• YOGESH KUMAR

      Articles written in Journal of Chemical Sciences

    • 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

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      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.

    • Eosin Y photocatalyzed access to Biginelli reaction using primary alcohols via domino multicomponent cascade: an approach towards sustainable synthesis of 3,4-dihydropyrimidin-2(1H)-ones

      GOBIND KUMAR GAURAV BHARGAVA YOGESH KUMAR RUPESH KUMAR

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      The Eosin Y photocatalyzed Biginelli protocol has been established by a cascade one-pot three-component reaction of primary alcohols, a-ketoester, and urea to provide pharmacologically promising 3,4-dihydropyrimidin-2(1H)-ones in high yields. The key benefits of the present scheme are the capability toallow operational simplicity, readily available substrates, straightforward workup and high yields. This EosinY based photocatalytic approach can permit conquering traditional metal-catalyzed reactions in a sustainablemanner, thus delivering economic and environmental rewards.

      An environmentally benign protocol for the synthesis of 3,4-DHPMs has been developed using inexpensive molecular oxygen, visible light as green energy source and eosin Y as photoreceptor-cum-sensitizer. The utilized photoreceptor revealed its unique properties in rapid intersystem crossing, high photo and chemical stability, ease of separation and high catalytic efficiency.

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