Cytotoxic analogs of luteinizing hormone-releasing hormone containing doxorubicin or 2-pyrrolinodoxorubicin, a derivative 500-1000 times more potent.
نویسندگان
چکیده
منابع مشابه
Targeted cytotoxic analogs of luteinizing hormone-releasing hormone: a reply.
We read with great interest the Highlight Review by Dr C GruÈ ndker entitled `Cytotoxic luteinizing hormonereleasing hormone conjugates and their use in gynecological cancer therapy' in the European Journal of Endocrinology (1). This excellent article provides a detailed description of recent developments in the field of targeted chemotherapy based on luteinizing hormone-releasing hormone (LH-R...
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To create cytotoxic hybrid analogs of somatostatin (SST), octapeptides RC-160 (D-Phe-Cys-Tyr-D-Trp- Lys-Val-Cys-Trp-NH2) and RC-121 (D-Phe-Cys-Tyr-D-Trp- Lys-Val-Cys-Thr-NH2) were linked to doxorubicin (DOX) or its superactive derivative, 2-pyrrolino-DOX (AN-201). The conjugation was performed by coupling N-9-fluorenylmethoxycarbonyl (N-Fmoc)-DOX-14-O-hemiglutarate or 2-pyrrolino-DOX-14-O-hemig...
متن کاملAnalogues of luteinizing hormone-releasing hormone containing cytotoxic groups.
In an attempt to produce better cytotoxic analogues, chemotherapeutic antineoplastic radicals including an alkylating nitrogen mustard derivative of D-phenylalanine (D-melphalan), reactive cyclopropane, anthraquinone derivatives [2-(hydroxymethyl)anthraquinone and the anticancer antibiotic doxorubicin], and an antimetabolite (methotrexate) were coupled to suitably modified agonists and antagoni...
متن کاملShort-chain analogs of luteinizing hormone-releasing hormone containing cytotoxic moieties.
Five hexapeptide and heptapeptide analogs of luteinizing hormone-releasing hormone (LH-RH) were synthesized for use as carriers for cytotoxic compounds. These short analogs were expected to enhance target selectivity of the antineoplastic agents linked to them. Native LH-RH-(3-9) and LH-RH-(4-9) containing D-lysine and D-ornithine at position 6 were amidated with ethylamine and acylated on the ...
متن کاملHigh yield conversion of doxorubicin to 2-pyrrolinodoxorubicin, an analog 500-1000 times more potent: structure-activity relationship of daunosamine-modified derivatives of doxorubicin.
A convenient, high yield conversion of doxorubicin to 3'-deamino-3'-(2''-pyrroline-1''-yl)doxorubicin is described. This daunosamine-modified analog of doxorubicin is 500-1000 times more active in vitro than doxorubicin. The conversion is effected by using a 30-fold excess of 4-iodobutyraldehyde in anhydrous dimethylformamide. The yield is higher than 85%. A homolog of this compound, 3'-deamino...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 1996
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.93.14.7269