Detail of "107-99-3"

Reference

4-[Benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds as selective H1-histamine receptor antagonists

4-[Benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds as selective H1-histamine receptor antagonists. Mossini, F.; Maggiali, C.; Morini, G.; Impicciatore, M.; Morini, G.; Molina, E.Chemicals with cas numbers 90042-88-9 and 91-85-0 also play role. (Ist. Chim. Farm. Tossicol., Univ. Parma, Parma, Italy). Farmaco, Ed. Sci., 39(3), 189-99 (Italian) 1984. CODEN: FRPSAX. ISSN: 0430-0920. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 28 4-[Benzyl-(2-dimethylaminoethyl)amino]pyrimidine (I) [90042-86-7] and 4-[p-methoxybenzyl-(2-dimethylaminoethyl)amino]pyrimidine (II) [90042-87-8], as well as the corresponding 2-position isomers with known antihistaminic activity, Hetramine (III) [531-08-8] and Neohetramine (IV) [91-85-0], were prepd. from 2,4,6-trichloropyrimdine [3764-01-0] by reaction with the appropriate benzylamine to give the isomeric 4- and 2-substituted derivs., removal of the remaining 2 Cl atoms, and reaction with (2-chloroethyl)dimethylamine [107-99-3]. Tests on the isolated guinea pig ileum showed I-IV to be selective H-antihistaminics. The most active compd. was II (8-10-fold more active than IV). The compds. with R = OMe had a higher affinity for the histamine receptor sites that those with R = H. .

Mutagenic and chemotherapeutic activity in L1210 leukemia of several monofunctional alkylating agents

Mutagenic and chemotherapeutic activity in L1210 leukemia of several monofunctional alkylating agents. Schmid, Franz A.; Otter, Glenys M.; Mehta, Bipin M. (Mem. Sloan-Kettering Cancer Cent., New York, NY 10021, USA). Cancer Res., 45(1), 40-4 (English) 1985. CODEN: CNREA8. ISSN: 0008-5472. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The mutagenic and chemotherapeutic activities of the following monofunctional alkylating agents were compared in vivo: b-chloroethylamine [689-98-5], dimethyl- [107-99-3] and diethylaminoethyl chloride [100-35-6]; methyl- [66-27-3] and ethylmethanesulfonate [62-50-0]; methyl- [684-93-5] and ethylnitrosourea [759-73-9]; and procarbazine [671-16-9]. The bifunctional alkylating agent diethylamine 2,2'-dichloro-N-methyl-hydrochloride was used as ref. The alkylating activity was assessed by reacting with 4-(p-nitrobenzyl)pyridine, and antitumor activity was detd. against L1210 in vitro and in vivo. The L1210 response, which is consistent with useful alkylating reactivity, was very marked with the 2 nitrosoureas and procarbazine. The nitrosoureas and, to some extent, procarbazine decreased the tumorigenicity of L1210 leukemia as evidenced by the increase in survival times with increasing nos. of treatment generations. After treatment for about five transfers (106 cells i.p.) with met hylnitrosourea (40 mg/kg, i.p., on Days 1, 3, and 5), the untreated control mice consistently survived free of tumor, whereas the treated mice died before Day 30. After treatment with ethylnitrosourea (80 mg/kg), the survival times also increased but more in the treated than in the corresponding control groups. Methylnitrosourea was most efficient in increasing the survival times and abolishing tumor transplantability. Antigenic change and loss of growth potential presumably were the reason for this increase in survival time, as indicated by tests in X-irradiated and nude mice. The fact that nitrosoureas and triazenes, besides reducing tumorigenicity, have similarities in their chem. in that they decomp. or are metabolically converted into diazohydroxides and then to carbonium ions is possibly of significance. That these alkylating agents may inhibit tumor growth through their mutagenic activity is discussed.