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Synthesis of novel perillyl-dihydropyrimidinone hybrids designed for antiproliferative activity.

ABSTRACT: A series of fifteen novel dihydropyrimidinone hybrid compounds were synthesized in good yields via a multicomponent reaction combined with the Huisgen reaction. The antiproliferative activity was investigated against nine tumor cell lines, and four hybrid compounds (TGI < 10 ?M) showed promising antiproliferative activity against the tumor cell lines OVCAR-3 (ovarian), UACC-62 (melanoma) and U251 (glioma). Several hybrid compounds assayed have high TGI values (TGI 147.92-507.82) for the human keratinocyte cell line (HaCat), which reveals selectivity to cancer cells.

SUBMITTER: Vendrusculo V

PROVIDER: S-EPMC6151448 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature

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Synthesis of novel perillyl-dihydropyrimidinone hybrids designed for antiproliferative activity.

Vendrusculo Vinicius V de Souza Vanessa P VP M Fontoura Luiz Antônio LA M D'Oca Marcelo G MG Banzato Thais P TP Monteiro Paula A PA Pilli Ronaldo A RA de Carvalho João Ernesto JE Russowsky Dennis D

MedChemComm 20180731 9

A series of fifteen novel dihydropyrimidinone hybrid compounds were synthesized in good yields <i>via</i> a multicomponent reaction combined with the Huisgen reaction. The antiproliferative activity was investigated against nine tumor cell lines, and four hybrid compounds (TGI < 10 μM) showed promising antiproliferative activity against the tumor cell lines OVCAR-3 (ovarian), UACC-62 (melanoma) and U251 (glioma). Several hybrid compounds assayed have high TGI values (TGI 147.92-507.82) for the h ...[more]

PMID: 30288229

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