Design of DNA Intercalators Based on 4-Carboranyl-1,8-Naphthalimides: Investigation of Their DNA-Binding Ability and Anticancer Activity.

ABSTRACT: In the present study, we continue our work related to the synthesis of 1,8-naphthalimide and carborane conjugates and the investigation of their anticancer activity and DNA-binding ability. For this purpose, a series of 4-carboranyl-1,8-naphthalimide derivatives, mitonafide, and pinafide analogs were synthesized using click chemistry, reductive amination, amidation, and Mitsunobu reactions. The calf thymus DNA (ct-DNA)-binding properties of the synthesized compounds were investigated by circular dichroism (CD), UV-vis spectroscopy, and thermal denaturation experiments. Conjugates 54-61 interacted very strongly with ct-DNA (∆T_m = 7.67-12.33 °C), suggesting their intercalation with DNA. They were also investigated for their in vitro effects on cytotoxicity, ce

SUBMITTER: Rykowski S 

PROVIDER: S-EPMC9101373 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature