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Zusammenfassung
Cytostatic Cl2Pt(NH2CHRCO2R1)2 (I) (R = H or a group derived from biol. acceptable amino acids and R1 = C>2 alkyl or hydroxy-substituted group) with low toxicity and a strong antitumor effect are prepd. by reaction of II with alcs. (R1OH) and HCl or by treatment of K2PtCl4 with amino acid ester hydrochlorides. The in vitro ED50 of I (R = H, R1 = Et) [82474-52-0], I (R = H, R1 = Bu) [82474-53-1], ...
Zusammenfassung
Cytostatic Cl2Pt(NH2CHRCO2R1)2 (I) (R = H or a group derived from biol. acceptable amino acids and R1 = C>2 alkyl or hydroxy-substituted group) with low toxicity and a strong antitumor effect are prepd. by reaction of II with alcs. (R1OH) and HCl or by treatment of K2PtCl4 with amino acid ester hydrochlorides. The in vitro ED50 of I (R = H, R1 = Et) [82474-52-0], I (R = H, R1 = Bu) [82474-53-1], and I (R = H, R1 = tert-Bu) [82474-54-2] against hormone-dependent human MDA-MB 231 mammary carcinoma cell culture were 1.0 * 10-5, 2.8 * 10-6, and 5.0 * 10-6M, resp. These complexes were as active as the free carboxylic acid contg. complexes, cis-PtCl2(NH2CHRCO2H)2.
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