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Specialty: Chemistry
Drug: Temodar
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Total 46 results found since Jan 2013.
Cocrystallization of lenvatinib and temozolomide to improve the performance in terms of stability, dissolution, and tabletability
CrystEngComm, 2023, Advance Article DOI: 10.1039/D3CE00473B, PaperZhi-Qing Wang, Xia-Lin Dai, Dai-Lin Gu, Chao Wu, Tong-Bu Lu, Xiang-Tian Long, Jia-Mei Chen Cocrystallization of two anti-melanoma drugs, lenvatinib and temozolomide, resulted in two drug –drug cocrystal solvates presenting improved performance in terms of stability, dissolution, and tabletability, which show great potential to be developed as a drug combination. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry
Source: RSC - CrystEngComm latest articles - July 7, 2023 Category: Chemistry Authors: Zhi-Qing Wang Source Type: research
Cocrystallization of lenvatinib and temozolomide to improve the performance in stability, dissolution, and tabletability
CrystEngComm, 2023, Accepted Manuscript DOI: 10.1039/D3CE00473B, PaperZhi-Qing Wang, Xia-Lin Dai, Dai-Lin Gu, Chao Wu, Tongbu Lu, Xiangtian Long, Jia-Mei Chen Two anti-melanoma drugs, lenvatinib and temozolomide, were cocrystallized to obtain two drug-drug cocrystal solvates, TMZ-LEN ·MeOH (1:1:1) and TMZ-LEN·EtOH (1:1:1). They were fully characterized by XRD and thermal analyses, NMR and... The content of this RSS Feed (c) The Royal Society of Chemistry
Source: RSC - CrystEngComm latest articles - June 21, 2023 Category: Chemistry Authors: Zhi-Qing Wang Source Type: research
A Click Chemistry-Based Artificial Metallo-Nuclease
Angew Chem Int Ed Engl. 2023 Jun 20:e202305759. doi: 10.1002/anie.202305759. Online ahead of print.ABSTRACTArtificial metallonucleases (AMNs) are promising DNA damaging drug candidates. Here, we demonstrate how the 1,2,3-triazole linker produced by the copper-catalysed azide-alkyne cycloaddition (CuAAC) reaction can be directed to build copper-binding AMN scaffolds. We selected biologically inert reaction partners tri-azidomethyl-mesitylene and ethynyl-thiophene to develop TC-Thio, a bioactive C3-symmetric ligand in which three thiophene-triazole moieties are positioned around a central mesitylene core. The ligand was char...
Source: Angewandte Chemie - June 20, 2023 Category: Chemistry Authors: Alex Gibney Raphael E F de Paiva Vandana Singh Robert Fox Damien Thompson Joseph Hennessy Creina Slator Christine McKenzie Pegah Johansson Vickie McKee Fredrik Westerlund Andrew Kellett Source Type: research
Discovery of new imidazotetrazinones with potential to overcome tumor resistance
We describe the design, organic synthesis, and characterization, including X-ray crystallography, of a series of novel analogues of the clinically used antitumor agent temozolomide, together with their in vitro biological evaluation. The work has resulted in the discovery of a new series of anticancer imidazotetrazines that offer the potential to overcome the resistance mounted by tumors against temozolomide. The rationally designed compounds that incorporate a propargyl alkylating moiety and a thiazole ring as isosteric replacement for a carboxamide, are readily synthesized (gram-scale), exhibit defined solid-state struct...
Source: European Journal of Medicinal Chemistry - June 1, 2023 Category: Chemistry Authors: Helen S Summers William Lewis Huw E L Williams Tracey D Bradshaw Christopher J Moody Malcolm F G Stevens Source Type: research
Scaffold hopping of N-benzyl-3,4,5-trimethoxyaniline: 5,6,7-Trimethoxyflavan derivatives as novel potential anticancer agents modulating hippo signaling pathway
Eur J Med Chem. 2023 Apr 26;256:115421. doi: 10.1016/j.ejmech.2023.115421. Online ahead of print.ABSTRACTScaffold hopping of N-benzyl-3,4,5-trimethoxyaniline afforded 5,6,7-trimethoxyflavan derivatives that were efficiently synthesized in four linear steps. As lung cancer is the most lethal cancer, twenty-three synthesized compounds were evaluated against a panel of lung cancer cells. Amongst, compounds 8q and 8e showed interesting activity. Hence, compounds 8q and 8e were evaluated against panels of diverse cancers. Compounds 8q and 8e showed broad spectrum anticancer activity. However, compound 8q was more effective and,...
Source: European Journal of Medicinal Chemistry - May 10, 2023 Category: Chemistry Authors: Ahmed H E Hassan Cai Yi Wang Hyo Jong Lee Su Jin Jung Yeon Ju Kim Soo Bin Cho Chae Hyeon Lee Gyeongpyo Ham Taegeun Oh Sang Kook Lee Yong Sup Lee Source Type: research
Molecules, Vol. 28, Pages 3809: Acetogenins-Rich Fractions of Annona coriacea Suppress Human Glioblastoma Viability and Migration by Regulating Necroptosis and MMP-2 Activity In Vitro
. M. A. Ribeiro
Glioblastoma (GBM) is an incurable primary brain tumor with a poor prognosis. Resection, radiation therapy, and temozolomide (TMZ) are insufficient to increase survival, making the treatment limited. Thus, the search for more effective and specific treatments is essential, making plants a promising source for elucidating new anti-glioblastoma compounds. Accordingly, this study investigated the effects of four fractions of hexane and ethyl acetate extract of Annona coriacea Mart., enriched with acetogenins, against GBM cell lines. All four fractions were selectively cytotoxic to GBM cells when compared t...
