indole series
Recently Published Documents


TOTAL DOCUMENTS

164
(FIVE YEARS 3)

H-INDEX

23
(FIVE YEARS 1)

Author(s):  
Abdelmadjid Benmohammed ◽  
Nawel Rekiba ◽  
Yassine Sehanine ◽  
Ahmed Amine Louail ◽  
Omar Khoumeri ◽  
...  

Marine Drugs ◽  
2020 ◽  
Vol 18 (4) ◽  
pp. 190 ◽  
Author(s):  
Wagdy M. Eldehna ◽  
Ghada S. Hassan ◽  
Sara T. Al-Rashood ◽  
Hamad M. Alkahtani ◽  
Abdulrahman A. Almehizia ◽  
...  

Diverse indoles and bis-indoles extracted from marine sources have been identified as promising anticancer leads. Herein, we designed and synthesized novel bis-indole series 7a–f and 9a–h as Topsentin and Nortopsentin analogs. Our design is based on replacing the heterocyclic spacer in the natural leads by a more flexible hydrazide linker while sparing the two peripheral indole rings. All the synthesized bis-indoles were examined for their antiproliferative action against human breast cancer (MCF-7 and MDA-MB-231) cell lines. The most potent congeners 7e and 9a against MCF-7 cells (IC50 = 0.44 ± 0.01 and 1.28 ± 0.04 μM, respectively) induced apoptosis in MCF-7 cells (23.7-, and 16.8-fold increase in the total apoptosis percentage) as evident by the externalization of plasma membrane phosphatidylserine detected by Annexin V-FITC/PI assay. This evidence was supported by the Bax/Bcl-2 ratio augmentation (18.65- and 11.1-fold compared to control) with a concomitant increase in the level of caspase-3 (11.7- and 9.5-fold) and p53 (15.4- and 11.75-fold). Both compounds arrested the cell cycle mainly in the G2/M phase. Furthermore, 7e and 9a displayed good selectivity toward tumor cells (S.I. = 38.7 and 18.3), upon testing of their cytotoxicity toward non-tumorigenic breast MCF-10A cells. Finally, compounds 7a, 7b, 7d, 7e, and 9a were examined for their plausible CDK2 inhibitory action. The obtained results (% inhibition range: 16%–58%) unveiled incompetence of the target bis-indoles to inhibit CDK2 significantly. Collectively, these results suggested that herein reported bis-indoles are good lead compounds for further optimization and development as potential efficient anti-breast cancer drugs.


2019 ◽  
Vol 89 (5) ◽  
pp. 870-880
Author(s):  
R. I. Baichurin ◽  
A. A. Fedorushchenko ◽  
N. I. Aboskalova ◽  
L. V. Baichurina ◽  
A. V. Felgendler ◽  
...  
Keyword(s):  

2018 ◽  
Vol 88 (5) ◽  
pp. 962-967
Author(s):  
N. I. Vikrishchuk ◽  
L. D. Popov ◽  
G. S. Borodkin ◽  
A. Yu. Dranikova ◽  
M. E. Kletskii ◽  
...  

2013 ◽  
Vol 47 (3) ◽  
pp. 125-129 ◽  
Author(s):  
K. F. Suzdalev ◽  
A. A. Spasov ◽  
D. S. Yakovlev ◽  
V. A. Kosolapov ◽  
A. F. Kucheryavenko ◽  
...  

2012 ◽  
Vol 22 (13) ◽  
pp. 4431-4436 ◽  
Author(s):  
David McGowan ◽  
Sandrine Vendeville ◽  
Tse-I Lin ◽  
Abdellah Tahri ◽  
Lili Hu ◽  
...  

ChemInform ◽  
2011 ◽  
Vol 42 (6) ◽  
pp. no-no
Author(s):  
Jan Bergman ◽  
Ivan Romero
Keyword(s):  

ChemInform ◽  
2010 ◽  
Vol 23 (21) ◽  
pp. no-no
Author(s):  
V. LEVACHER ◽  
N. BOUSSAD ◽  
G. DUPAS ◽  
J. BOURGUIGNON ◽  
G. QUEGUINER
Keyword(s):  

Sign in / Sign up

Export Citation Format

Share Document