Synthesis of Benzophenones and in vitro Evaluation of Their Anticancer Potential in Breast and Prostate Cancer Cells

authors	Saidi, L; Rocha, DHA; Talhi, O; Bentarzi, Y; Nedjar-Kolli, B; Bachari, K; Paz, FAA; Helguero, LA; Silva, AMS
nationality	International
journal	CHEMMEDCHEM
author keywords	benzophenones; cancer; cytotoxicity; drug design; synthesis design
keywords	1,3-BIS-SILYL ENOL ETHERS; ALDOL REACTIONS; DERIVATIVES; INHIBITORS; XANTHONES; PYRIDINE; ANALOGS
abstract	Breast and prostate cancers are frequently treated with chemotherapy. Several novel chemicals are being reported for this purpose, particularly synthetic and natural benzophenones. This work reports the synthesis of substituted 2-hydroxybenzophenones through 1,4-conjugate addition/intramolecular cycloaddition/dehydration of nitromethane on key intermediate chromones. Structures were extensively studied by means of 2D NMR spectroscopy and single-crystal XRD. Their cytotoxicity was evaluated in vitro in two breast cancer cell lines (MDA-MB-231 and T47-D) and one prostate cancer cell line (PC3). The most potent compound exhibited good cytotoxic effects against the three cancer cell lines (IC50 values ranging from 12.09 to 26.49 mu m) and induced cell-cycle retardation only on prostate cancer cells, which suggested that it might exert cell-type-specific effects.
publisher	WILEY-V C H VERLAG GMBH
issn	1860-7179
isbn	1860-7187
year published	2019
volume	14
issue	10
beginning page	1041
ending page	1048
digital object identifier (doi)	10.1002/cmdc.201900127
web of science category	Chemistry, Medicinal; Pharmacology & Pharmacy
subject category	Pharmacology & Pharmacy
unique article identifier	WOS:000468773400007