Share This Author
Temozolomide: mechanisms of action, repair and resistance.
Several small molecule inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1), a critical BER protein are yielding promising results clinically, both in combination with TMZ and as single agent chemotherapy in patients whose tumours possess homologous recombination DNA repair defects.
Cannabinoid receptor agonists are mitochondrial inhibitors: a unified hypothesis of how cannabinoids modulate mitochondrial function and induce cell death.
The development of the antitumour benzothiazole prodrug, Phortress, as a clinical candidate.
This review traces the development of a series of potent and selective antitumour benzothiazoles from the discovery of the initial lead compound, 2-(4-amino-3-methylphenyl)benzothiazole (DF 203) in…
A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine
CDKI-73 was more potent than the pan-cdk inhibitor flavopiridol and showed >200-fold selectivity against primary leukemia cells when compared with normal CD34+ cells and was equipotent in poor prognostic sub-groups of leukemia patients and showed cytotoxic synergy with the nucleoside analog fludarabine.
Thioredoxin reductase inhibition by antitumor quinols: a quinol pharmacophore effect correlating to antiproliferative activity
- Eng-Hui Chew, Jun Lu, T. Bradshaw, A. Holmgren
- Chemistry, BiologyFASEB journal : official publication of the…
- 1 June 2008
It is proposed that TrxR inhibition is a critical cellular event that contributes to the proapoptotic effects of quinols and is correlated with their antipro liferative and cytotoxic efficacies.
Overcoming multiple drug resistance mechanisms in medulloblastoma
ABCB1 is associated with high-risk MB and inhibition of ABCB1 by vardenafil may represent a valid approach in these patients, and Imidazotetrazine analogues of TMZ and the BH3 mimetic obatoclax are promising clinical candidates in drug resistant MB tumours expressing MGMT and BCL2 anti-apoptotic members respectively.
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
The most potent broad spectrum agent in the NCI cell panel was 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (10h) which, unlike the 6-fluoro isomer (10d), produces no exportable metabolites in the presence of sensitive MCF-7 cells.
Antitumor benzothiazoles. 3. Synthesis of 2-(4-aminophenyl)benzothiazoles and evaluation of their activities against breast cancer cell lines in vitro and in vivo.
Four compounds have been evaluated in vivo against human mammary carcinoma models in nude mice and compound 9a showed the most potent growth inhibition against the ER+ (MCF-7 and BO) and ER- (MT-1 and MT-3) tumors.
The discovery of the potent and selective antitumour agent 2-(4-amino-3-methylphenyl)benzothiazole (DF 203) and related compounds.
Structural-activity relationship studies within this simple antitumour benzothiazole pharmacophore revealed that 2-(4-aminophenyl) Benzothiazoles bearing a 3'- methyl, 3-bromo, 3'-iodo or 3'-chloro substituent are especially potent, extending the spectrum of in vitro antitumours activity to ovarian, lung, renal and colon carcinoma cell lines with a remarkable selectivity profile (NCI analysis).
Novel antitumour indole alkaloid, Jerantinine A, evokes potent G2/M cell cycle arrest targeting microtubules
- V. J. Raja, K. Lim, C. Leong, T. Kam, T. Bradshaw
- Biology, ChemistryInvestigational New Drugs
- 15 June 2014
The potent anti-proliferative, pro-apoptotic, and tubulin-destabilising activities of jerantinine A warrant further development of this molecule as a potential chemotherapeutic agent.