1025423-97-5Relevant articles and documents
Synthesis and SAR of novel capsazepine analogs with significant anti-cancer effects in multiple cancer types
Chapa, Jorge De La,Valdez, Matthew,Ruiz, Franscisco,Gonzales, Keith,Mitchell, Wes,McHardy, Stanton F.,Hart, Matthew,Polusani, Srikanth R.,Gonzales, Cara B.
, p. 208 - 215 (2018/12/11)
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 50 50s of 1–2.5 μM in HSC-3and PC-3cells. Thus, we propose that these novel CPZ analogs may serve as efficacious therapeutic agents against multiple tumor types that warrant further development for clinical application.