Acridine--a neglected antibacterial chromophore

Abstract

The use of acridines as antimicrobial agents was first proposed by Ehrlich and Benda in 1912, and the first clinical use of these agents occurred in 1917. Many compounds containing the acridine chromophore were synthesized and tested, and the aminoacridines found wide use, both as antibacterial agents and as antimalarials, during World War II. The emergence of the penicillins eclipsed the acridines in antisepsis due to the greater therapeutic efficacies of the former. However, with the current massive increases in drug-resistant bacterial infection, new acridine derivatives may be of use. In addition, the topical utilization of aminoacridines in conjunction with directed low-power light offers bactericidal action at much lower doses.

RETRACTED: Acriflavine inhibits HIF-1 dimerization, tumor growth, and vascularization

“…The HIF-2␣ PAS-B crystal structure was shown to contain an internal cavity, which accommodated a small molecule that partially disrupted the heterodimerization of isolated HIF-2␣ and HIF-1␤ PAS subdomains in vitro but was not reported to have any effect on heterodimerization of the full length proteins or on HIF-1 transcriptional activity (13). We show that ACF binds to the PAS-B subdomain of HIF-1␣ or HIF-2␣, thereby blocking het- ACF has known trypanocidal, antibacterial, and antiviral activities (14). Effects of ACF on cancer cells were first reported 50 years ago (15).…”

“…Unlike other drugs that indirectly inhibit HIF-1 activity, ACF binds directly to both HIF-1␣ and HIF-2␣. ACF has been administered to patients for at least 5 months without major side effects (14), suggesting that it may be a candidate for clinical trials. ACF can also serve as the lead compound for development of drugs to treat patients with cancer subtypes in which increased HIF-1␣ or HIF-2␣ levels are associated with disease progression and patient mortality (2,5).…”

Small-Molecule Inhibitor Which Reactivates p53 in Human T-Cell Leukemia Virus Type 1-Transformed Cells

“…9AA was initially identified as an antibacterial agent (42,47). Subsequently, it was found that staining of histopathological sections with 9AA could be used to locate malignant cells in many tumor tissues.…”

A simple one-pot synthesis of new 9-aroyl-3,4,6,7,9,10-hexahydro-1,8(2H,5H)-acridinediones

“…The 1,8-acridinediones and their derivatives are known to exhibit a wide range of biological and pharmaceutical properties such as antibacterial, 1 antimicrobial, 2 anticancer, [3][4][5] antitumor, [6][7] antifungal, 8 antimalarial, 9 antiviral, 10 larvicidal 11 and hypertensive 12 activities. Electroluminescent devices based on decahydroacridinedione (DAD) derivatives exhibit good efficiencies and excellent color purity.…”