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Novel 1,2,4-triazole derivatives as apoptotic inducers targeting p53: Synthesis and antiproliferative activity.

Abstract：

:A series of novel thiazolo[3,2-b][1,2,4]-triazoles 3a-n has been synthesized and evaluated in vitro as potential antiproliferative. Compounds 3b-d exhibited significant antiproliferative activity. Compound 3b was the most potent with Mean GI50 1.37 µM comparing to doxorubicin (GI50 1.13 µM). The transcription effects of 3b, 3c and 3d on the p53 were assessed and compared with the reference doxorubicin. The results revealed an increase of 15-27 in p53 level compared to the test cells and that p53 protein level of 3b, 3c and 3d was significantly inductive (1419, 571 and 787 pg/mL, respectively) in relation to doxorubicin (1263 pg/mL). The docking study of the new compounds 3a-n revealed high binding scores for the new compounds toward p53 binding domain in MDM2. The docking analyses revealed the highest affinities for compounds 3b-d which induced p53 activity in MCF-7 cancer cells. Compound 3b which exhibited the highest antiproliferative activity and induced the highest increase in p53 level in MCF-7 cells showed also the highest affinity to MDM2.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Gomaa HAM,El-Sherief HAM,Hussein S,Gouda AM,Salem OIA,Alharbi KS,Hayallah AM,Youssif BGM

doi

10.1016/j.bioorg.2020.104369

subject

Has Abstract

pub_date

2020-12-01 00:00:00

pages

104369

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31667-9

journal_volume

105

pub_type

杂志文章

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