Source: Molecules - April 29, 2023 Category: Chemistry Authors: Lorena R. Sousa Ana Gabriela S. Oliveira Ant ônio Arantes Jo ão Gabriel M. Junqueira Gerso P. Alexandre Vanessa G. P. Severino Rui Manuel Reis Bonglee Kim Rosy I. M. A. Ribeiro Tags: Article Source Type: research
Oxazolo5,4-fquinoxaline-type selective inhibitors of glycogen synthase kinase-3 α (GSK-3α): Development and impact on temozolomide treatment of glioblastoma cells
Bioorg Chem. 2023 Mar 4;134:106456. doi: 10.1016/j.bioorg.2023.106456. Online ahead of print.ABSTRACTThe 2-(3-pyridyl)oxazolo[5,4-f]quinoxalines CD-07 and FL-291 are ATP-competitive GSK-3 kinase inhibitors. Here, we investigated the impact of FL-291 on neuroblastoma cell viability and showed that treatment at 10 μM (i.e. ∼500 times the IC50 against the GSK-3 isoforms) has no significant effect on the viability of NSC-34 motoneuron-like cells. A study performed on primary neurons (non-cancer cells) led to similar results. The structures co-crystallized with GSK-3β revealed similar binding modes for FL-291 and CD-07, wit...
Source: Bioorganic Chemistry - March 13, 2023 Category: Chemistry Authors: Mohamed Hasyeoui Fr édéric Lassagne William Erb Manal Nael Khaled M Elokely Apirat Chaikuad Stefan Knapp Adrian Jorda Soraya L Vall és Emie Quissac Ma ïté Verreault Thomas Robert St éphane Bach Ali Samarat Florence Mongin Source Type: research
Locally Implantable Nanofibre Meshes by Sustained Release of Temozolomide for Combined Thermo-chemotherapy to Treat Glioblastoma
New J. Chem., 2023, Accepted Manuscript DOI: 10.1039/D3NJ00534H, PaperEmiho Oe, Nanami Fujisawa, Lili Chen, Koichiro Uto, Yoshitaka Matsumoto, Mitsuhiro Ebara Glioblastoma (GBM) is a highly malignant brain tumour that arises from astrocytes or supportive brain tissue in adults. Although there are several therapeutic options, recurrence rates remain high with a... The content of this RSS Feed (c) The Royal Society of Chemistry
Source: RSC - New J. Chem. latest articles - February 21, 2023 Category: Chemistry Authors: Emiho Oe Source Type: research
Molecules, Vol. 28, Pages 1394: Bio-Prospecting of Crude Leaf Extracts from Thirteen Plants of Brazilian Cerrado Biome on Human Glioma Cell Lines
Conclusion: These findings highlight M. chamissois chloroform partition as a promising component and may guide the search for the development of additional new anticancer therapies.
Source: Molecules - February 1, 2023 Category: Chemistry Authors: Silva Rosa Gomes Vital Alves Evangelista Longato Carloni Oliveira Pinto Rom ão Rezende Ara újo Oliveira Souza Oliveira Ribeiro Reis Tags: Article Source Type: research
Multilevel Pharmacological Effects of Antipsychotics in Potential Glioblastoma Treatment
Curr Top Med Chem. 2023 Jan 2. doi: 10.2174/1568026623666230102095836. Online ahead of print.ABSTRACTGlioblastoma Multiforme (GBM) is a debilitating type of brain cancer with a high mortality rate. Despite current treatment options such as surgery, radiotherapy, and the use of temozolomide and bevacizumab, it is considered incurable. Various methods, such as drug repositioning, have been used to increase the number of available treatments. Drug repositioning is the use of FDA-approved drugs to treat other diseases. This is possible because the drugs used for this purpose have polypharmacological effects. This means that th...
Source: Current Topics in Medicinal Chemistry - January 2, 2023 Category: Chemistry Authors: Wireko Andrew Awuah Jacob Kalmanovich Aashna Mehta Helen Huang Toufik Abdul-Rahman Jyi Cheng Ng Rohan Yarlagadda Karl Kamanousa Mrinmoy Kundu Esther Patience Nansubuga Mohammad Mehedi Hasan Mykola Lyndin Arda Isik Vladyslav Sikora Athanasios Alexiou Source Type: research
Calixarene Derivatives: A Mini-Review on their Synthesis and Demands in Nanosensors and Biomedical Fields
Mini Rev Med Chem. 2022 Sep 28. doi: 10.2174/1389557522666220928120727. Online ahead of print.ABSTRACTNanotechnology has been widely studied in biomedical applications in the last decade. The revolution in nanotechnology triggers the fabrication of nanomaterials with novel properties and functionalities, making the research in nanosensors and biomedical rapidly expanding. Nanosensors application has improved the sensitivity by enhancing their catalytic activity, conductivity, and biocompatibility. Calixarene is excellent as a sensing element used as a sensor due to its unique host-guest properties. Three major types of cal...
Source: Mini Reviews in Medicinal Chemistry - September 29, 2022 Category: Chemistry Authors: Nur Farah Nadia Abd Karim Faridah Lisa Supian Mazlina Musa Shahrul Kadri Ayop Mohd Syahriman Mohd Azmi Muhammad Dain Yazid Wong Yeong Yi Source Type: research
