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Cytochromes P450 and drug resistance (1993)

Doehmer, Johannes ; Goeptar, Arnold R. ; Vermeulen, Nico P. E.

Springer

Cytotechnology 12 (1993), S. 357-366

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ISSN: 1573-0778

Keywords: anticancer drugs ; cytochrome P450 ; drug resistance ; metabolic activation

Source: Springer Online Journal Archives 1860-2000

Topics: Biology , Medicine , Process Engineering, Biotechnology, Nutrition Technology

Notes: Abstract Cytochromes P450 are the key enzymes for activating and inactivating many drugs, in particular anticancer drugs. Therefore, individual expression levels of cytochromes P450 may play a crucial role in drug safety and drug efficacy. Overexpression of cytochrome P450 may yield rapid turnover and elimination of drugs before the target site was reached and any pharmacological effect is observed. Therefore, it may be vital to know the individual cytochrome P450 status in order to select the appropriate drug before drug resistance occurs. Expression levels and activity of cytochromes P450 depend on many different factors. These factors include tissue and organ specific expression, sex- and age-dependent expression, genetic differences yielding polymorphic forms, competitive inhibition or induction of cytochromes P450 due to multiple drug interaction, nutrition and diet. Genetically engineered test cells defined for cytochromes P450 are available for studying drugs for metabolic activation and for identifying the metabolically competent cytochrome P450 isoform.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1007/BF00744673

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Modellversuche zur Synthese von Anhydrogliotoxin-Analoga: Eine bequeme Synthese von Thiazoloindolon-Derivaten (1974)

Ottenheijim, Harry C. J. ; Vermeulen, Nico P. E. ; Breuer, Leon F. J. M.

Weinheim : Wiley-Blackwell

Liebigs Annalen 1974 (1974), S. 206-212

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ISSN: 0075-4617

Keywords: Chemistry ; Organic Chemistry

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Chemistry and Pharmacology

Description / Table of Contents: Model Experiments for the Synthesis of Anhydrogliotoxin Analogs: A Convenient Synthesis of Thiazoloindolone DerivativesThe addition of thioglycolic acid (11, R=H) or 2-mercaptopropionic acid (12, R=H) to ethyl 2-ethoxycarbonyl-3,3-dimethylindolenine (5) yields the hexahydrothiazolo[3,2-a]-indolones 6 and 14, respectively. When the ethyl ester 11 (R=C2H5) is used instead of the acid 11 (R = H), this reaction proceeds only in the presence of a trace of acid. - Compound 6 can be converted into the a,cw-dichlorosulfenyl chloride 18, which reacts quantitatively with ethanethiol to yield19. 3-Mercaptopropionic acid (21) reacts with 5 to yield 22. The conversions of 6 → 19 and 5 → 22 are model reactions for the synthesis of the seco-anhydrogliotoxin analog 20 and the dethiornethyleneanhydrogliotoxin analog 24, respectively. First attempts in this direction are discussed.

Notes: Die Addition von Thioglykolsäure (11, R = H) oder 2-Mercaptopropionsäure (12, R = H) am 2-Äthoxycarbonyl-3,3-dirnethylindolenin (5) führt zu den Hexahydrothiazolo[3,2-a]- indolonen 6 bzw. 14. Verwendet man statt der Säure 11 (R = H) deren Äthylester 11,/ (R=C2H5), so verläuft die Reaktion nur in Anwesenheit von Spuren einer Säure. - Die Verbindung 6 wird zum α,α-Dichlorsulfenylchlorid 18 umgesetzt, das mit Äthanthiol quantitativ unter Bildung von 19 reagiert. 3-Mercaptopropionsaure (21) reagiert mit 5 unter Bildung von 22. Die Umwandlungen von 6 in 19 und von 5 in 22 sind Modellreaktionen für die Synthese des seco-Anhydrogliotoxin-Analogons 20 bzw. des Desthiornethylenanhydrogliotoxin-Analogons 24. Erste Versuche dazu werden diskutiert.