10477-72-2Relevant articles and documents
Synthesis of androstene oxime-nitrogen mustard bioconjugates as potent antineoplastic agents
Acharya, Pratap Chandra,Bansal, Ranju
, p. 73 - 83 (2017)
In the present study, synthesis and antineoplastic activity of phenylacetic acid and benzoic acid nitrogen mustard conjugates of various steroidal oximes are reported for the first time. The conjugation was achieved through a more stable oxime-ester linkage and the resulting newly synthesized conjugates were evaluated in vitro on various human cancer cell lines for cytotoxicity. The extent of their alkylating activity was investigated by the in vitro colorimetric 4-(p-nitrobenzyl)pyridine (NBP) assay. The 17E-steroidal oxime-benzoic acid mustard ester 3β-acetoxy-17E-[p-(N,N-bis(2-chloroethyl)amino)]benzoyloxyimino-androst-5-ene (8) emerged as the most potent conjugate having significant cytotoxicity on most of the NCI 60-cell lines. Outstanding growth inhibition was observed on the IGROV1 ovarian cancer cell line with GI50?=?0.937?μM. In general, the D-ring derived androstene oxime-nitrogen mustard conjugates were found to possess better antineoplastic activity over a variety of cancer cells in comparison to those derived from other rings of the steroid skeleton.
Nitrogen Mustard Derivatives
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, (2014/10/16)
The disclosure includes compounds of Formula (1): wherein X1, X2, Q, Z, R1, and R2 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
Benzimidazole derivatives
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, (2008/06/13)
Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents. STR1