Synthesis, and biological evaluation of 2-(4-aminophenyl)benzothiazole derivatives as photosensitizing agents

Bioorganic & Medicinal Chemistry
Wan-Ping HuJeh-Jeng Wang

Abstract

Photodynamic therapy (PDT) employing exogenous photosensitizers is currently being approved for treatment of basal cell carcinoma (BCC). 2-(4-Aminophenyl)benzothiazoles (6) consist of chromophoric structure and absorb light in the UVA (315-400 nm). These results encouraged us to design and synthesize a diversity of 2-phenylbenzothiazoles (6). Studies on the apoptotic mechanism involved in photosensitive effects induced by UVA-activated 6 in BCC cells are carried out in the present article. 6-UVA-treated cells displayed several features of apoptosis, including an increase in the sub-G1 population, a significantly increased annexin V binding, and activation of caspase-3. 6-UVA induced a decrease in mitochondrial membrane potential (Deltapsi(mt)) and ATP via enhanced ROS generation and promoted phosphorylation of extracellular signal-regulated kinase (ERK) and p38 MAPK expression. These results suggest that 6-UVA elicits photosensitive effects in mitochondria processes which involve ERK and p38 activation, and ultimately lead to BCC cell apoptosis.

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Citations

Aug 16, 2014·European Journal of Medicinal Chemistry·Moustafa T GabrMohamed M El-Kerdawy
Sep 10, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·Leyla YurttaşSeref Demirayak
Apr 13, 2012·Expert Opinion on Investigational Drugs·Kamal AhmedKashi Reddy Methuku
Oct 4, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Prabodh Chander SharmaDharam Pal Pathak
Jul 11, 2019·Mini Reviews in Medicinal Chemistry·Nandini PathakC Mallikarjuna Rao
Feb 16, 2021·Nucleosides, Nucleotides & Nucleic Acids·Surajit HansdaRita Ghosh
Sep 19, 2020·Heliyon·Surajit HansdaRita Ghosh
Jul 30, 2014·The Journal of Organic Chemistry·Agnieszka BodziochGreta Utecht

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