Design and synthesis of novel pyrazolo[1,5-a]pyrimidine derivatives bearing nitrogen mustard moiety and evaluation of their antitumor activity in vitro and in vivo
0301 basic medicine
0303 health sciences
Antineoplastic Agents
Apoptosis
Chemistry Techniques, Synthetic
3. Good health
Mice
03 medical and health sciences
Pyrimidines
Cell Line, Tumor
Drug Design
Animals
Humans
Female
Mechlorethamine
Drug Screening Assays, Antitumor
Cell Proliferation
DOI:
10.1016/j.ejmech.2016.04.068
Publication Date:
2016-05-01T09:54:06Z
AUTHORS (8)
ABSTRACT
A series of novel pyrazolo[1,5-a]pyrimidine derivatives bearing nitrogen mustard moiety were designed, synthesized and evaluated for their antiproliferative activities against five human cancer cell lines (A549, SH-SY5Y, HepG2, MCF-7 and DU145) in vitro. Among these compounds, 13b exhibited potent inhibitory effect on the proliferation of the five tumor cells and was able to inhibit cell cycle arrest at G1 phase and induce cell apoptosis. In HepG2 HCC xenograft compound 13b was selected for evaluating the antitumor activity in vivo which exhibited significant cancer growth inhibition with low host toxicity in vivo.
SUPPLEMENTAL MATERIAL
Coming soon ....
REFERENCES (32)
CITATIONS (36)
EXTERNAL LINKS
PlumX Metrics
RECOMMENDATIONS
FAIR ASSESSMENT
Coming soon ....
JUPYTER LAB
Coming soon ....