Induction of apoptosis in cervical cancer cells by the duplex drug 5-FdU–ECyd, coupling 2′-deoxy-5-fluorouridine and 3′-C-ethinylcytidine

The conjugated antimetabolite 5-FdU-ECyd and its cellular and molecular effects on platinum-sensitive vs. -resistant ovarian cancer cellsin vitro

“…Moreover, in (isogenic or independent) platinum-resistant OC cells, 5-FdU-ECyd induced a similar apoptotic response, indicating that its mechanism of action is independent of platinum-resistance status. These findings are in accordance to our previous in vitro study on cervical cancer, reporting that nano molar 5-FdU-ECyd induces apoptotic cell death and early S-phase arrest, also including platinum-resistant SiHa cells [ 12 ]. Besides apoptosis induction, we noticed that 5-FdU-ECyd induces autophagy.…”

“…caspase 3 ), indicated that our transcriptome data reflect a rather early response signature to 5-FdU-ECyd. The p53-pathway, which is a major driver of cell cycle arrest and apoptosis [ 27 ], was consistently activated in A2780 and A2780cis cells, which is in accordance to our in vitro experiments on 5-FdU-ECyd mediated apoptosis and is also in line with previous studies, reporting that 5-FdU-ECyd induces apoptosis and G1-arrest in cervical cancer cells in vitro [ 12 ]. CDKN1A and c-Fos were among the most consistently up-regulated genes, showing a significant up-regulation already after 6 h of 5-FdU-ECyd treatment.…”

Regioselective synthesis and theoretical studies of an anti-neoplastic fluoro-substituted dispiro-oxindole

“…Cisplatin is the drug of choice either alone or in combination with topotecan 46 for cervical chemotherapy and cisplatin in combination with 5-uorouracil has also been reported. 47,48 However, severe sideeffects such as bone-marrow depression, neutropenia, thrombocytopenia and anaemia due to haematological toxicity along with nephrotoxicity and neurotoxicity 49 and acquired chemoresistance 50 throughout the course of treatment, have limited the usage of cisplatin.…”

Rational design, synthesis, and 2D-QSAR study of anti-oncological alkaloids against hepatoma and cervical carcinoma

“…26 The combination of cisplatin with 5-uorouracil has also been reported. 27,28 However, severe side-effects like bone-marrow depression, neutropenia, thrombocytopenia and anaemia due to haematological toxicity along with nephrotoxicity and neurotoxicity 29 and acquired chemoresistance 30 throughout the course of treatment have limited the usage of cisplatin. Other reports describe the severe renal toxicity and gastrointestinal side effects of cisplatin that limits its clinical application.…”