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Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line
- Source :
- Bioorganicmedicinal chemistry letters. 27(4)
- Publication Year :
- 2016
-
Abstract
- Taking into account that multidrug resistance (MDR) is the main cause for chemotherapeutic failure in cancer treatment and as a continuation of our efforts to overcome this problem we report the evaluation of one cyclic selenoanhydride (1) and ten selenoesters (2-11) in MDR human colon adenocarcinoma Colo 320 cell line. The most potent derivatives (1, 9-11) inhibited the ABCB1 efflux pump much stronger than the reference compound verapamil. Particularly, the best one (9) was 4-fold more potent than verapamil at a 10-fold lower concentration. Furthermore, the evaluated derivatives exerted a potent and selective cytotoxic activity. In addition, they were strong apoptosis inducers as the four derivatives triggered apoptotic events in a 64-72% of the examined MDR Colo 320 human adenocarcinoma cells.
- Subjects :
- 0301 basic medicine
ATP Binding Cassette Transporter, Subfamily B
Colorectal cancer
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
Apoptosis
Pharmacology
Biochemistry
Anhydrides
03 medical and health sciences
Structure-Activity Relationship
0302 clinical medicine
Cell Line, Tumor
Organoselenium Compounds
Drug Discovery
medicine
Cytotoxic T cell
Humans
Molecular Biology
Chemistry
Organic Chemistry
Cancer
Esters
medicine.disease
digestive system diseases
Multiple drug resistance
030104 developmental biology
Verapamil
Drug Resistance, Neoplasm
030220 oncology & carcinogenesis
Colonic Neoplasms
Molecular Medicine
Adenocarcinoma
Efflux
medicine.drug
Protein Binding
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 27
- Issue :
- 4
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....644b17a5033757ede5dd982eed861f85