ArticlePharmaceuticals (Basel, Switzerland)2021
Design, Synthesis, Anticancer Activity, and Solid Lipid Nanoparticle Formulation of Indole- and Benzimidazole-Based Compounds as Pro-Apoptotic Agents Targeting Bcl-2 Protein.
Article in Pharmaceuticals (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 32 citations in OpenAlex.
- From Scaffold to Therapy: Benzimidazole Pharmacophore Evolution in Breast Cancer Research.Chemistry & biodiversity · 2026Review
- Dual inhibition of cell cycle progression and apoptotic resistance in breast cancer by novel benzimidazole-based therapeutics.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Identification of potential natural BCL-2 inhibitors for leukemia through an integrated virtual screening approach.BMC pharmacology & toxicology · 2025Article
- Development of indole hybrids for potential lung cancer treatment - part II.Future medicinal chemistry · 2025Review
- Targeting Bcl-2 with Indole Scaffolds: Emerging Drug Design Strategies for Cancer Treatment.Mini reviews in medicinal chemistry · 2025Review
- Pioneering the Battle Against Breast Cancer: The Promise of New Bcl-2 Family.Anti-cancer agents in medicinal chemistry · 2025Review
- Optimized Nanostructured Lipid Carriers for Metformin: Enhanced Anti-Inflammatory Activity and Protection Against Type 2 Diabetes-Induced Organ Damage.International journal of nanomedicine · 2025Article
- Regulation of hippo signaling mediated apoptosis by Rauvolfia tetraphylla in triple-negative breast cancer.Medical oncology (Northwood, London, England) · 2024Article
- Ginger Oil Nanoemulsion Formulation Augments Its Antiproliferative Effect in Ehrlich Solid Tumor Model.Foods (Basel, Switzerland) · 2023Article
- In silico design and cell-based evaluation of two dual anti breast cancer compounds targeting Bcl-2 and GPER.Scientific reports · 2023Article
- Design, Synthesis, and Potent Anticancer Activity of Novel Indole-Based Bcl-2 Inhibitors.International journal of molecular sciences · 2023Article
- Deciphering Molecular Aspects of PotentialMetabolites · 2023Article
- Rational Design, Synthesis and Biological Evaluation of Novel Pyrazoline-Based Antiproliferative Agents in MCF-7 Cancer Cells.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Phenolics fromBiology · 2022Article
- Special Issue "Anticancer Drugs 2021".Pharmaceuticals (Basel, Switzerland) · 2022Article
- Antioxidant and Anti-Inflammatory Activity ofAntioxidants (Basel, Switzerland) · 2021Article
- Synthesis, In Silico Prediction and In Vitro Evaluation of Antimicrobial Activity, DFT Calculation and Theoretical Investigation of Novel Xanthines and Uracil Containing Imidazolone Derivatives.International journal of molecular sciences · 2021Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cancer is a multifactorial disease necessitating identification of novel targets for its treatment. Inhibition of Bcl-2 for triggered pro-apoptotic signaling is considered a promising strategy for cancer treatment. Within the current work, we aimed to design and synthesize a new series of benzimidazole- and indole-based derivatives as inhibitors of Bcl-2 protein. The market pan-Bcl-2 inhibitor, obatoclax, was the lead framework compound for adopted structural modifications. The obatoclax's pyrrolylmethine linker was replaced with straight alkylamine or carboxyhydrazine methylene linkers providing the new compounds. This strategy permitted improved structural flexibility of synthesized compounds adopting favored maneuvers for better fitting at the Bcl-2 major hydrophobic pocket. Anti-cancer activity of the synthesized compounds was further investigated through MTT-cytotoxic assay, cell cycle analysis, RT-PCR, ELISA and DNA fragmentation. Cytotoxic results showed compounds
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