{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,27]],"date-time":"2026-04-27T19:09:10Z","timestamp":1777316950270,"version":"3.51.4"},"reference-count":26,"publisher":"MDPI AG","issue":"20","license":[{"start":{"date-parts":[[2025,10,10]],"date-time":"2025-10-10T00:00:00Z","timestamp":1760054400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/100009326","name":"Cancer Research Society","doi-asserted-by":"publisher","award":["22471"],"award-info":[{"award-number":["22471"]}],"id":[{"id":"10.13039\/100009326","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100000024","name":"Canadian Institutes of Health Research","doi-asserted-by":"publisher","award":["392334"],"award-info":[{"award-number":["392334"]}],"id":[{"id":"10.13039\/501100000024","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Aligo Innovation","award":["150923"],"award-info":[{"award-number":["150923"]}]},{"name":"\u201cMinist\u00e8re de l\u2019\u00c9conomie et de l\u2019Innovation\u201d, Qu\u00e9bec Government"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>The design of innovative compounds displaying anti-inflammatory activity in oncological context is a subject of great interest in drug development. It has been proved that a pro-inflammatory microenvironment which accelerates cancer growth and cellular differentiation is often present in malignant bladder tumor. In earlier work, we reported the synthesis of p-aminobenzoic acid derivatives that act as anti-inflammatory compounds able to inhibit the pro-inflammatory markers present in bladder cancer microenvironment. DAB-1 rapidly emerged as an effective lead candidate in this investigation, with its ability to shrink by 90% in 25 days the size of human bladder cancer tumors in an ectopic mouse model. This manuscript discloses the synthesis of 23 new hydrazide derivatives of DAB-1 and reports their in vitro and in vivo biological evaluation. It was discovered that most of the new compounds are essentially nontoxic against RAW 264.7 cells, as evaluated by an MTT assay. Anti-inflammatory activity of the new derivatives was investigated by evaluation of their impact on cellular nitric oxide production, measured by a Griess assay. Some compounds did significatively inhibit nitric oxide production much more effectively than the original DAB-1. Striking activity of 14, which is around four times more potent than DAB-1, promotes this derivative as new lead compound in this study. The study of these analogs reveals that a phenolic\/anisole core is a key component to achieve high biological activity. Furthermore, mice models of acute inflammation and invasive BCa tumors were used to assess the in vivo impact of derivative 14, and it was found that this compound does reduce inflammation in these mice, possess similar anti-inflammatory activity but higher anti-tumoral activity compared to DAB-1 with no apparent signs of toxicity.<\/jats:p>","DOI":"10.3390\/molecules30204035","type":"journal-article","created":{"date-parts":[[2025,10,10]],"date-time":"2025-10-10T12:32:47Z","timestamp":1760099567000},"page":"4035","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Exploring the Synthesis, Anti-Inflammatory and Anti-Tumor Potential of 4-Maleimidylphenyl-Hydrazide Derivatives"],"prefix":"10.3390","volume":"30","author":[{"given":"Francis","family":"Cloutier","sequence":"first","affiliation":[{"name":"Laboratoire de Recherche en Chimie M\u00e9dicinale (LRCM) et Groupe de Recherche en Signalisation Cellulaire (GRSC), D\u00e9partement de Chimie, Biochimie et Physique, Universit\u00e9 du Qu\u00e9bec \u00e0 Trois-Rivi\u00e8res, Trois-Rivi\u00e8res, QC G8Z 4M3, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4714-2041","authenticated-orcid":false,"given":"Alexis","family":"Paquin","sequence":"additional","affiliation":[{"name":"Laboratoire de Recherche en Chimie M\u00e9dicinale (LRCM) et Groupe de Recherche en Signalisation Cellulaire (GRSC), D\u00e9partement de Chimie, Biochimie et Physique, Universit\u00e9 du Qu\u00e9bec \u00e0 Trois-Rivi\u00e8res, Trois-Rivi\u00e8res, QC G8Z 4M3, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maude","family":"Cloutier","sequence":"additional","affiliation":[{"name":"Laboratoire de Recherche en Chimie M\u00e9dicinale (LRCM) et Groupe de Recherche en Signalisation Cellulaire (GRSC), D\u00e9partement de Chimie, Biochimie et Physique, Universit\u00e9 du Qu\u00e9bec \u00e0 Trois-Rivi\u00e8res, Trois-Rivi\u00e8res, QC G8Z 4M3, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yassine","family":"Oufqir","sequence":"additional","affiliation":[{"name":"Laboratoire de Recherche en Oncologie et Immunobiologie (LROI) et Groupe de Recherche en Signalisation Cellulaire (GRSC), D\u00e9partement de Biologie M\u00e9dicale, Universit\u00e9 du Qu\u00e9bec \u00e0 Trois-Rivi\u00e8res, Trois-Rivi\u00e8res, QC G8Z 4M3, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4550-6075","authenticated-orcid":false,"given":"Laurie","family":"Fortin","sequence":"additional","affiliation":[{"name":"Laboratoire de Recherche en Oncologie et Immunobiologie (LROI) et Groupe de Recherche en Signalisation Cellulaire (GRSC), D\u00e9partement de Biologie M\u00e9dicale, Universit\u00e9 du Qu\u00e9bec \u00e0 Trois-Rivi\u00e8res, Trois-Rivi\u00e8res, QC G8Z 4M3, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Julie","family":"Girouard","sequence":"additional","affiliation":[{"name":"Laboratoire de Recherche en Oncologie et Immunobiologie (LROI) et Groupe de Recherche en Signalisation Cellulaire (GRSC), D\u00e9partement de Biologie M\u00e9dicale, Universit\u00e9 du Qu\u00e9bec \u00e0 Trois-Rivi\u00e8res, Trois-Rivi\u00e8res, QC G8Z 4M3, Canada"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Heidar-Ali","family":"Tajmir-Riahi","sequence":"additional","affiliation":[{"name":"Laboratoire de Recherche en Chimie M\u00e9dicinale (LRCM) et Groupe de Recherche en Signalisation Cellulaire (GRSC), D\u00e9partement de Chimie, Biochimie et Physique, Universit\u00e9 du Qu\u00e9bec \u00e0 Trois-Rivi\u00e8res, Trois-Rivi\u00e8res, QC G8Z 4M3, 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