Developing multitarget coumarin based anti-breast cancer agents: synthesis and molecular modeling study.

ABSTRACT: A new series of 7-substituted coumarin scaffolds containing a methyl ester moiety at the C⁴-position were synthesized and tested for their in vitro anti-proliferative activity against MCF-7 and MDA-MB-231 breast cancer cell lines using Doxorubicin (DOX) as reference. Compounds 2 and 8 showed noticeable selectivity against MCF-7 with IC₅₀ = 6.0 and 5.8 µM, respectively compared to DOX with IC₅₀ = 5.6 µM. Compounds 10, 12, and 14 exhibited considerable selectivity against Estrogen Negative cells with IC₅₀ = 2.3, 3.5, and 1.9 µM, respectively) compared to DOX with (IC₅₀ = 7.3 µM). The most promising compounds were tested as epidermal growth factor receptor and aromatase (ARO) enzymes inhibitors using erlotinib and exemestane (EXM) as stan

SUBMITTER: Takla FN 

PROVIDER: S-EPMC10435442 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature