{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,25]],"date-time":"2026-06-25T15:58:17Z","timestamp":1782403097272,"version":"3.54.5"},"reference-count":74,"publisher":"MDPI AG","issue":"10","license":[{"start":{"date-parts":[[2021,9,27]],"date-time":"2021-09-27T00:00:00Z","timestamp":1632700800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceuticals"],"abstract":"<jats:p>A library of sulfonate and sulfonamide derivatives of Resveratrol was synthesized and tested for its aromatase inhibitory potential. Interestingly, sulfonate derivatives were found to be more active than sulfonamide bioisosteres with IC50 values in the low micromolar range. The sulfonate analogues 1b\u2013c and 1j exhibited good in vitro antiproliferative activity on the MCF7 cell line, evidenced by MTT and LDH release assays. Structure\u2013activity relationships suggested that electronic and lipophilic properties could have a different role in promoting the biological response for sulfonates and sulfonamides, respectively. Docking studies disclosed the main interactions at a molecular level of detail behind the observed inhibition of the more active compounds whose chemical stability has been evaluated with nano-liquid chromatography. Finally, 1b\u2013c and 1j were highlighted as sulfonates to be further developed as novel and original aromatase inhibitors.<\/jats:p>","DOI":"10.3390\/ph14100984","type":"journal-article","created":{"date-parts":[[2021,9,27]],"date-time":"2021-09-27T21:40:30Z","timestamp":1632778830000},"page":"984","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":31,"title":["Design, Synthesis and Biological Evaluation of Aromatase Inhibitors Based on Sulfonates and Sulfonamides of Resveratrol"],"prefix":"10.3390","volume":"14","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-2401-7547","authenticated-orcid":false,"given":"Marialuigia","family":"Fantacuzzi","sequence":"first","affiliation":[{"name":"Unit of Medicinal Chemistry, Department of Pharmacy, \u201cG. d\u2019Annunzio\u201d University, 66100 Chieti, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2283-4159","authenticated-orcid":false,"given":"Marialucia","family":"Gallorini","sequence":"additional","affiliation":[{"name":"Unit of Anatomy, Department of Pharmacy, \u201cG. d\u2019Annunzio\u201d University, 66100 Chieti, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1965-1519","authenticated-orcid":false,"given":"Nicola","family":"Gambacorta","sequence":"additional","affiliation":[{"name":"Unit of Medicinal Chemistry, Department of Pharmacy, \u201cA. Moro\u201d University, 70121 Bari, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4369-1772","authenticated-orcid":false,"given":"Alessandra","family":"Ammazzalorso","sequence":"additional","affiliation":[{"name":"Unit of Medicinal Chemistry, Department of Pharmacy, \u201cG. d\u2019Annunzio\u201d University, 66100 Chieti, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zeineb","family":"Aturki","sequence":"additional","affiliation":[{"name":"Institute for Biological Systems (ISB), Italian National Research Council, Monterotondo, 00015 Rome, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8042-6009","authenticated-orcid":false,"given":"Marwa","family":"Balaha","sequence":"additional","affiliation":[{"name":"Unit of Anatomy, Department of Pharmacy, \u201cG. d\u2019Annunzio\u201d University, 66100 Chieti, Italy"},{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Kafr El Sheikh 33516, Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8698-9440","authenticated-orcid":false,"given":"Simone","family":"Carradori","sequence":"additional","affiliation":[{"name":"Unit of Medicinal Chemistry, Department of Pharmacy, \u201cG. d\u2019Annunzio\u201d University, 66100 Chieti, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8483-1885","authenticated-orcid":false,"given":"Letizia","family":"Giampietro","sequence":"additional","affiliation":[{"name":"Unit of Medicinal Chemistry, Department of Pharmacy, \u201cG. d\u2019Annunzio\u201d University, 66100 Chieti, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2957-8650","authenticated-orcid":false,"given":"Cristina","family":"Maccallini","sequence":"additional","affiliation":[{"name":"Unit of Medicinal Chemistry, Department of Pharmacy, \u201cG. d\u2019Annunzio\u201d University, 66100 Chieti, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Amelia","family":"Cataldi","sequence":"additional","affiliation":[{"name":"Unit of Anatomy, Department of Pharmacy, \u201cG. d\u2019Annunzio\u201d University, 66100 Chieti, Italy"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6533-5539","authenticated-orcid":false,"given":"Orazio","family":"Nicolotti","sequence":"additional","affiliation":[{"name":"Unit of Medicinal Chemistry, Department of Pharmacy, \u201cA. 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