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Herein we report novel hybrid compounds based on valproic acid and DNA-alkylating triazene moieties, 1, with therapeutic potential for glioblastoma multiforme chemotherapy. We identified hybrid compounds 1d and 1e to be remarkably more potent against glioma and more efficient in decreasing invasive cell properties than temozolomide and endowed with chemical and plasma stability. In contrast to temozolomide, which undergoes hydrolysis to release an alkylating metabolite, the valproate hybrids showed a low potential to alkylate DNA. Key physicochemical properties align for optimal CNS penetration, highlighting the potential of these effective triazene based-hybrids for enhanced anticancer chemotherapy.
This article was published in the following journal.
Name: European journal of medicinal chemistry
Emergence of drug resistance and targeting all stages of the parasite life cycle are currently the major challenges in antimalarial chemotherapy. Molecular hybridization combining two scaffolds in a s...
The global pandemic of drug-sensitive cancers and the increasing threat from drug-resistant cancers make an urgent need to develop more effective anti-cancer candidates. Quinolone derivatives possess ...
A series of diindolylmethanes (5a-t) were designed, synthesized, and examined for their cytotoxicity against four human cancer cell lines like prostate (DU-145), lung (A549), breast (MCF-7) and cervic...
In this work we synthesized two novel isostructural twin hybrids Comp1: [H(CHN)Cu][PMoO] & Comp2: [H(CHN)Cu][PWO], based on the Keggin ions (PMoO & PWO), Cu(I) cation, and 4,4'-bipyridine, by in situ ...
Quinoline derivatives 2, 3, quinolinyl based pyrazolines 4a,b, 5 and quinolinyl pyrazolinyl thiazole hybrids 6a-d, 7a-c and 8a-d were synthesized and screened for their anti-proliferative activity aga...
Deep brain stimulation (DBS) for essential tremor is based on the intermedius ventralis nucleus of the thalamus (VIM) stimulation. This structure is however very difficult to target, as it...
Irinotecan has demonstrated activity in malignant gliomas in multiple phase II studies. The activity is limited, with an approximately 15 % response rate and a progression-free survival of...
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This is a study to assess the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD) and anti-tumor activity of DS-1001b in patients with gliomas that harbor IDH1-R132 mutation...
A quantitative prediction of the biological, ecotoxicological or pharmaceutical activity of a molecule. It is based upon structure and activity information gathered from a series of similar compounds.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A cytoplasmic receptor and peroxin that contains a series of TETRACOTIPEPTIDE REPEATS and binds to PEROXISOME TARGETING SIGNAL 1 (SKL-type). It is essential for protein import into PEROXISOMES; mutations in the PEX5 gene are associated with PEROXISOMAL DISORDERS such as ZELLWEGER SYNDROME.
A cytoplasmic receptor and peroxin that contains a series of WD40 REPEATS and binds to PEROXISOME TARGETING SIGNAL 2. It is essential for protein import into PEROXISOMES; mutations in the human PEX7 gene are associated with PEROXISOMAL DISORDERS such as Type 1 CHONDRODYSPLASIA PUNCTATA, RHIZOMELIC.
Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.
According to the American Brain Tumor Association, just over 24,000 patients will be diagnosed with a primary malignant brain tumour during 2012 in the US alone. Some 80% of primary malignant brain tumours are gliomas, a broad term which includes all tum...
Bioinformatics is the application of computer software and hardware to the management of biological data to create useful information. Computers are used to gather, store, analyze and integrate biological and genetic information which can then be applied...