Novel unit B cryptophycin analogues as payloads for targeted therapy

Figueras Agustí E, Borbély AN, Ismail M, Frese M, Sewald N (2018)
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY 14: 1281-1286.

Zeitschriftenaufsatz | Veröffentlicht | Englisch
 
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Abstract / Bemerkung
Cryptophycins are naturally occurring cytotoxins with great potential for chemotherapy. Since targeted therapy provides new perspectives for treatment of cancer, new potent analogues of cytotoxic agents containing functional groups for conjugation to homing devices are required. We describe the design, synthesis and biological evaluation of three new unit B cryptophycin analogues. The O-methyl group of the unit B D-tyrosine analogue was replaced by an O-(allyloxyethyl) moiety, an O-(hydroxyethyl) group, or an O-(((azidoethoxy) ethoxy) ethoyxethyl) substituent. While the former two maintain cytotoxicity in the subnanomolar range, the attachment of the triethylene glycol spacer with a terminal azide results in a complete loss of activity. Docking studies of the novel cryptophycin analogues to beta-tubulin provided a rationale for the observed cytotoxicities.
Stichworte
cryptophycin; cytotoxic agents; novel payloads; tubulin inhibitors; tumour targeting
Erscheinungsjahr
2018
Zeitschriftentitel
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
Band
14
Seite(n)
1281-1286
ISSN
1860-5397
Page URI
https://pub.uni-bielefeld.de/record/2920953

Zitieren

Figueras Agustí E, Borbély AN, Ismail M, Frese M, Sewald N. Novel unit B cryptophycin analogues as payloads for targeted therapy. BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY. 2018;14:1281-1286.
Figueras Agustí, E., Borbély, A. N., Ismail, M., Frese, M., & Sewald, N. (2018). Novel unit B cryptophycin analogues as payloads for targeted therapy. BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, 14, 1281-1286. doi:10.3762/bjoc.14.109
Figueras Agustí, E., Borbély, A. N., Ismail, M., Frese, M., and Sewald, N. (2018). Novel unit B cryptophycin analogues as payloads for targeted therapy. BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY 14, 1281-1286.
Figueras Agustí, E., et al., 2018. Novel unit B cryptophycin analogues as payloads for targeted therapy. BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, 14, p 1281-1286.
E. Figueras Agustí, et al., “Novel unit B cryptophycin analogues as payloads for targeted therapy”, BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, vol. 14, 2018, pp. 1281-1286.
Figueras Agustí, E., Borbély, A.N., Ismail, M., Frese, M., Sewald, N.: Novel unit B cryptophycin analogues as payloads for targeted therapy. BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY. 14, 1281-1286 (2018).
Figueras Agustí, Eduard, Borbély, Adina Noémi, Ismail, Mohamed, Frese, Marcel, and Sewald, Norbert. “Novel unit B cryptophycin analogues as payloads for targeted therapy”. BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY 14 (2018): 1281-1286.

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