Some fluoroquinazolinones (A–H) were designed, synthesized and biologically evaluated for their antitumor activity against the two cell lines, MCF-7 and MDA-MBA-231. New derivative G (IC50 = 0.44 ± 0.01 µM) showed antitumor activity, better than that of the reference drug erlotinib (IC50 = 1.14 ± 0.04 µM) against MCF-7. New derivative E (IC50 = 0.43 ± 0.02 µM) showed higher activity than the reference drug erlotinib (IC50 = 2.55 ± 0.19 µM) against MDA-MBA-231. Furthermore, the EGFR (epidermal growth factor receptor) and tubulin inhibition assays were carried out for the highest active derivatives to reveal the expected mechanism of action. They exhibited significant results compared to the reference drugs. Molecular docking simulations were performed on EGFR and tubulin binding sites to rationalize the experimental results and describe their binding modes. The results of the molecular modeling study were correlated with that of the antitumor screening.
1 September 2021 in Journal of Taibah University Medical Sciences
This study examines the effect of behavioural therapy (biofeedback) and interferential current on bladder dysfunction in multiple sclerosis patients. Fifty patients with secondary progressive type multiple sclerosis (SPMS) suffering from bladder dysfunction were divided equally into two groups randomly. Group A (GA) received behavioural therapy (biofeedback training), while Group B (GB) received interferential current training. Both groups were assessed by urodynamics for detrusor pressure and maximum flow rate before and after eight weeks of behavioural therapy and interferential training. Both groups, GA and GB, showed significant increase in the detrusor pressure and maximum flow rate after eight weeks of training. There was no significant difference between both methods. However, GA showed more improvement by close observation. Both behavioural therapy and interferential current training effectively managed bladder dysfunction in patients with SPMS, with more evident effects in behavioural therapy patients by close observation.