2. Academic Validation
  3. Transformation of asiatic acid into a mitocanic, bimodal-acting rhodamine B conjugate of nanomolar cytotoxicity

Transformation of asiatic acid into a mitocanic, bimodal-acting rhodamine B conjugate of nanomolar cytotoxicity

  • Eur J Med Chem. 2018 Nov 5:159:143-148. doi: 10.1016/j.ejmech.2018.09.066.
Michael Kahnt 1,  Jana Wiemann 1,  Lucie Fischer 1,  Sven Sommerwerk 1,  René Csuk 2
Affiliations

Affiliations

  • 1 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany.
  • 2 Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120, Halle (Saale), Germany. Electronic address: rene.csuk@chemie.uni-halle.de.
PMID: 30278332 DOI: 10.1016/j.ejmech.2018.09.066
Abstract

Based on their biological activity Natural Products continue to represent optimal lead structures for the development of novel drug candidates. We focused on the syntheses of several derivatives of the triterpene asiatic acid and on the evaluation of their cytotoxic activity in a photometric sulforhodamin B assay. Especially, benzamide 2 and rhodamine B conjugate 11 show a distinct cytotoxicity for several human tumor cell lines, e.g. EC50 (A2780) = 110 ± 1 nM and EC50 (A2780) = 8 ± 2 nM, respectively. Interestingly, compound 11 showed for two human tumor cell lines (HT29 and 518A2) non-linear, bimodal dose-response relationships.

Keywords

Asiatic acid; Bimodal; Cytotoxicity; Mitocan; Rhodamine B; Triterpene.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z