Chemotherapeutic Dyes. III. 5-Heterocyclicamino-9-dialkylaminobenzo [a]phenoxazines¹

In Vitro Efficacies, ADME, and Pharmacokinetic Properties of Phenoxazine Derivatives Active against Mycobacterium tuberculosis

“…Structures of the phenoxazine nucleus (boxed) and the phenoxazine derivatives examined in this study. All of these compounds (PhX1, PhX2, PhX6, PhX8, PhX10, PhX14, and PhX15) were prepared previously(8,9,11,28,29) and evaluated for antitumor activity and activities against TB and malaria.respect, activities compared well with the median MICs recorded for CLO of 0.25 M (19, 32). Activities against CHO and Vero cell lines are reported as 50% inhibitory concentrations (IC 50 ) values; selectivities with respect to cytotoxicities against M. tuberculosis are promising.…”

“…1), and they have well-defined redox properties (7). A subclass of phenoxazines known as benzo[a]phenoxazines, which bear a fused aryl system, were originally prepared in a notable effort to develop drugs for TB (8); these also were shown to possess antitumor activity (9). Thus, the compounds PhX1, PhX2, PhX6, PhX8, PhX10, and PhX14 have been assessed in basic screens against cancer and TB (8,9), while PhX1 and PhX15 (10) and PhX6 and PhX8 (11) (Fig.…”

Intracellular Accumulation of Novel and Clinically Used TB Drugs Potentiates Intracellular Synergy

“…The compounds PhX1, PhX2, PhX6, PhX8, PhX10, PhX14, PhX15, and DPINH were prepared as reported previously ( 30 , 106 – 110 ). Compounds were synthesized according to the methodologies reported by Crossley et al unless otherwise stated ( 106 , 111 ). RMB041 and WHN296 were synthesized according to previously reported methodologies ( 29 , 112 ).…”