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Abstract:
In our research on novel anticancer agents, a series of N-6-hydrazone purine derivatives were designed and synthesized by analysis of a pharmacophore model for ATP-competitive inhibitors. The activities screening results showed that N-6-hydrazone purine derivatives 21 and 26 not only showed potential antiproliferative activity against the A549 and MCF-7 cell lines comparable to Vandetanib as a positive control but also had moderate antiplatelet aggregation activity. In order to investigate the possible targets, a molecular docking study was carried out on the fourteen kinases associated with anticancer and antiplatelet aggregation activities. The results indicated that compounds 21 and 26 had the potential activity to target VEGFR-2, PI3K alpha, EGFR, and HER2 kinases. The inhibition of the kinases assay showed that compound 26 could target VEGFR-2, PI3K alpha, and EGFR (IC50 = 0.822, 3.040 and 6.625 mu M). All results indicated that compound 26 will be an encouraging framework as potential new multi-target anticancer agent with potential antiplatelet aggregation activity.
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CHEMICAL BIOLOGY & DRUG DESIGN
ISSN: 1747-0277
Year: 2022
Issue: 3
Volume: 101
Page: 568-580
3 . 0
JCR@2022
3 . 0 0 0
JCR@2022
ESI Discipline: BIOLOGY & BIOCHEMISTRY;
ESI HC Threshold:43
JCR Journal Grade:3
CAS Journal Grade:4
Cited Count:
WoS CC Cited Count: 4
SCOPUS Cited Count: 4
ESI Highly Cited Papers on the List: 0 Unfold All
WanFang Cited Count:
Chinese Cited Count:
30 Days PV: 7
Affiliated Colleges: