Synthesis, Chemistry, and Preliminary Pharmacology of Arsenical Nitrogen Mustards and Structurally Related Nonalkylating Arsenicals¹

The structure and reactivity of arsenic compounds: Biological activity and drug design

“…The stretching frequencies for the Group V-oxide, E=O bonds are 1195 and 880 cm-1 for E = P and E = As, respectively [161]. Infrared spectroscopy shows the absence of As=O in the arsenoso compounds [162]. The i.r.…”

“…I.r. data indicate [162] that the actual structure of the arsenoso compound involves di-tri-or tetrameric structures linked via As-O-As bridges rather than containing a formal As= O bond. The uncertainty in structure means that the magnitude of the toxicity figures for these and the arseno compounds should be interpreted with caution.…”

“…No direct correlation between As oxidation state and activity is apparent either. It has been proposed [162] that the observation that the compound RC6H4AsO [R=N(CH2CH2C1)2] is the most active is best explained by a mechanism of action involving a synergism between the alkylating ability of the R group and the SH-inhibition properties of As(Ill), i.e. the compound acts at two sites simultaneously.…”

“…Toxicity (~tmole/kg) and antitumour activity of arsenic nitrogen mustards and related compounds 1. Data from reference [162] Redrawn from Ref. [250].…”

Arsenic – Pesticides with an Ambivalent Character

“…It was efficient in various similar diseases such as relapsing fever, Vincent´s angina. Arsenic trioxide is also known as an anti-bacterial and anti-cancer agent (Bardos, tta-Gupta, and Hebborn 1966). Inorganic As has been also used pharmacologically for the treatment of eczema, pemphigus and psoriasis under the name of Fowler´s solution.…”