Design and synthesis of novel multi-target tetrabromophthalimides as CBS and Topo-II inhibitors and DNA intercalators.

ABSTRACT: Microtubules are highly dynamic structures and constitute a crucial component of the cellular cytoskeleton. Besides, topoisomerases (Topo) play a fundamental role in maintaining the appropriate structure and organization of DNA. On the other hand, dual mechanism drug candidates for cancer treatment primarily aim to enhance the efficacy of cancer treatment and potentially overcome drug resistance. Hence, this work was tailored to design and synthesize new multi-target tetrabromophthalimide derivatives (2a-2k) that are capable of inhibiting the colchicine binding site (CBS) and topoisomerase II (Topo-II). The conducted in vitro studies showed that compound 2f showed the lowest IC₅₀ value (6.7 μg mL^-1) against the MDA-MB-468 cancer cell line. Additionally, compoun

SUBMITTER: Abdel-Motaal M 

PROVIDER: S-EPMC11403875 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature