39618-23-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel benzo[b]thiophene-diaryl urea derivatives as potential anticancer agents
Zarei, Omid,Azimian, Fereshteh,Hamzeh-Mivehroud, Maryam,Shahbazi Mojarrad, Javid,Hemmati, Salar,Dastmalchi, Siavoush
, p. 1438 - 1448 (2020/05/28)
A hybrid pharmacophore approach was applied to design and synthesize a series of benzo[b]thiophene-diaryl urea derivatives 17a–g with potential anticancer effect. In vitro antiproliferative activities of all target compounds were evaluated against HT-29 a
Synthesis and biological evaluation of diaryl urea derivatives designed as potential anticarcinoma agents using de novo structure-based lead optimization approach
Azimian, Fereshteh,Dastmalchi, Siavoush,Hamzeh-Mivehroud, Maryam,Hemmati, Salar,Shahbazi Mojarrad, Javid
, (2020/07/13)
To develop inhibitors blocking VEGFR2 and the Raf/MEK/ERK mitogen-activated protein kinase signaling pathway new compounds based on sorafenib were designed, synthesized and biologically evaluated. Using de novo design method, a library of new ligands was
Design and synthesis of phthalazine-based compounds as potent anticancer agents with potential antiangiogenic activity via VEGFR-2 inhibition
Elmeligie, Salwa,Aboul-Magd, Asmaa M.,Lasheen, Deena S.,Ibrahim, Tamer M.,Abdelghany, Tamer M.,Khojah, Sohair M.,Abouzid, Khaled A. M.
, p. 1347 - 1367 (2019/07/29)
In the designed compounds, either a biarylamide or biarylurea moiety or an N-substituted piperazine motif was linked to position 1 of the phthalazine core. The anti-proliferative activity of the synthesised compounds revealed that eight compounds (6b, 6e, 7b, 13a, 13c, 16a, 16d and 17a) exhibited excellent broad spectrum cytotoxic activity in NCI 5-log dose assays against the full 60 cell panel with GI50 values ranging from 0.15 to 8.41 μM. Moreover, the enzymatic assessment of the synthesised compounds against VEGFR-2 tyrosine kinase showed the significant inhibitory activities of the biarylureas (12b, 12c and 13c) with IC50s of 4.4, 2.7 and 2.5 μM, respectively, and with 79.83, 72.58 and 71.6% inhibition of HUVEC at 10 μM, respectively. Additionally, compounds (7b, 13c and 16a) were found to induce cell cycle arrest at S phase boundary. Compound 7b triggered a concurrent increase in cleaved caspase-3 expression level, indicating the apoptotic-induced cell death.
Antimetastatic effect of sulfamate carbonic anhydrase IX inhibitors in breast carcinoma xenografts
Gieling, Roben G.,Babur, Muhammad,Mamnani, Lupti,Burrows, Natalie,Telfer, Brian A.,Carta, Fabrizio,Winum, Jean-Yves,Scozzafava, Andrea,Supuran, Claudiu T.,Williams, Kaye J.
experimental part, p. 5591 - 5600 (2012/08/28)
A panel of compounds belonging to the underexposed sulfamate class of carbonic anhydrase (CA, EC 4.2.1.1) inhibitors was generated that displayed high specificity at nanomolar levels for the tumor-associated CA IX/XII isoforms. Three of the specific CA IX
Ureido-substituted sulfamates show potent carbonic anhydrase IX inhibitory and antiproliferative activities against breast cancer cell lines
Winum, Jean-Yves,Carta, Fabrizio,Ward, Carol,Mullen, Peter,Harrison, David,Langdon, Simon P.,Cecchi, Alessandro,Scozzafava, Andrea,Kunkler, Ian,Supuran, Claudiu T.
supporting information; experimental part, p. 4681 - 4685 (2012/07/31)
A series of 50 sulfamates were obtained by reacting 4-aminophenol with isocyanates followed by sulfamoylation. Most of the new compounds were nanomolar inhibitors of the tumor-associated carbonic anhydrase (CA, EC 4.2.1.1) isoforms IX and XII, whereas the
Synthesis and Investigation of Effects of 2-amino>phenoxy>-2-methylpropionic Acids on the Affinity of Hemoglobin for Oxygen: Structure-Activity Relationships
Lalezari, Iraj,Lalezari, Parviz
, p. 2352 - 2357 (2007/10/02)
A series of 2-carbonyl>amino>phenoxy>-2-methylpropionic acids and other substituted phenoxyacetic acids were synthesized and tested for their ability to reduce the affinity of hemoglobin for oxygen. 2-4-(3,4,5-Trichloro
