Discovery of Potent Antagonists of the Antiapoptotic Protein XIAP for the Treatment of Cancer was written by Oost, Thorsten K.;Sun, Chaohong;Armstrong, Robert C.;Al-Assaad, Ali-Samer;Betz, Stephen F.;Deckwerth, Thomas L.;Ding, Hong;Elmore, Steven W.;Meadows, Robert P.;Olejniczak, Edward T.;Oleksijew, Andrew;Oltersdorf, Tilman;Rosenberg, Saul H.;Shoemaker, Alexander R.;Tomaselli, Kevin J.;Zou, Hua;Fesik, Stephen W.. And the article was included in Journal of Medicinal Chemistry in 2004.Reference of 86069-86-5 The following contents are mentioned in the article:
Inhibitor of apoptosis (IAP) proteins are overexpressed in many cancers and have been implicated in tumor growth, pathogenesis, and resistance to chemo- or radiotherapy. On the basis of the NMR structure of a SMAC peptide complexed with the BIR3 domain of X-linked IAP (XIAP), a novel series of XIAP antagonists was discovered. The most potent compounds in this series bind to the baculovirus IAP repeat 3 (BIR3) domain of XIAP with single-digit nanomolar affinity and promote cell death in several human cancer cell lines. In a MDA-MB-231 breast cancer mouse xenograft model, these XIAP antagonists inhibited the growth of tumors. Close structural analogs that showed only weak binding to the XIAP-BIR3 domain were inactive in the cellular assays and showed only marginal in vivo activity. Our results are consistent with a mechanism in which ligands for the BIR3 domain of XIAP induce apoptosis by freeing up caspases. The present study validates the BIR3 domain of XIAP as a target and supports the use of small mol. XIAP antagonists as a potential therapy for cancers that overexpress XIAP. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Reference of 86069-86-5).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Reference of 86069-86-5
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem