- New imidazo[2,1-: B] thiazole-based aryl hydrazones: Unravelling their synthesis and antiproliferative and apoptosis-inducing potential
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Herein, we have designed and synthesized new imidazo[2,1-b]thiazole-based aryl hydrazones (9a-w) and evaluated their anti-proliferative potential against a panel of human cancer cell lines. Among the synthesized compounds, 9i and 9m elicited promising cytotoxicity against the breast cancer cell line MDA-MB-231 with IC50 values of 1.65 and 1.12 μM, respectively. Cell cycle analysis revealed that 9i and 9m significantly arrest MDA-MB-231 cells in the G0/G1 phase. In addition, detailed biological studies such as annexin V-FITC/propidium iodide, DCFH-DA, JC-1 and DAPI staining assays revealed that 9i and 9m triggered apoptosis in MDA-MB-213 cells. Overall, the current work demonstrated the cytotoxicity and apoptosis-inducing potential of 9i and 9m in breast cancer cells and suggested that they could be explored as promising antiproliferative leads in the future. This journal is
- Babu, Bathini Nagendra,Devi, Ganthala Parimala,Kamal, Ahmed,Kumar, C. Ganesh,Rani Routhu, Sunitha,Shareef, Mohd Adil
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supporting information
p. 1178 - 1184
(2020/11/03)
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- Synthesis, crystal structure, antimicrobial activity and docking studies of new imidazothiazole derivatives
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A series of imidazothiazole derivatives were synthesized via Claisen–Schmidt condensation of aldehyde 3, and different methyl ketones and their chemical structures were confirmed using 13C NMR, 1H NMR and LC–MS. In addition, the mole
- Koudad,El Hamouti,Elaatiaoui,Dadou,Oussaid,Abrigach,Pilet,Benchat,Allali
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p. 297 - 306
(2019/09/03)
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- DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor
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The constitutive androstane receptor (CAR) is a xenobiotic sensor governing the transcription of genes involved in drug disposition, energy homeostasis, and cell proliferation. However, currently available human CAR (hCAR) agonists are nonselective, which
- Liang, Dongdong,Li, Linhao,Lynch, Caitlin,Diethelm-Varela, Benjamin,Xia, Menghang,Xue, Fengtian,Wang, Hongbing
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supporting information
p. 1039 - 1044
(2019/07/03)
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- Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies
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The DNA alkylating prodrug cyclophosphamide (CPA), alone or in combination with other agents, is one of the most commonly used anti-cancer agents. As a prodrug, CPA is activated by cytochrome P450 2B6 (CYP2B6), which is transcriptionally regulated by the
- Liang, Dongdong,Li, Linhao,Lynch, Caitlin,Mackowiak, Bryan,Hedrich, William D.,Ai, Yong,Yin, Yue,Heyward, Scott,Xia, Menghang,Wang, Hongbing,Xue, Fengtian
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- Synthesis of new triazole fused imidazo[2,1-b]thiazole hybrids with emphasis on Staphylococcus aureus virulence factors
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A series of new triazole fused imidazo[2,1-b]thiazole hybrids (9a–u) were designed, synthesized and evaluated as antimicrobial agents. Compounds 9c, 9d, 9e, 9j and 9l showed promising broad spectrum antimicrobial activity. Further, compound 9c exhibited s
- Shareef, Mohd Adil,Sirisha, Kanugala,Sayeed, Ibrahim Bin,Khan, Irfan,Ganapathi, Thipparapu,Akbar, Syed,Ganesh Kumar,Kamal, Ahmed,Nagendra Babu, Bathini
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supporting information
(2019/08/20)
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- Investigation on the effects of antimicrobial imidazo[2,1-b]Thiazole derivatives on the genitourinary microflora
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Background: Fused five-membered heterocyclic rings containing bridgehead nitrogen atom are particularly versatile in the field of medicinal chemistry because of their different biological activities. Among them, the imidazo[2,1-b]thiazole is an attractive
- Morigi, Rita,Vitali, Beatrice,Prata, Cecilia,Palomino, Rogers A. ?.,Graziadio, Alessandra,Locatelli, Alessandra,Rambald, Mirella,Leoni, Alberto
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p. 311 - 319
(2018/05/17)
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- CAR ACTIVATOR AGENTS FOR CYCLOPHOSPHAMIDE-BASED TREATMENTS OF CANCER
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The invention relates to selective small molecule human constitutive androstane receptor (hCAR) activators of Formula (I) or (II), pharmaceutical compositions thereof, and use thereof for the treatment of hematologic malignancies and other cancers. The sm
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Page/Page column 84; 85
(2019/01/10)
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