Browsing by Author "Prasad, K. J. Rajendra"

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    Synthesis and Cytotoxicity of Novel Indoloquinolines and Benzonaphthyridines from 4-Chloro-2,8-dimethylquinoline and Variety of Hetero Amines
    (2021) Prabha, Kolandaivel; Satheeshkumar, Rajendran; Prasad, K. J. Rajendra
    The synthesis of hetero substituted indoloquinolines and thiophene substituted benzonaphthyridienes from two heterocycles tethered by nitrogen or sulfur intermediates. Further it was cyclized using Pd(OAc)(2) catalyst to yield products, i. e., various heteroindolo quinolines and polyphosphoric acid (PPA) mediated thiophene substituted naphthyridines. All the potential intermediates and their respective final products were screened for anticancer activity against HeLa and K562 cancer cells, and it showed good cytotoxicity against HeLa and K562 cells compared standard Adriamycin (ADR) drugs. Among the newly synthesized compounds, compounds 3 a, 3 b, 4 b and 5 a displayed stronger cytotoxic activity against both HeLa and K562 cells compared standard Adriamycin (ADR) drug. This might be due to the presence of benzothiazole and isoquinoline moieties, which enhanced the cytotoxic activity. Subsequently, compounds 3 c, 3 d, 4 a, 5 b and 7 also showed better cytotoxic activity with IC50 values <19 mu M against HeLa and K562 cells, which was due to the presence of quinoline and thiophene moieties, which enhanced the cytotoxic activity.
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    Synthesis, In Vitro Cytotoxicity, and DFT Studies of Novel 2-Amino Substituted Benzonaphthyridines as PDK1 Inhibitors
    (2022) Prabha, Kolandaivel; Satheeshkumar, Rajendran; Nasif, Vesim; Saranya, Jayapalan; Sayin, Koray; Natarajan, Jeyakumar; Chandrasekar, Chinnarasu; Prasad, K. J. Rajendra
    The present work emphasizes the utility of 2,4-dichloro-5-methylbenzo[h][1,6]naphthyridine as starting precursors. The reaction of 2,4-dichloro-5-methylbenzo[h][1,6]naphthyridine with a variety of aliphatic and aromatic amines yielded 2-amino substituted 2,4-dichlorobenzo[h]naphthyridines. All the compounds were examined for their in vitro anticancer activity against six human cancer lines and docked with PDK1 inhibitors. The structure-activity relationship studies are revealed that the compounds holding aminocarbazole moiety and triazole amine moiety improve the activity profile. All the structures of synthesized compounds were optimized at B3LYP-D3/6-31G(d) level in the water. Furthermore, the electronic properties and biological reactivity of the synthesized compounds are explored using computational techniques.