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PubMed Publications| Keyword search (4,163 papers available) |  |
"Jaunky DB" Authored Publications:
| Title | Authors | PubMed ID | |
|---|---|---|---|
| 1 | Characterization of a recently synthesized microtubule-targeting compound that disrupts mitotic spindle poles in human cells | Jaunky DB; Larocque K; Husser MC; Liu JT; Forgione P; Piekny A; | 34880347 BIOLOGY |
| 2 | 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 |
| 3 | Dual disassembly and biological evaluation of enzyme/oxidation-responsive polyester-based nanoparticulates for tumor-targeting delivery. | Hong SH, Larocque K, Jaunky DB, Piekny A, Oh JK | 30223243 CHEMBIOCHEM |
| 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 JT, Jaunky DB, Larocque K, Chen F, Mckibbon K, Sirouspour M, Taylor S, Shafeii A, Campbell D, Braga H, Piekny A, Forgione P | ||||
| Link: | https://pubmed.ncbi.nlm.nih.gov/34416378/ | ||||
| DOI: | 10.1016/j.bmcl.2021.128327 | ||||
| Publication: | Bioorganic & medicinal chemistry letters | ||||
| Keywords: | Anticancer; Colchicine; Microtubules; SAR study; Thienoisoquinoline; | ||||
| 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. |
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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. |
