An article Synthesis and molecular docking study of new pyrazole derivatives as potent anti-breast cancer agents targeting VEGFR-2 kinase WOS:000552629800008 published article about GROWTH-FACTOR RECEPTOR-2; BIOLOGICAL EVALUATION; ANTICANCER EVALUATION; INHIBITORS; ANGIOGENESIS; RESISTANCE; MECHANISM; DISCOVERY; DESIGN in [Dawood, Dina H.] Natl Res Ctr, Chem Nat & Microbial Prod Dept, Pharmaceut & Drug Ind Res Div, 33 El Bohouth St,POB 12622, Giza, Egypt; [Nossier, Eman S.] Al Azhar Univ, Fac Pharm Girls, Dept Pharmaceut Chem, POB 11754, Cairo, Egypt; [Ali, Mamdouh M.; Mahmoud, Abeer E.] Natl Res Ctr, Biochem Dept, Genet Engn & Biotechnol Res Div, 33 El Bohouth St,POB 12622, Giza, Egypt in 2020.0, Cited 50.0. Category: Triazoles. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5
Based on the previous studies that revealed the valuable role of pyrazole scaffold in cancer management and VEGFR-2 inhibition, a new set of pyrazole conjugated with pyrazoline, triazolopyrimidine and pyrazolone moieties were synthesized and investigated for their anticancer efficiency against human breast cancer MCF-7. The anticancer screening revealed the significant sensitivity of breast carcinoma towards compounds 4b, 5c, 6c, 7b, 7c and 12c with IC50 values ranging from 16.50 – 26.73 mu M in comparison with tamoxifen (IC50 = 23.31 mu M). Moreover, the new analogues were further examined for their VEGFR-2 inhibitory activity, among the tested derivatives 5c, 6c, 7b, 7c and 12c displayed prominent inhibitory efficiency versus VEGFR-2 kinase with % inhibition ranging from 70 to 79%. Compounds 6c, 7c and 12c revealed inhibitory efficiency in nanomolar level with IC50 (913.51, 225.17 and 828.23 nM, respectively) comparing to sorafenib (IC50 = 186.54 nM). Flow cytometric analysis revealed that the promising compound 12c prompted pre-G1 apoptosis and cell growth cessation at G2/M phase and stimulated apoptosis via activation of caspase-3. Moreover, molecular docking study of the promising derivatives was performed to highlight their binding modes and interactions with the amino acid residues of VEGFR-2 enzyme.
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Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics