Synthesis and biological evaluation of novel N⁹-heterobivalent β-carbolines as angiogenesis inhibitors.

ABSTRACT: A series of novel N⁹-heterobivalent β-carbolines has been synthesized. All the novel compounds were tested for their anticancer activity against six tumour cell lines in vitro. Among these molecules, compounds 5b, and 5w exhibited strong cytotoxic activities with IC₅₀ value of lower than 20 μM. Acute toxicities and antitumor efficacies of the selected compounds in mice were also evaluated, compounds 5b and 5w exhibited that tumour inhibition rate of over 40% in the Sarcoma 180 and Lewis lung cancer animal models. Preliminary structure-activity relationships (SARs) analysis indicated that: (1) C¹-methylation and C⁷-methoxylation were favorable for increased activities; (2) 3-Pyridyl or 2-thienyl group substituent into position-1 of the β-carboline

SUBMITTER: Guo L 

PROVIDER: S-EPMC6327987 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature