All Outputs (11)

Autophagy modulation: a prudent approach in cancer treatment? (2018)
Journal Article

Autophagy is a tightly controlled process comprising lysosomal degradation and recycling of cellular proteins and organelles. In cancer, its paradoxical dual role of cytoprotection and cytotoxicity is context-dependent and controversial. Autophagy pr... Read More about Autophagy modulation: a prudent approach in cancer treatment?.

Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines (2018)
Journal Article

The cytotoxic activity of ethanol extract of Parquetina nigrescen was investigated using a (3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, methylene blue and Trypan Blue exclusion assay on four human cancer cell lines, MCF... Read More about Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines.

Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system (2018)
Journal Article

The intestinal lymphatic system plays an important role in the pathophysiology of multiple diseases including lymphomas, cancer metastasis, autoimmune diseases, and human immunodeficiency virus (HIV) infection. It is thus an important compartment for... Read More about Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system.

Sustainable Syntheses of (-)-Jerantinines A & e and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site (2018)
Journal Article

The jerantinine family of Aspidosperma indole alkaloids from Tabernaemontana corymbosa are potent microtubule-targeting agents with broad spectrum anticancer activity. The natural supply of these precious metabolites has been significantly disrupted... Read More about Sustainable Syntheses of (-)-Jerantinines A & e and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site.

Nucleoside based self-assembling drugs for localized drug delivery (2018)
Journal Article

We have synthesized a range of gelators based on nucleoside analogues gemcitabine and lamivudine, characterizing representative gels from the series using rheology and TEM. Growth inhibition studies of gemcitabine derivatives confirmed the feasibilit... Read More about Nucleoside based self-assembling drugs for localized drug delivery.

Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery (2018)
Journal Article

1,2-Diazetidin-3-ones are readily accessible, small ring scaffolds that upon functionalization have the potential to produce diverse 3-dimensional structures for drug discovery. Thus treatment of diazo hydrazides, obtained from simple hydrazides and... Read More about Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery.

Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation (2018)
Journal Article

Low molecular weight gelators (LMWGs) of chemotherapeutic drugs represent a valid alternative to the existing poly-mer-based formulations used for targeted delivery of anticancer drugs. Herein we report the design and development of novel self-assemb... Read More about Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation.

Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position (2018)
Journal Article

A series of 3-(benzyl-substituted)-imidazo[5,1-d]-1,2,3,5-tetrazines (13) and related derivatives with 3-heteromethyl groups has been synthesised and screened for growth-inhibitory activity in vitro against two pairs of glioma cell lines with temozol... Read More about Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position.

Discovery of a highly active anticancer analogue of cardamonin that acts as an inducer of caspase-dependent apoptosis and modulator of the mTOR pathway (2018)
Journal Article

Nineteen analogues of cardamonin were semi-synthesized and tested against A549 and HK1 cell lines. The analogues were fully characterized via IR and NMR analyses, while compound 19 (a Cu (II) complex of cardamonin) was further characterized via HRMS,... Read More about Discovery of a highly active anticancer analogue of cardamonin that acts as an inducer of caspase-dependent apoptosis and modulator of the mTOR pathway.

Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells (2018)
Journal Article

The efficacy of temozolomide (TMZ) treatment for cancers is currently limited by inherent or the development of resistance, particularly, but not exclusively, due to the expression of the DNA repair enzyme O6-methylguanine-DNA methyltransferase (MGMT... Read More about Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells.

Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging (2018)
Journal Article

The short shelf-life of water-soluble quantum dots (QDs) due to colloidal instability represents a major drawback to their exploitation. This work examines the colloidal stability of PbS nanoparticles capped with dihydrolipoic acid–polyethylene glyco... Read More about Stable DHLA–PEG capped PbS quantum dots: from synthesis to near-infrared biomedical imaging.