Detail of "81424-67-1"

Reference

Mutagenicity of the anticancer drug, caracemide, and related compounds for Salmonella

Mutagenicity of the anticancer drug, caracemide, and related compounds for Salmonella. Lee, Mei Sie; Lin, Ding Ping; Wang, Ching Yung (Dep. Chem. Carcinog., Michigan Cancer Found., Detroit, MI 48201, USA). Mutat.In this article, certain chemicals are used. One of their cas registry numbers is 106831-25-8 Res., 172(3), 199-209 (English) 1986. CODEN: MUREAV. ISSN: 0027-5107. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 23 Caracemide (I) [81424-67-1], is a novel anticancer drug. Since it was derived from acetohydroxamic acid (II) [546-88-3], a known mutagen, its potential metabolites and related compds. were synthesized and tested for mutagenicities in Salmonella typhimurium TA98 and TA100. These compds. were: MeNHCONH(OCONHMe) (III) [4543-63-9], MeCONH(OCONHMe) (IV) [104671-59-2], MeCONOH(CONHMe) (V) [106807-80-1], MeNHCOONH2 (VI) [42865-89-4], MeNHCONHOH (VII) [7433-46-7], MeNHCOON(CONHMe)2 (VIII) [24954-53-8], and NOH(CONHMe)2 (IX) [24966-35-6]. The mutagenicities in the absence of rat liver homogenate were: VI ? IV > II, III, V. The other compds. were not mutagenic. I was mutagenic only in the presence of rat liver homogenate. The concns. required to induce mutagenicities of these compds. were 0.05-5 mmol/plate. The major hydrolysis products at 25°, pH 7, were III, IV, and V from I; II and III from IV; and II, III, VII and MeNHCONH(OCOMe) [106807-79-8] from V. III was stable at pH 7. Treatment of IV with HCl yielded VI. Hydrolysis of III or V with ammonia yielded VII. These results suggest that caracemide may be activated enzymically or nonenzymically by deacetylation or decarbamoylation, and its anticancer activity may be related to the reactivity of its metabolites with DNA. .

Inhibition of ribonucleotide reductase by caracemide

Inhibition of ribonucleotide reductase by caracemide. Moore, E. Colleen; Loo, Ti Li (Cancer Cent., Univ. Texas, Houston, TX, USA). Cancer Treat. Rep., 68(10), 1293-4 (English) 1984. CODEN: CTRRDO. ISSN: 0361-5960. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Caracemide [81424-67-1], a new antitumor agent now in clin. trial, was tested against partially purified ribonucleotide reductase [9047-64-7] from rat Novikoff tumor. It was found to be an active inhibitor, about one-ninth as effective as hydroxyurea.