Search results for "2]oxazole"

showing 10 items of 12 documents

Transcriptome and computational analysis assess the anti-tubulin activity of [1,2]oxazole derivatives in lymphoma

2022

Cancer Researchanti-tubulinOncologylymphoma[12]oxazole

Pyrrolo[2',3':3,4]cyclohepta[1,2-d][1,2]oxazoles, a New Class of Antimitotic Agents Active against Multiple Malignant Cell Types

2020

A new class of pyrrolo[2',3':3,4]cyclohepta[1,2-d][1,2]oxazoles was synthesized for the treatment of hyperproliferative pathologies, including neoplasms. The new compounds were screened in the 60 human cancer cell lines of the NCI drug screen and showed potent activity with GI50 values reaching the nanomolar level, with mean graph midpoints of 0.08-0.41 μM. All compounds were further tested on six lymphoma cell lines, and eight showed potent growth inhibitory effects with IC50 values lower than 500 nM. Mechanism of action studies showed the ability of the new [1,2]oxazoles to arrest cells in the G2/M phase in a concentration dependent manner and to induce apoptosis through the mitochondrial…

CellsMitosisAntineoplastic AgentsApoptosisAntimitotic AgentsDrug Screening Assays[12]oxazoles antimitotic agents lymphoma tubulin polymerization inhibitorsDose-Response RelationshipStructure-Activity Relationshipchemistry.chemical_compoundModelsDrug DiscoverymedicineHumansStructure–activity relationshipColchicineOxazolesAntimitotic Agents; Antineoplastic Agents; Apoptosis; Cell Proliferation; Cells Cultured; Dose-Response Relationship Drug; Drug Screening Assays Antitumor; G2 Phase Cell Cycle Checkpoints; HeLa Cells; Humans; Mitosis; Models Molecular; Molecular Structure; Oxazoles; Structure-Activity RelationshipCell Proliferationchemistry.chemical_classificationReactive oxygen speciesCulturedMolecular StructureChemistryMolecularDepolarizationAntitumorMolecular biologyG2 Phase Cell Cycle CheckpointsMechanism of actionApoptosisCell cultureMolecular MedicineAntimitotic AgentDrugmedicine.symptomHeLa Cells

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CCDC 707421: Experimental Crystal Structure Determination

2009

Related Article: L.Kiss, M.Nonn, E.Forro, R.Sillanpaa, F.Fulop|2009|Tetrahedron Lett.|50|2605|doi:10.1016/j.tetlet.2009.03.119

Ethyl 4-(benzoylamino)-3-methyl-4566a-tetrahydro-3aH-cyclopenta[d][12]oxazole-5-carboxylateSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates

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Identification of pyrrolo[3',4':3,4]cyclohepta[1,2-d][1,2]oxazoles as promising new candidates for the treatment of lymphomas

2023

Unsatisfactory outcomes for relapsed/refractory lymphoma patients prompt continuing efforts to develop new therapeutic strategies. Our previous studies on pyrrole-based anti-lymphoma agents led us to synthesize a new series of twenty-six pyrrolo[3′,4':3,4]cyclohepta[1,2-d] [1,2]oxazole derivatives and study their antiproliferative effects against a panel of four non-Hodgkin lymphoma cell lines. Several candidates showed significant anti-proliferative effects, with IC50's reaching the sub-micromolar range in at least one cell line, with compound 3z demonstrating sub-micromolar growth inhibitory effects towards the entire panel. The VL51 cell line was the most sensitive, with an IC50 value of…

Pharmacology2-d][1Antitumor agentsLymphoma4’:3Organic ChemistryGeneral MedicineIsoxazolespyrrolo[3′2]oxazolesHematological malignanciesAntitumor agents; Hematological malignancies; Isoxazoles; Lymphoma; pyrrolo[3′4’:34]cyclohepta[12-d][12]oxazolespyrrolo[3′4’:34]cyclohepta[12-d][12]oxazoles4]cyclohepta[1Drug Discovery

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CCDC 1519195: Experimental Crystal Structure Determination

2017

Related Article: Y. Hernández, I.S. Marcos, N.M. Garrido, F. Sanz, D. Diez|2017|Acta Crystallogr.,Sect.E:Cryst.Commun.|73|85|doi:10.1107/S2056989016019952

Space GroupCrystallography2-(phenylsulfonyl)hexahydropyrrolo[12-b][12]oxazoleCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates

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CCDC 1898859: Experimental Crystal Structure Determination

2019

Related Article: Przemysław Woliński, Agnieszka Kącka-Zych, Błażej Dziuk, Krzysztof Ejsmont, Agnieszka Łapczuk-Krygier, Ewa Dresler|2019|J.Mol.Struct.|1192|27|doi:10.1016/j.molstruc.2019.04.061

Space GroupCrystallographyCrystal SystemCrystal Structure3a-nitro-2-phenyltetrahydro-2H-[12]oxazolo[23-b][12]oxazoleCell ParametersExperimental 3D Coordinates

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CCDC 1898860: Experimental Crystal Structure Determination

2019

Related Article: Przemysław Woliński, Agnieszka Kącka-Zych, Błażej Dziuk, Krzysztof Ejsmont, Agnieszka Łapczuk-Krygier, Ewa Dresler|2019|J.Mol.Struct.|1192|27|doi:10.1016/j.molstruc.2019.04.061

Space GroupCrystallographyCrystal SystemCrystal Structure3a-nitrotetrahydro-2H-[12]oxazolo[23-b][12]oxazole-2-carbonitrileCell ParametersExperimental 3D Coordinates

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CCDC 830704: Experimental Crystal Structure Determination

2016

Related Article: Hanene Jelizi, Nadia Wannassi, Mohamed El Baker Rammah, Kabula Ciamala, Michael Knorr, Yoann Rousselin, Marek M. Kubicki, Carsten Strohmann and Mironel Enescu|2014|J.Heterocycl.Chem.|51|383|doi:10.1002/jhet.1588

Space GroupCrystallographyCrystal SystemCrystal StructureCell Parameters3-(4-methoxyphenyl)-4-phenyl-8b-(pyrrolidin-1-yl)-48b-dihydro-3aH-indeno[21-d][12]oxazoleExperimental 3D Coordinates

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CCDC 1564490: Experimental Crystal Structure Determination

2017

Related Article: Fernando Rabasa-Alcañiz, Javier Torres, María Sánchez-Roselló, Tomás Tejero, Pedro Merino, Santos Fustero, Carlos del Pozo|2017|Adv.Synth.Catal.|359|3752|doi:10.1002/adsc.201700975

Space GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates3-methyl-5-(nitromethyl)-10b-(trifluoromethyl)-133a4510b-hexahydro-8H-[13]dioxolo[67]naphtho[21-c][12]oxazole

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CCDC 831070: Experimental Crystal Structure Determination

2014

Space GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates4-Methyl-3-(4-methylphenyl)-8b-(morpholin-4-yl)-48b-dihydro-3aH-indeno[21-d][12]oxazole

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