Reference

Evaluation of cardiac subacute toxicity of epirubicin, chlorambucil, cisplatin, methotrexate and a homo-aza-steroid ester with antitumor activity in rats using serum biochemical parameters

Evaluation of cardiac subacute toxicity of epirubicin, chlorambucil, cisplatin, methotrexate and a homo-aza-steroid ester with antitumor activity in rats using serum biochemical parameters. Pispirigos, Kyriakos; Paradelis, Athanasios G.; Karakiulakis, George ( School Pharmacy, University Patras, Patras 26110, Greece). Arzneimittel-Forschung, 47(1), 92-96 (English) 1997 Cantor. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Cardiac subacute toxicity induced by the antineoplastic drugs epirubicin (CAS 56390-09-1), chlorambucil (CAS 305-03-3), cisplatin (CAS 15663-27-1), and methotrexate (CAS 59-05-2) and the steroid alkylating agent 3b-hydroxy-13a-amino-13,17-seco-5a-androstan-17-oic-13,17-lactam {p-[bis(2-chloroethyl)amino] phenyl} acetate was investigated in rats using serum biochem. parameters. Toxicol. evaluation was performed in serum samples following the administration of dose regimens of the agents that were previously shown to be effective in suppressing malignant tumor growth or to prolong survival in tumor-bearing animals. Cardiac subacute toxicity was evaluated by measuring serum enzyme activity of creatine kinase, creatine kinase isoenzyme-MB, lactate dehydrogenase, and aspartate aminotransferase. The use of the above serum biochem. parameters indicated that the cardiac subacute toxicity impact of the antitumor drugs was epirubicin >> methotrexate = chlorambucil = cisplatin > homo-aza-steroid ester.

Self-association of doxorubicin and related compounds in aqueous solution

Self-association of doxorubicin and related compounds in aqueous solution. Menozzi, Milena; Valentini, Luigi; Vannini, Elisabetta; Arcamone, Federico (Milan 20146, Italy). J. Pharm. Sci., 73(6), 766-70 (English) 1984. CODEN: JPMSAE. ISSN: 0022-3549. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 22, 33 The dimerization of doxorubicin-HCl (I-HCl) [25316-40-9], daunorubicin-HCl [23541-50-6], and their 4-demethoxy, 4'-epi, and 4'-deoxy analogs was studied spectrophotometrically. Self-assocn. was influenced by buffer compn. and ionic strength. Kd (Dimerization const.) values were 1.3 ′ 104 and 2.3 ′ 104 M-1 for doxorubicin and daunorubicin, resp., and ranged from 3.8 ′ 103-6.1 ′ 103 M-1 for the 4-demethoxy analogs. For 4'-epi- [56390-09-1] and 4'-deoxydoxorubicin-HCl [63521-85-7], tetramerization was also considered. On this basis, values of 2.0 ′ 104 and 2.2 ′ 104 M-1 were found, resp., for the formation const. of the dimerization process. Stability of the dimeric species appears to be strongly influenced by substitution of the chromophore moiety.