Synthesis of novel perillyl–dihydropyrimidinone hybrids designed for antiproliferative activity. Issue 9 (23rd August 2018)

• Record Type: Journal Article
• Authors: Vendrusculo, Vinicius; de Souza, Vanessa P.; M. Fontoura, Luiz Antônio; M. D'Oca, Marcelo G.; Banzato, Thais P.; Monteiro, Paula A.; Pilli, Ronaldo A.; de Carvalho, João Ernesto; Russowsky, Dennis
• Is Part Of: MedChemComm. Volume 9:Issue 9(2018)
• Page Start: 1553
• Page End: 1564
• Publication Date: 2018-08-23
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c8md00270c
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : A series of fifteen novel dihydropyrimidinone hybrid compounds were synthesized in good yields via a multicomponent reaction combined with the Huisgen reaction. 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 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 human keratinocyte cell line (HaCat), which reveals selectivity to cancer cells.