On the formation of steroidal amidoesters of 4-[N,N-bis(2-chloroethyl)amino]benzoic acid and their cytotoxic activity

The 4-[N,N-bis(2-chloroethyl)amino]benzoate of 17β-acetamido-5α-androstan-3β-ol, 17β-acetamido-5-androsten-3β-ol, 3β-acetamido-5α-androstan-17β-ol and 3α-acetamido-5β-androstan-17β-ol have been prepared and their antineoplastic effect evaluated against MIA Pa-Ca-2 pancreatic carcinoma, T47D breast c...

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Veröffentlicht in:	European journal of medicinal chemistry 1999-07, Vol.34 (7), p.645-649
Hauptverfasser:	Camoutsis, C, Sambani, C, Trafalis, D.T.P, Peristeris, P
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenocarcinoma - drug therapy Adenocarcinoma - pathology Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Biological and medical sciences Carcinoma - drug therapy Carcinoma - pathology Cell Division - drug effects cytotoxicity Esters - chemical synthesis Esters - pharmacology General aspects Humans Medical sciences MIA Pa-Ca-2, T47D, A431 cells MTT assay Pharmacology. Drug treatments Prednisolone - chemical synthesis Prednisolone - pharmacology steroidal 4-[N,N-bis(2-chloroethyl)amino]benzoate amidoesters Tumor Cells, Cultured
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Zusammenfassung:	The 4-[N,N-bis(2-chloroethyl)amino]benzoate of 17β-acetamido-5α-androstan-3β-ol, 17β-acetamido-5-androsten-3β-ol, 3β-acetamido-5α-androstan-17β-ol and 3α-acetamido-5β-androstan-17β-ol have been prepared and their antineoplastic effect evaluated against MIA Pa-Ca-2 pancreatic carcinoma, T47D breast carcinoma and A431 squamus cell carcinoma. Among the compounds tested, the compound 17β-acetamido-3β-hydroxy-5-androsten-4-[N, N-bis(2-chloroethyl)amino]benzoate appeared to possess a significant cytotoxic effect against A431 cells.
ISSN:	0223-5234 1768-3254
DOI:	10.1016/S0223-5234(00)80033-1