Synthesis and Bioactivity Assessment of Novel Spiro Pyrazole-Oxindole Congeners Exhibiting Potent and Selective in vitro Anticancer Effects

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Heba M Abo-SalemMourad A M Aboul-Soud

Abstract

The present work aims to design and synthesize novel series of spiro pyrazole-3,3'-oxindoles analogues and investigate their bioactivity as antioxidant and antimicrobial agents, as well as antiproliferative potency against selected human cancerous cell lines (i.e., breast, MCF-7; colon, HCT-116 and liver, HepG-2) relative to healthy noncancerous control skin fibroblast cells (BJ-1). The mechanism of their cytotoxic activity has been also examined by immunoassaying the levels of key anti- and proapoptotic protein markers. The analytical and spectral data of the all synthesized target congeners were compatible with their structures. Synthesized compounds showed diverse moderate to powerful antimicrobial and antioxidant activities. Results of MTT assay revealed that seven synthesized compounds (i.e., 11a, 11b, 12a, 12b, 13b, 13c and 13h) particularly exhibited significant cytotoxicity against the three cancerous cell lines under investigation. Ranges of IC50 values obtained were 5.7-21.3 and 5.8-37.4 µg/mL against HCT-116 and MCF-7, respectively; which is 3.8 and 6.5-fold (based on the least IC50 values) more significant relative to the reference chemotherapeutic drug doxorubicin. In HepG-2 cells, the analogue 13h the highest cyto...Continue Reading

References

Dec 14, 1999·The Journal of Biological Chemistry·M Oren
Sep 21, 2002·Cancer Cell·Kurt DegenhardtEileen White
Jan 29, 2003·Angiogenesis·Jacqueline L WhatmoreChristopher J Moody
May 14, 2004·Journal of Virology·Chun-Jen Chen, Shinji Makino
May 14, 2005·CA: a Cancer Journal for Clinicians·Irene M GhobrialAlex A Adjei
Feb 14, 2006·Science·Saquib A LakhaniRichard A Flavell
Jun 15, 2007·Toxicologic Pathology·Susan Elmore
Sep 7, 2012·Chemical Reviews·Girija S Singh, Zelalem Y Desta
Jan 1, 2010·Saudi Journal of Biological Sciences·Faris Q AlenziRichard K H Wyse
Oct 30, 2013·Anti-cancer Agents in Medicinal Chemistry·Sunil SagarMandeep Kaur
Jul 6, 2014·European Journal of Medicinal Chemistry·Bin YuHong-Min Liu
Jul 12, 2014·BioMed Research International·Mohamed HassanNoriaki Sakuragi
Oct 27, 2015·Anti-cancer Agents in Medicinal Chemistry·Blassan Plackal Adimuriyil George, Heidi Abrahamse
Nov 29, 2015·BioMedicine·Viswanadha Vijaya Padma
Nov 11, 2017·In Vitro Cellular & Developmental Biology. Animal·Mona Nazemi MoghaddamZohreh Zeraatkar
Feb 3, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mourad A M Aboul-SoudTalat A El-Kersh

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Citations

Feb 19, 2021·European Journal of Medicinal Chemistry·Darshana BoraNagula Shankaraiah

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Methods Mentioned

BETA
ELISA
NMR
Enzyme-Linked

Software Mentioned

SPSS

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