cis-chloroethylnitrosourea

cis-chloroethylnitrosourea is a member of the **chloroethylnitrosourea (CENU) class**, a group of alkylating agents used as antineoplastic (anticancer) drugs. These compounds exert their cytotoxic effects through **alkylation of DNA, particularly by inducing DNA interstrand cross-links (ICLs)**, which cause inhibition of DNA replication and transcription, ultimately leading to apoptosis (cell death) of cancer cells[1]. Like other CENU drugs, decomposition of cis-chloroethylnitrosourea generates a chloroethylating intermediate that attacks the O6 position of guanine bases in DNA, forming O6-chloroethylguanine, progressing to N1,O6-ethanoguanine and finally forming dG-dC cross-links. The primary clinical use of related CENUs includes treatment of brain tumors (e.g., gliomas, glioblastomas), malignant lymphomas, neurogliomas, and various solid tumors. However, resistance to these drugs often arises from increased cellular levels of the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (AGT), which counteracts their cross-linking effect[1].

Other names

cis-chloroethylnitrosourea