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evaluation of novel synthetic pyrazolones as CDK9 inhibitors with enhanced pharmacokinetic properties.
Future Med Chem
December 2024
Heterocyclic Synthesis Laboratory, Department of Chemistry, Faculty of Science, Ain Shams University 11566, Abbassia, Cairo, Egypt.
The structural optimization of our recently reported CDK9 inhibitor to furnish novel aminopyrazolones and methylpyrazolones with improved pharmacokinetics. The synthesis of the targeted compounds was accomplished via conventional, grinding and microwave-assisted processes. The cytotoxicity of them was assayed against three carcinomas.
View Article and Find Full Text PDFEpCAM-targeted betulinic acid analogue nanotherapy improves therapeutic efficacy and induces anti-tumorigenic immune response in colorectal cancer tumor microenvironment.
J Biomed Sci
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Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
Background: Betulinic acid (BA) has been well investigated for its antiproliferative and mitochondrial pathway-mediated apoptosis-inducing effects on various cancers. However, its poor solubility and off-target activity have limited its utility in clinical trials. Additionally, the immune modulatory role of betulinic acid analogue in the tumor microenvironment (TME) is largely unknown.
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EJNMMI Radiopharm Chem
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Nuclear Medical Applications Institute, Belgian Nuclear Research Centre (SCK CEN), Mol, Belgium.
Background: Glioblastoma (GBM), is the most fatal form of brain cancer, with a high tendency for recurrence despite combined treatments including surgery, radiotherapy, and chemotherapy with temozolomide. The C-X-C chemokine receptor 4 (CXCR4) plays an important role in tumour radioresistance and recurrence, and is considered as an interesting GBM target. TRT holds untapped potential for GBM treatment, with CXCR4-TRT being a promising strategy for recurrent GBM treatment.
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Radiation Medicine Centre, Bhabha Atomic Research Centre, Parel, Mumbai 400012, India.
Cancer is a major public health problem worldwide, and it is the second leading cause of death of humans in the world. The present study has been directed toward the preparation of methotrexate-loaded surface-modified solid lipid nanoparticles (SLNs) for potential use as a chemotherapeutic formulation for cancer therapy. A lipid (C-AAP) derived from myristic acid (CHO) and acetaminophen (AAP) was employed as a targeting ligand for human breast and lung cancer cells that overexpress the cyclooxygenases-2 (COX-2) enzyme.
View Article and Find Full Text PDFLipid-Based Nanocarrier by Targeting with LHRH Peptide: A Promising Approach for Prostate Cancer Radio-Imaging and Therapy.
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Netaji Subhas Chandra Bose Cancer Hospital, 3081 Nayabad, Kolkata 700094, India.
Prostate cancer is a prevalently detected malignancy with a dismal prognosis. Luteinizing-hormone-releasing-hormone (LHRH) receptors are overexpressed in such cancer cells, to which the LHRH-decapeptide can specifically bind. A lipid-polyethylene glycol-conjugated new LHRH-decapeptide analogue (D-P-HLH) was synthesized and characterized.
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