51516-82-6Relevant academic research and scientific papers
Novel pyrazolo[3,4-d]pyrimidines: design, synthesis, anticancer activity, dual EGFR/ErbB2 receptor tyrosine kinases inhibitory activity, effects on cell cycle profile and caspase-3-mediated apoptosis
Maher, Mai,Kassab, Asmaa E.,Zaher, Ashraf F.,Mahmoud, Zeinab
, p. 532 - 546 (2019)
A series of novel pyrazolo[3,4-d]pyrimidines was synthesised. Twelve synthesised compounds were evaluated for their anticancer activity against 60 human tumour cell lines by NCI (USA). Compound 7d proved prominent anticancer activity. It showed 1.6-fold more potent anti-proliferative activity against OVCAR-4 cell line with IC50 = 1.74 μM. It also exhibited promising potent anticancer activity against ACHN cell line with IC50 value 5.53 μM, representing 2.2-fold more potency than Erlotinib. Regarding NCI-H460 cell line, compound 7d (IC50 = 4.44 μM) was 1.9-fold more potent than Erlotinib. It inhibited EGFR and ErbB2 kinases at sub-micromolar level (IC50 = 0.18 and 0.25 μM, respectively). Dual inhibition of EGFR and ErbB2 caused induction of apoptosis which was confirmed by a significant increase in the level of active caspase-3 (11-fold). It showed accumulation of cells in pre-G1 phase and cell cycle arrest at G2/M phase.
Novel pyrazolopyrimidine urea derivatives: Synthesis, antiproliferative activity, VEGFR-2 inhibition, and effects on the cell cycle profile
El-Dash, Yara,Gedawy, Ehab M.,Kassab, Asmaa E.
, (2020/03/04)
A series of novel diaryl urea pyrazolopyrimidine derivatives was designed and synthesized. All the synthesized compounds were evaluated for cytotoxic activity by the National Cancer Institute. A significant antiproliferative activity at a 10-μM dose was s
Pyrazolyl-tetrazoles and imidazolyl-pyrazoles as potential anticoagulants and their integrated multiplex analysis virtual screening
Louren?o, André L.P.G.,Vegi, Percilene F.,Faria, Jéssica V.,Pinto, Gustavo S.P.,Dos Santos, Maurício S.,Sathler, Plínio C.,Saito, Max S.,Santana, Marcos,Dutra, Tatiana P.P.,Rodrigues, Carlos R.,Monteiro, Robson Q.,Bernardino, Alice M.R.,Castro, Helena C.
, p. 33 - 47 (2018/12/13)
This article reports a novel virtual screening algorithm seeking the rational identification of novel lead anticoagulants. Seven 5-(3-methyl-1-aryl-1H-pyrazol-4-yl)-1H-tetrazoles and seven novel 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-3-methyl-1H-pyrazole
Synthesis and activity of novel tetrazole compounds and their pyrazole-4-carbonitrile precursors against Leishmania spp
Faria, Jéssica V.,Dos Santos, Maurício S.,Bernardino, Alice M.R.,Becker, Klaus M.,Machado, Gérzia M.C.,Rodrigues, Raquel F.,Canto-Cavalheiro, Marilene M.,Leon, Leonor L.
supporting information, p. 6310 - 6312 (2013/11/19)
A new series of 5-(1-aryl-3-methyl-1H-pyrazol-4-yl)-1H-tetrazole derivatives (4a-m) and their precursor 1-aryl-3-methyl-1H-pyrazole-4- carbonitriles (3a-m) were synthesized and evaluated as antileishmanials against Leishmania braziliensis and Leishmania amazonensis promastigotes in vitro. In parallel, the cytotoxicity of these compounds was evaluated on the RAW 264.7 cell line. The results showed that among the assayed compounds the substituted 3-chlorophenyl (4a) (IC50/24 h = 15 ± 0.14 μM) and 3,4-dichlorophenyl tetrazoles (4d) (IC50/24 h = 26 ± 0.09 μM) were the most potent against L. braziliensis promastigotes, as compared the reference drug pentamidine, which presented IC50 = 13 ± 0.04 μM. In addition, 4a and 4d derivatives were less cytotoxic than pentamidine. However, these tetrazole derivatives (4) and pyrazole-4- carbonitriles precursors (3) differ against each of the tested species and were more effective against L.braziliensis than on L. amazonensis.
