Synthesis and antitumor effects of novel benzyl naphthyl sulfoxide/sulfone derivatives derived from Rigosertib

Abstract

In this work, a series of novel benzyl naphthyl sulfoxides/sulfones derived from Rigosertib were designed and synthesized as potential antitumor agents.

Synthetic Approaches and Clinical Application of Representative Small-Molecule Inhibitors of Cyclin-Dependent Kinase for Cancer Therapy

“…Rigosertib Sodium, an experimental drug being developed by Onconova Therapeutics, Inc., is currently undergoing Phase III clinical trials. Its primary focus lies in the treatment of refractory anemia with excess blasts and chronic myelomonocytic leukemia (CML), showcasing its potential as a promising antineoplastic agent [69]. When administered, Rigosertib specifically targets and attaches to the Ras-binding domain (RBD) that is present in various Ras effector proteins, such as Raf kinase and phosphatidylinositol 3kinase (PI3K).…”

Recent trends in the synthesis and applications of β-iodovinyl sulfones: a decade of progress

“…6 Various resulting vinyl sulfone analogues exhibit a wide range of promising biological activities (Fig. 1), for instance, a neuroprotective (nrf2) agent ( A ) 7 for remedial Parkinson's disease, a Chagas agent ( B ) 8 used as an antiparasitic drug, Recilisib sodium ( C ) 9 is an antitumor agent, Rigosertib ( D ) 10 is a promising anticancer (phase III stage) drug candidate, and K11017 ( E ) 11 is a cysteine protease inhibitor.…”