Partition coefficient determination of a series of isoindolines-2-substituted and its correlation with their antiproliferative activity on HeLa cells

2012 ◽  
Vol 22 (8) ◽  
pp. 4039-4045 ◽  
Author(s):  
Cynthia R. Trejo Muñoz ◽  
Teresa Mancilla Percino ◽  
Elvia Mera Jiménez ◽  
José Correa-Basurto ◽  
José G. Trujillo Ferrara
1985 ◽  
Vol 50 (8) ◽  
pp. 1642-1647 ◽  
Author(s):  
Štefan Baláž ◽  
Anton Kuchár ◽  
Ernest Šturdík ◽  
Michal Rosenberg ◽  
Ladislav Štibrányi ◽  
...  

The distribution kinetics of 35 2-furylethylene derivatives in two-phase system 1-octanol-water was investigated. The transport rate parameters in direction water-1-octanol (l1) and backwards (l2) are partition coefficient P = l1/l2 dependent according to equations l1 = logP - log(βP + 1) + const., l2 = -log(βP + 1) + const., const. = -5.600, β = 0.261. Importance of this finding for assesment of distribution of compounds under investigation in biosystems and also the suitability of the presented method for determination of partition coefficients are discussed.


1977 ◽  
Vol 182 (2) ◽  
pp. 556-562 ◽  
Author(s):  
John F. Tallman ◽  
Peter H. Fishman ◽  
Richard C. Henneberry

2021 ◽  
Author(s):  
Flaviano Melo Ottoni ◽  
Lucas Bonfim Marques ◽  
Juliana Martins Ribeiro ◽  
Lucas Lopardi Franco ◽  
José Dias Souza Filho ◽  
...  

Abstract Lapachol (1), a natural naphthoquinone, presents several biological activities including antitumor activity, used as anticancer coadjuvant whose use was abandoned because of adverse effects. Herein, we reported the synthesis and cytotoxicity evaluation against cancer cell lines of a series of Oglycosides and glycosyl triazoles derived from lapachol. In addition to the determination of IC50, the DNA fragmentation and clonogenicity were also evaluated. The glycoside derived from D-glucose (5) was far more active than lapachol (1) and more active in tumor cell lines HL60, Jurkat, THP-1 and MDA-MB-231 than to the non-tumoral PBMC cell line, indicating an improvement in activity and selectivity as compared with lapachol (1). Compound 5 and the glycosides derived from D-galactose (14), D-N-acetylglucosamine (15) and L-fucose (16) showed good results in the DNA fragmentation and clonogenicity assays in the studies of subdiploid DNA content, indicating a pro-apoptotic potential and a good antiproliferative activity of these glycosides.


Sign in / Sign up

Export Citation Format

Share Document