Conjugation of substituted ferrocenyl to thiadiazine as apoptosis-inducing agents targeting the Bax/Bcl-2 pathway.

Abstract:

:Ferrocene compounds are a class of biologically active compounds that has antitumour and antifungal properties. This study investigated the induction of apoptosis in human fibrosarcoma cells (HT1080) after treatment with a series of 6-ferrocenyl-3-subsituted7H-1,2,4-triazolo[3,4-b]- 1,3,4-thiadiazine (FTFs). We found that FTFs could suppress the viability of HT1080 cells. Cell cycle analysis showed that proliferative inhibition of HT1080 cells occurred through apoptosis, as the cells were blocked in G1 phase. Moreover, mitochondrial membrane staining assay demonstrated that FTFs exposure significantly decreased mitochondrial membrane potential. Finally, under the stress of FTFs, Bax/Bcl-2 ratio in HT1080 cells was significantly increased. These results suggested that FTFs-induced apoptosis in HT1080 cells may work dependent on a Bax/Bcl-2 pathway.

journal_name

Eur J Med Chem

authors

Miao R,Wei J,Lv M,Cai Y,Du Y,Hui X,Wang Q

doi

10.1016/j.ejmech.2011.08.007

subject

Has Abstract

pub_date

2011-10-01 00:00:00

pages

5000-9

issue

10

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00579-4

journal_volume

46

pub_type

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