, type I (SR-BI) was identified. The series was identified via a high-throughput screen of the National Institutes of Health Mole
- Dockendorff, Chris,Faloon, Patrick W.,Germain, Andrew,Yu, Miao,Youngsaye, Willmen,Nag, Partha P.,Bennion, Melissa,Penman, Marsha,Nieland, Thomas J.F.,Dandapani, Sivaraman,Perez, José R.,Munoz, Benito,Palmer, Michelle A.,Schreiber, Stuart L.,Krieger, Monty
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supporting information
p. 2594 - 2598
(2015/06/02)
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- NOVEL TETRAZOLO HYDRAZINE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER
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Provided are novel tetrazolo hydrazone derivatives or pharmaceutically acceptable salts thereof. The derivatives and the salts may inhibit the proliferation of cancer cells in a low molar concentration and inhibit the activity of cancer cells through the regulation of expression of apoptosis-related genes or the like, thus expressing excellent anti-cancer activity, and therefore, can be used effectively in preventing or treating cancer.
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- HETEROCYCLE-BISAMIDE INHIBITORS OF SCAVENGER RECEPTOR BL
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This appl ication describes compounds and methods that can inhibit Scavenger receptor class B, type I (SR-BI) activity, wh ich compounds and methods can be used, for example, to med iate h igh-density l ipoprotein (H DL) l ipid uptake and treat hepatitis C vira l infections. The compounds have the formu la : wherein R1 and R2 are independently H, halogen, cyano, haloalkyl, ha loa lkyloxy or OMe; or R1 and R2 together are -O-CH2-O- or -0- CF2-O-; R3 is H, ha logen, cyano, ha loalkyl or ha loa lkyloxy; R4 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylmethyl or C3-6cycloheteroalkyl, wherein the heteroatom is N or 0; R5 is H or CH3; R6 is C1-6alkyl or C3-6cycloalkyl; and A, B, D and E are each, independently, CH, N, 0 or S, wherein at least one of A, B, D and E is N, and another of A, B, D and E is N, 0 or S.
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Page/Page column 22; 43
(2014/05/07)
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- Rhodium-catalyzed olefination of aryl tetrazoles via direct C-H bond activation
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Rh(III)-catalyzed direct olefination reaction via aromatic C-H bond activation is described using tetrazole as the directing group. This reaction provides a straightforward way for the synthesis of ortho-alkenyl aryl tetrazoles. Various functional groups tolerate the reaction conditions and afford the corresponding products in moderate to excellent yields.
- Wang, Liang,Wu, Wenting,Chen, Qun,He, Mingyang
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supporting information
p. 7923 - 7926
(2015/01/09)
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- Ligand-free nano copper oxide catalyzed cyanation of aryl halides and sequential one-pot synthesis of 5-substituted-1H-tetrazoles
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An expedient and sequential one-pot synthesis of 5-substituted-1H- tetrazoles via [2+3] cycloaddition of aryl nitriles with sodium azide is reported. The required aryl nitriles were synthesized via the nano-copper oxide promoted cyanation of aryl iodides generated in situ.
- Yapuri, Umanadh,Palle, Sadanandam,Gudaparthi, Omprakash,Narahari, Srinivasa Reddy,Rawat, Dhwajbahadur K.,Mukkanti, Khagga,Vantikommu, Jyothi
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p. 4732 - 4734
(2013/08/23)
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- Probing the antiamoebic and cytotoxicity potency of novel tetrazole and triazine derivatives
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A series of compounds bearing a Tetrazole and Triazine ring motif conjugated with a SO2NH function were synthesized and investigated for their antiamoebic potency. Cytotoxicity of the compounds was checked on human hepatocellular carcinoma cell line HepG2. Incorporation of Triazine ring in place of tetrazole resulted in a precipitous increase in the antiamoebic activity of the compounds. Antiamoebic activity of the investigated compounds was found to be position and substituent dependent. In vitro cytotoxicity results revealed noncytotoxic nature of all the tested compounds up to a concentration of 25 μM. Compound 5c and 5d were obtained as least cytotoxic (IC50 > 100 μM) and excellent Entamoeba histolytica inhibitors with IC50 values of 1.05 μM and 1.02 μM respectively.
- Wani, Mohmmad Younus,Bhat, Abdul Roouf,Azam, Amir,Choi, Inho,Athar, Fareeda
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p. 313 - 320
(2012/03/27)
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- CuFe2O4 nanoparticles: A magnetically recoverable and reusable catalyst for the synthesis of 5-substituted 1H-tetrazoles
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An efficient and economical protocol for the synthesis of 5-substituted 1H-tetrazoles from various nitriles and sodium azide is described using magnetically recoverable and reusable CuFe2O4 nanoparticles. A wide variety of aryl nitriles underwent [2+3] cycloaddition under mild reaction conditions to afford tetrazoles in good to excellent yields. The catalyst was magnetically separated and reused five times without significant loss of catalytic activity.
- Sreedhar,Kumar, A. Suresh,Yada, Divya
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experimental part
p. 3565 - 3569
(2011/07/29)
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- 5-Aryltetrazole Compounds, compositions thereof, and uses therefor
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The present invention relates to 5-Aryltetrazole compounds, compositions comprising a 5-Aryltetrazole compound, and methods for treating an inflammation disease, a reperfusion disease, hyperuricemia, gout, or tumor-lysis syndrome in an animal in need ther
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