Mimicry of sorafenib: novel diarylureas as VEGFR2 inhibitors and apoptosis inducers in breast cancer

In this present study, new chalcone derivatives were synthesized from 4-aminoacetophenone, which were confirmed by spectroscopic methods. The toxic risks of chalcones to humans and the environment were investigated by a web-based platform called ADMETlab. With this program, the possible toxic effects of the compounds on liver, respiratory system, and eyes were evaluated. For the topical insecticidal activity, adult female Caribbean fruit fly, Anastrepha suspensa, was targeted. Results of the toxicity tests showed that chalcone derivatives are effective against female A. suspensa. Among the synthesized chalcones, 1-(4-cinnamoylphenyl)-3-(p-tolyl)urea (2) exhibited the greatest insecticidal activity, resulting in 73 % mortality at 100 µg/fly after 24 h, whereas other derivatives showed less than 30 % mortality. Our results demonstrate that insecticidal activity may be modulated by the presence of a certain phenyl ring in the structure of derivative 2 and, therefore, has potential for design of efficient chemicals for tephritid fruit fly management.

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Mimicry of sorafenib: novel diarylureas as VEGFR2 inhibitors and apoptosis inducers in breast cancer

Abstract: Thirteen diarylurea derivatives were designed and synthesized as sorafenib mimetics.

Cited by 3 publications

References 45 publications

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Insecticidal effect of new synthesized chalcone derivatives on Caribbean fruit fly, Anastrepha suspensa

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