3-Arylindanones and related compounds as antiproliferative agents against colorectal cancer.
Ankita SrivastavaKusumoori RaviKaneez FatimaMayank MaheshwariRaghib AshrafMohammad HasanainPankaj YadavHina IqbalYogesh KumarSuaib LuqmanDebabrata ChandaFeroz KhanKaruna ShankerJayanta SarkarArvind Singh NegiPublished in: Chemical biology & drug design (2019)
Diverse benzylidene indanones and their derivatives were synthesized as anticancer agents. Two of the analogues, that is 7 and 22, exhibited significant antiproliferative activity against several human cancer cell lines. Both the compounds possessed antimitotic activity and induced apoptosis in DLD1 colorectal adenocarcinoma cells through activation of caspase pathways. In cell cycle analysis, both the compounds induced predominantly G2/M phase arrest in DLD1 cells. Molecular docking studies revealed that compound 7 occupies colchicine binding pocket of β-tubulin. Both the compounds were safe in acute oral toxicity in rodents. Both the compounds are further being optimized for better efficacy.
Keyphrases
- induced apoptosis
- cell cycle
- endoplasmic reticulum stress
- molecular docking
- oxidative stress
- signaling pathway
- cell proliferation
- diabetic rats
- cell cycle arrest
- endothelial cells
- drug induced
- molecular dynamics simulations
- cell death
- liver failure
- radiation therapy
- papillary thyroid
- pi k akt
- locally advanced
- acute respiratory distress syndrome
- squamous cell
- data analysis
- aortic dissection