Fabrication of large-area Epitaxial Graphene by Chemical Vapor Deposition for device applications

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Design, synthesis and biological evaluation of Arylpiperazine-based novel Phthalimides: active inducers of testicular germ cell apoptosis

Publication . Singh, Anil K.; Bhardwaj, Jitender K.; Olival, Ana; Kumar, Yogesh; Podder, Avijit; Maheshwari, Ankur; Agrawal, Renuka; Latha, N.; Singh, Brajendra K.; Tomás, Helena; Rodrigues, João; Kishan, Ram; Rupini, B.; Rathi, Brijesh

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 as potential 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 mechanisms responsible 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 nuclear condensation. 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.

2016Artigo científico

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Entidade financiadora

Fundação para a Ciência e a Tecnologia

Programa de financiamento

5876-PPCDTI

Número da atribuição

PTDC/CTM-NAN/121108/2010