ArticleCancer cell international2016
Evidence that phospholipase C is involved in the antitumour action of NSC768313, a new thieno[2,3-b]pyridine derivative.
Article in Cancer cell international, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 35 citations in OpenAlex.
- β-Ketoamides in Thieno[2,3-Molecules (Basel, Switzerland) · 2026Article
- Mammalian PI-Phospholipase C Isozymes: Structural and Functional Insights and Roles in Health and Disease.Medicina (Kaunas, Lithuania) · 2025Review
- Synthesis of Thieno[2,3-c]pyridine Derivatives by 1,2,3-Triazole-Mediated Metal-Free Denitrogenative Transformation Reaction.ChemistryOpen · 2025Article
- Thieno[2,3-International journal of molecular sciences · 2025Article
- Thieno[2,3-Endocrine oncology (Bristol, England) · 2025Article
- Biochemical Pathways Delivering Distinct Glycosphingolipid Patterns in MDA-MB-231 and MCF-7 Breast Cancer Cells.Current issues in molecular biology · 2024Review
- Deciphering the Interplay: Thieno[2,3-International journal of molecular sciences · 2024Article
- Phosphatidylcholine-Specific Phospholipase C as a Promising Drug Target.Molecules (Basel, Switzerland) · 2023Review
- Synthesis and Anti-Proliferative Activity of 5-Benzoyl and 5-Benzylhydroxy Derivatives of 3-Amino-2-Arylcarboxamido-Thieno[2-3-International journal of molecular sciences · 2023Article
- Novel Thieno [2,3-International journal of molecular sciences · 2022Article
- Disruption of Crystal Packing in Thieno[2,3-Molecules (Basel, Switzerland) · 2022Article
- Conjugation of Palbociclib with MHI-148 Has an Increased Cytotoxic Effect for Breast Cancer Cells and an Altered Mechanism of Action.Molecules (Basel, Switzerland) · 2022Article
- Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs.Oncology and therapy · 2021Article
- Tethered Aryl Groups Increase the Activity of Anti-Proliferative Thieno[2,3-Pharmaceutics · 2021Article
- Thieno[2,3-Medicines (Basel, Switzerland) · 2021Article
- Unusual Oxidative Dimerization in the 3-Aminothieno[2,3-ACS omega · 2021Article
- Glycosphingolipid expression at breast cancer stem cells after novel thieno[2,3-b]pyridine anticancer compound treatment.Scientific reports · 2020Article
- Investigation into Improving the Aqueous Solubility of the Thieno[2,3-b]pyridine Anti-Proliferative Agents.Molecules (Basel, Switzerland) · 2018Article
- GPCR Modulation of Thieno[2,3-b]pyridine Anti-Proliferative Agents.Molecules (Basel, Switzerland) · 2017Article
- Multi-walled carbon nanotubes act as a chemokine and recruit macrophages by activating the PLC/IP3/CRAC channel signaling pathway.Scientific reports · 2017Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThe thieno[2,3-b]pyridines were discovered by virtual high throughput screening as potential inhibitors of phospholipase C (PLC) isoforms and showed potent growth inhibitory effects in National Cancer Institute's human tumour cell line panel (NCI60). The mechanism of the anti-proliferative activity of thieno[2,3-b]pyridines is explored here.
objectivesWe aimed to investigate the basis for the anti-proliferative activity of these thieno[2,3-b]pyridines and to determine whether the cellular inhibition was related to their inhibition of PLC.
methodsFour breast cancer cell lines were used to assess the anti-proliferative effects (IC50 values) of six representative thieno[2,3-b]pyridines. The most potent compound (derivative 3; NSC768313), was further studied in MDA-MB-231 cells. DNA damage was examined by γH2AX expression level, and cell cycle arrest by flow cytometry. Cell morphology was examined by tubulin antibody staining. The growth inhibitory effect of combination treatment with derivative 3 and paclitaxel (tubulin inhibitor), doxorubicin (topoisomerase II inhibitor) or camptothecin (topoisomerase I inhibitor) was evaluated. A preliminary mouse toxicity assay was used to evaluate the pharmacological properties.
resultsAddition of the thieno[2,3-b]pyridine derivative 3 to the MDA-MB-231 cells induced G2/M growth inhibition, cell cycle arrest in G2-phase, membrane blebbing and the formation of multinucleated cells. It did not induce DNA damage, mitotic arrest or changes in calcium ion flux. Combination of derivative 3 with paclitaxel showed a high degree of synergy, while combinations with doxorubicin and camptothecin showed only additive effects. A mouse pharmacokinetic study of derivative 3 showed that after intraperitoneal injection of a single does (10 mg/Kg), the Cmax was 0.087 μmol/L and the half-life was 4.11 h.
conclusionsThe results are consistent with a mechanism in which thieno[2,3-b]pyridine derivatives interact with PLC isoforms (possibly PLC-δ), which in turn affect the cellular dynamics of tubulin-β, inducing cell cycle arrest in G2-phase. We conclude that these compounds have novelty because of their PLC target and may have utility in combination with mitotic poisons for cancer treatment.
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