Keyword search (4,163 papers available)

"Chen F" Authored Publications:

Title Authors PubMed ID
1 Overlap and Covalency in a κN-Arylnitrosyl Cu(II) Metalloradical Formed by Hydroxylamine Oxidative Binding MacKay A; Zsombor-Pindera J; Effaty F; Sheibany N; Gennarini F; Habibian M; Chen F; Askari MS; Brytskyi M; Kroeker S; Kennepohl P; Ottenwaelder X; 41524899
CHEMBIOCHEM
2 Substituted diphenylamine antioxidants and synthetic phenolic antioxidants in leachate from domestic landfills in China: Occurrence and removal via treatment Zhang LH; Chen F; Zhang XM; Zhang X; Liang B; Bai SS; Zhang ZF; Li YF; Ren NQ; 41270417
CHEMBIOCHEM
3 Intramolecular H-bond stabilization of a primary hydroxylamine in salen-type metal complexes Singh H; MacKay A; Sheibany N; Chen F; Mosser M; Rouet PÉ; Rousseau F; Askari MS; Ottenwaelder X; 34545379
CHEMBIOCHEM
4 Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent Liu JT; Jaunky DB; Larocque K; Chen F; Mckibbon K; Sirouspour M; Taylor S; Shafeii A; Campbell D; Braga H; Piekny A; Forgione P; 34416378
BIOLOGY
5 Comparative genomics reveals high biological diversity and specific adaptations in the industrially and medically important fungal genus Aspergillus. de Vries RP, Riley R, Wiebenga A, Aguilar-Osorio G, Amillis S, Uchima CA, Anderluh G, Asadollahi M, Askin M, Barry K, Battaglia E, Bayram Ö, Benocci T, Braus-Stromeyer SA, Caldana C, Cánovas D, Cerqueira GC, Chen F, Chen W, Choi C, Clum A, Dos Santos RA, Damásio AR, Diallinas G, Emri T, Fekete E, Flipphi M, Freyberg S, Gallo A, Gournas C, Habgood R, Hainaut M, Harispe ML, Henrissat B, Hildén KS, Hope R, Hossain A, Karabika E, Karaffa L, Karányi Z, Kraševec N, Kuo A, Kusch H, LaButti K, Lagendijk EL, Lapidus 28196534
NA

 

Title:Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent
Authors:Liu JTJaunky DBLarocque KChen FMckibbon KSirouspour MTaylor SShafeii ACampbell DBraga HPiekny AForgione P
Link:https://pubmed.ncbi.nlm.nih.gov/34416378/
DOI:10.1016/j.bmcl.2021.128327
Publication:Bioorganic & medicinal chemistry letters
Keywords:AnticancerColchicineMicrotubulesSAR studyThienoisoquinoline
PMID:34416378 Category: Date Added:2021-08-21
Dept Affiliation: BIOLOGY
1 Department of Chemistry & Biochemistry, Concordia University, 7141 rue Sherbrooke O., Montréal, QC H4B 1R6, Canada.
2 Department of Biology, Concordia University, 7141 rue Sherbrooke O., Montréal, QC H4B 1R6, Canada.
3 Center for Green Chemistry and Catalysis, Department of Chemistry, McGill University, 801 rue Sherbrooke O., Montréal, QC H3A 0B8, Canada.
4 Department of Chemistry & Biochemistry, Concordia University, 7141 rue Sherbrooke O., Montréal, QC H4B 1R6, Canada; Department of Biology, Concordia University, 7141 rue Sherbrooke O., Montréal, QC H4B 1R6, Canada.

Description:

Several derivatives of a series that share a thienoisoquinoline scaffold have demonstrated potent anti-cancer activity against cancer cell lines A549, HeLa, HCT-116 in the submicromolar concentration range. Structure-activity relationship (SAR) studies on a range of derivatives aided in identifying key pharmacophores in the lead compound. A series of compounds have been identified as the most promising with submicromolar IC50 values against a lung cancer cell line (A549). Microscopy studies of cancer cells treated with the lead compound revealed that it causes mitotic arrest and disrupts microtubules. Further evaluation via an in vitro microtubule polymerization assay and competition studies indicate that the lead compound binds to tubulin via the colchicine site.





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