Structure–Cytotoxicity Relationships of Analogues of N14-Desacetoxytubulysin H

Autor:	Michael Howard Block, Jay Harper, Fengjiang Wang, Lakshmaiah Gingipalli, Dorin Toader, Melissa Vasbinder, Mark Roth, Vahe Bedian, Jianquo Ma, Shenlan Mao, Adeela Kamal, Sambaiah Thota, Mei Su
Rok vydání:	2016
Předmět:	N14-desacetoxytubulysin H 010405 organic chemistry Stereochemistry Chemistry Drug Discovery Molecular Medicine 010402 general chemistry Cytotoxicity 01 natural sciences 0104 chemical sciences
Zdroj:	Journal of Medicinal Chemistry. 59:10781-10787
ISSN:	1520-4804 0022-2623
Popis:	Herein we report structure–cytotoxicity relationships for analogues of N14-desacetoxytubulyisn H 1. A novel synthetic approach toward 1 enabled the discovery of compounds with a range of activity. Calculated basicity of the N-terminus of tubulysins was shown to be a good predictor of cytotoxicity. The impact of structural modifications at the C-terminus of 1 upon cytotoxicity is also described. These findings will facilitate the development of new tubulysin analogues for the treatment of cancer.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::19dbf215b81576a8aaefcc74e7c4d0a3 https://doi.org/10.1021/acs.jmedchem.6b01023 Zobrazit plný text záznamu