New pyridine and chromene scaffolds as potent vasorelaxant and anticancer agents.

ABSTRACT: Based on studies that have reported the association between cancer and cardiovascular diseases, new series of pyridine- (3a-o) and/or chromene- (4a-e) carbonitrile analogous were designed, synthesized and screened for their vasodilation and cytotoxic properties. The majority of the new chemical entities demonstrated significant vasodilation efficacies, compounds 3a, 3h, 3j, 3m, 3o, 4d and 4e exhibited the most promising potency with IC₅₀ = 437.9, 481.0, 484.5, 444.8, 312.1, 427.6 and 417.2 μM, respectively, exceeding prazosin hydrochloride (IC₅₀ = 487.3 μM). Compounds 3b-e, 3k and 3l also, revealed moderate vasodilation activity with IC₅₀ values ranging from 489.7 to 584.5 μM. In addition, the anti-proliferative activity evaluation of the experimental compo

SUBMITTER: Dawood DH 

PROVIDER: S-EPMC9040659 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature