Articles written in Journal of Chemical Sciences
Volume 128 Issue 8 August 2016 pp 1245-1263 Regular Article
Design, synthesis and biological evaluation of Arylpiperazine-based novel Phthalimides: Active inducers of testicular germ cell apoptosis
ANIL K SINGH JITENDER K BHARDWAJ ANA OLIVAL YOGESH KUMAR AVIJIT PODDER ANKUR MAHESHWARI RENUKA AGRAWAL N LATHA BRAJENDRA K SINGH HELENA TOMÁS JOÃO RODRIGUES RAM KISHAN B RUPINI BRIJESH RATHI
Understanding of apoptosis or programmed cell death has provided the basis for novel therapeutics that has resulted in rationally designed anticancer strategies. Recently, inducers of apoptosis have been used in cancer therapy. In this work, we describe the role of chiral phthalimides functionalized with piperazines aspotential apoptotic inducers. The listed twenty phthalimides were assessed for their in vitro apoptotic activity against testicular germ cells. All phthalimides showed a significant apoptotic response (∼39 to ∼68%). TUNEL assay and acridine orange fluorescence staining were carried out to investigate the molecular mechanismsresponsible for the cell death. Phthalimides exhibited substantial apoptotic induction following the intrinsic pathway mechanism. Studies advocated that the apoptotic induction was mediated through caspase-9, caspase-3, JNK MAP kinase and tumor suppressor p53, which was accompanied by DNA fragmentation and nuclearcondensation. Besides, the best five phthalimides regarding apoptotic action were evaluated for in vitro cytotoxic effects against CAL-72 and MCF-7 cancer cell lines. Compounds showed efficient killing of cancer cells. This discovery of functionalized phthalimides as apoptotic inducers would be highly valuable in understanding the mechanism of apoptosis at the molecular level and opens up new possibilities for therapeutic strategies.
Volume 135, 2023
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