Synthesis and SAR of novel capsazepine analogs with significant anti-cancer effects in multiple cancer types

Autor:	Jorge J. De La Chapa, Cara B. Gonzales, Srikanth R. Polusani, Stanton F. McHardy, Matthew Hart, Wes Mitchell, Franscisco Ruiz, Keith Gonzales, Matthew C. Valdez
Rok vydání:	2018
Předmět:	Clinical Biochemistry TRPV1 Pharmaceutical Science Mice Nude TRPV Cation Channels Antineoplastic Agents 01 natural sciences Biochemistry HeLa chemistry.chemical_compound Structure-Activity Relationship In vivo Cell Line Tumor Neoplasms Drug Discovery medicine Animals Humans Viability assay Molecular Biology Cell Proliferation biology Molecular Structure 010405 organic chemistry Organic Chemistry Antagonist Cancer medicine.disease biology.organism_classification Xenograft Model Antitumor Assays 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry Cancer research Molecular Medicine Female Pharmacophore Capsaicin Capsazepine
Zdroj:	Bioorganicmedicinal chemistry. 27(1)
ISSN:	1464-3391
Popis:	We previously demonstrated that capsazepine (CPZ), a synthetic transient receptor potential Vanilloid subtype 1 (TRPV1) antagonist, has significant anti-cancer effects in vivo. The purpose of this study was to develop more potent analogs based upon CPZ pharmacophore and structure–activity relationships (SAR) across analogs. We generated 30 novel compounds and screened for their anti-proliferative effects in cultured HeLa cervical cancer cells. Cell viability assays identified multiple compounds with IC50s
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1545938d90654e6d3972f00b6d91f1e5 https://pubmed.ncbi.nlm.nih.gov/31014563 Zobrazit plný text záznamu Full Text from ScienceDirect