Boronated Conjugates of Protohemin IX with L-Amino Acids: Synthesis and Antitumor Activity

2007 ◽  
Vol 72 (12) ◽  
pp. 1707-1716
Author(s):  
Valentina A. Olshevskaya ◽  
Arina N. Savchenko ◽  
Alexander Yu. Gorshkov ◽  
Valentina N. Luzgina ◽  
Victor V. Tatarskii ◽  
...  

We report the synthesis of novel conjugates of protohemin IX with neutral and anionic boron polyhedra and L-amino acids. The amino acids are linked to the porphyrin macrocycle via the amide or ester bond. The serine containing boronated protohemin was the most cytotoxic for K562 human leukemia cell line. This compound interacted with double-stranded DNA in vitro and caused apoptosis of tumor cells including those that are resistant to several chemotherapeutic drugs.

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
L. I. Nagy ◽  
L. Z. Fehér ◽  
G. J. Szebeni ◽  
M. Gyuris ◽  
P. Sipos ◽  
...  

Combination therapy of bortezomib with other chemotherapeutics is an emerging treatment strategy. Since both curcumin and bortezomib inhibit NF-κB, we tested the effects of their combination on leukemia cells. To improve potency, a novel Mannich-type curcumin derivative, C-150, was synthesized. Curcumin and its analogue showed potent antiproliferative and apoptotic effects on the human leukemia cell line, HL60, with different potency but similar additive properties with bortezomib. Additive antiproliferative effects were correlated well with LPS-induced NF-κB inhibition results. Gene expression data on cell cycle and apoptosis related genes, obtained by high-throughput QPCR, showed that curcumin and its analogue act through similar signaling pathways. In correlation with in vitro results similar additive effect could be obsereved in SCID mice inoculated systemically with HL60 cells. C-150 in a liposomal formulation given intravenously in combination with bortezomib was more efficient than either of the drugs alone. As our novel curcumin analogue exerted anticancer effects in leukemic cells at submicromolar concentration in vitro and at 3 mg/kg dose in vivo, which was potentiated by bortezomib, it holds a great promise as a future therapeutic agent in the treatment of leukemia alone or in combination.


RSC Advances ◽  
2018 ◽  
Vol 8 (62) ◽  
pp. 35625-35639 ◽  
Author(s):  
Lotfali Saghatforoush ◽  
Keyvan Moeini ◽  
Seyed Abolfazl Hosseini-Yazdi ◽  
Zahra Mardani ◽  
Alireza Hajabbas-Farshchi ◽  
...  

A compartmental Schiff base ligand and its copper, cobalt and zinc complexes were prepared. Thein vitroactivities of all compounds against the human leukemia cell line K562 were investigated along with docking and DFT studies.


2015 ◽  
Vol 70 (3-4) ◽  
pp. 79-85 ◽  
Author(s):  
Mehmet Alp ◽  
A. Selen Gurkan-Alp ◽  
Tulin Ozkan ◽  
Asuman Sunguroglu

Abstract A series of novel 5-(4-methylpiperazin-1-yl)-2-phenyl-1H-benzimidazoles (5–14) were synthesized and evaluated for their in vitro antiproliferative activities against the human leukemia cell line HL-60. Compounds 5–7 and 10–12 exhibited potent antiproliferative activities against this cell line. The quantitative analysis of apoptosis by flow cytometry demonstrated that the percentages of apoptotic HL-60 cells treated with compounds 5 and 10–12 were significantly higher than in the control.


Leukemia ◽  
2000 ◽  
Vol 14 (2) ◽  
pp. 299-306 ◽  
Author(s):  
Y Nomura ◽  
O Inanami ◽  
K Takahashi ◽  
A Matsuda ◽  
M Kuwabara

1984 ◽  
Vol 89 (1) ◽  
pp. 122-131 ◽  
Author(s):  
Atsushi Komiyama ◽  
Yukiaki Miyagawa ◽  
Kohki Aoyama ◽  
Taro Akabane ◽  
Yoshio Uehara

1992 ◽  
Vol 7 (1-2) ◽  
pp. 157-164 ◽  
Author(s):  
Toshio Kakihara ◽  
Toshiyuki Yamada ◽  
Takeaki Fukuda ◽  
Yoshihisa Ohnishi ◽  
Kenji Kishi ◽  
...  

2012 ◽  
Vol 13 (12) ◽  
pp. 6191-6196 ◽  
Author(s):  
Jun Liu ◽  
Shi-Zhong Cai ◽  
Yue Zhou ◽  
Xian-Ping Zhang ◽  
Dian-Feng Liu ◽  
...  

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