Potent Anticancer Activity with High Selectivity of a Chiral Palladium N-Heterocyclic Carbene Complex

ACS Omega
Anuj KumarPrasenjit Ghosh

Abstract

Five enantiomeric pairs of palladium complexes of 1,2,4-triazole-derived chiral N-heterocyclic carbene ligands were investigated to probe the influence of chirality on the compound's anticancer activity. Although no chirality-related influence was observed for any of the enantiomeric pair, strong anticancer activity was seen for a particular pair, (1S,2S,5R)-1c and (1R,2R,5S)-1c, which was significantly more active than the benchmark drug cisplatin for human breast cancer cells, MCF-7 (ca. 24-27-fold), and human cervical cancer cells, HeLa (ca. three- to fourfold). Broadening its scope of application, (1R,2R,5S)-1c also exhibited antiproliferative activity against lung cancer (A549), skin cancer (B16F10), and multidrug-resistant mammary tumor (EMT6/AR1) cell lines. Interestingly, (1R,2R,5S)-1c displayed 8- and 16-fold stronger antiproliferative activity toward B16F10 and MCF-7 relative to their respective noncancerous counterparts, L929 (fibroblast skin cells) and MCF10A (epithelial breast cells), thereby upholding the potential of these complexes for further development as anticancer agents. (1R,2R,5S)-1c inhibited tumor-cell proliferation by blocking the cells at the G2 phase. (1R,2R,5S)-1c caused DNA damage in MCF-7 cells, l...Continue Reading

References

Jul 4, 1990·Journal of the National Cancer Institute·P SkehanM R Boyd
Oct 23, 1980·Nature·R WingR E Dickerson
Dec 1, 1993·British Journal of Cancer·J E LiebmannJ B Mitchell
Jan 5, 2001·Journal of Medicinal Chemistry·R A Casero, P M Woster
Feb 7, 2001·Proceedings of the National Academy of Sciences of the United States of America·R Takimoto, W S El-Deiry
Jul 9, 2002·Apoptosis : an International Journal on Programmed Cell Death·C Soldani, A Ivana Scovassi
Feb 28, 2004·Journal of Natural Products·Nicholas H Oberlies, David J Kroll
May 4, 2005·Biochemical and Biophysical Research Communications·Jian Yu, Lin Zhang
Sep 1, 2005·Bioorganic & Medicinal Chemistry·Vandana SrivastavaSuman P S Khanuja
Oct 1, 2008·Biochemical Pharmacology·Krishnan Rathinasamy, Dulal Panda
May 9, 2009·Chemical Reviews·Gordon M CraggDavid J Newman
Jun 30, 2009·The Journal of Biological Chemistry·Saverio TarditoRenata Franchi-Gazzola
Jul 2, 2010·Dalton Transactions : an International Journal of Inorganic Chemistry·Nial J WheateRabbab Oun
Nov 17, 2010·Journal of Medicinal Chemistry·Gilles GasserNils Metzler-Nolte
Oct 4, 2011·Talanta·Susanne NussbaumerSandrine Fleury-Souverain
Sep 18, 2012·Antioxidants & Redox Signaling·Chu-Chiao Wu, Shawn B Bratton
Jan 25, 2014·Chemical Reviews·Katja Dralle Mjos, Chris Orvig
Jun 24, 2014·Analytical Methods : Advancing Methods and Applications·Xue Wang, Michael G Roper
Jan 9, 2016·CA: a Cancer Journal for Clinicians·Rebecca L SiegelAhmedin Jemal
Jan 14, 2016·Journal of Agricultural and Food Chemistry·Mohamed Ali SeyedKavitha Vijayaraghavan

❮ Previous
Next ❯

Citations

Sep 5, 2019·Dalton Transactions : an International Journal of Inorganic Chemistry·Isabel de la Cueva-AliqueEva Royo
Oct 14, 2019·Biochemical Pharmacology·Anuradha KumariDulal Panda
Nov 24, 2018·Biochemical Pharmacology·Afsana NaazDulal Panda
Nov 5, 2019·ACS Omega·Scott M HutchinsonJeanne L Bolliger

❮ Previous
Next ❯

Methods Mentioned

BETA
X-ray
flow cytometry
NMR
column chromatography
electrophoresis
Assay

Software Mentioned

ImageJ
ORTEP

Related Concepts

Related Feeds

Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis

Apoptosis in Cancer

Apoptosis is an important mechanism in cancer. By evading apoptosis, tumors can continue to grow without regulation and metastasize systemically. Many therapies are evaluating the use of pro-apoptotic activation to eliminate cancer growth. Here is the latest research on apoptosis in cancer.