Rakesh sreerama - Academia.edu (original) (raw)
Papers by Rakesh sreerama
![Research paper thumbnail of Synthesis and Biological Evaluation of Novel 1,2,3-Triazole Based Pyrido[4,3-d]pyrimidines as Potent Anticancer and EGFR Inhibitors](https://attachments.academia-assets.com/116521915/thumbnails/1.jpg)
](Russian Journal of General Chemistry, Dec 1, 2021
A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Ch... more A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan eLam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.
Russian Journal of Bioorganic Chemistry
Phosphorus, Sulfur, and Silicon and the Related Elements
A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (5a-5l) in good yields ... more A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (5a-5l) in good yields (63 to 77%) using different sulfonic acids and 4-(prop-2-yn-1-yl)thiomorpholine 1,1-dioxide through the in situ generated sulfonyl azides was developed. The structures of the newly synthesized compounds were confirmed by 1 H NMR, 13 C NMR, mass spectrometry, and elemental analysis. The newly synthesized compounds were screened for in vitro antibacterial activity and free radical scavenging activity in terms of hydrogen donating or radical scavenging ability by the DPPH method. Among all, the compound N-(4-((4-((1,1-dioxidothiomorpholino) methyl)-1H-1,2,3-triazol-1yl)sulfonyl)phenyl) acetamide (5l) was found to exhibit potent activity as compared to the standard drugs.
Journal of Molecular Structure
A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (<b>5a–5l</b&g... more A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (<b>5a–5l</b>) in good yields (63 to 77%) using different sulfonic acids and 4-(prop-2-yn-1-yl)thiomorpholine 1,1-dioxide through the <i>in situ</i> generated sulfonyl azides was developed. The structures of the newly synthesized compounds were confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR, mass spectrometry, and elemental analysis. The newly synthesized compounds were screened for <i>in vitro</i> antibacterial activity and free radical scavenging activity in terms of hydrogen donating or radical scavenging ability by the DPPH method. Among all, the compound <i>N</i>-(4-((4-((1,1-dioxidothiomorpholino) methyl)-1H-1,2,3-triazol-1-yl)sulfonyl)phenyl) acetamide (<b>5l</b>) was found to exhibit potent activity as compared to the standard drugs.
Russian Journal of General Chemistry, Dec 1, 2021
A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Ch... more A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan eLam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol. In addition, cell cycle assay indicated that these 1,6-diaryl pyridin-2(1H)-one compounds induced cell cycle arrest in the G1/M phase in the HepG2 cell line.
Russian Journal of Bioorganic Chemistry
Phosphorus, Sulfur, and Silicon and the Related Elements
A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (5a-5l) in good yields ... more A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (5a-5l) in good yields (63 to 77%) using different sulfonic acids and 4-(prop-2-yn-1-yl)thiomorpholine 1,1-dioxide through the in situ generated sulfonyl azides was developed. The structures of the newly synthesized compounds were confirmed by 1 H NMR, 13 C NMR, mass spectrometry, and elemental analysis. The newly synthesized compounds were screened for in vitro antibacterial activity and free radical scavenging activity in terms of hydrogen donating or radical scavenging ability by the DPPH method. Among all, the compound N-(4-((4-((1,1-dioxidothiomorpholino) methyl)-1H-1,2,3-triazol-1yl)sulfonyl)phenyl) acetamide (5l) was found to exhibit potent activity as compared to the standard drugs.
Journal of Molecular Structure
A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (<b>5a–5l</b&g... more A one-pot procedure for the synthesis of novel 1,2,3-triazole derivatives (<b>5a–5l</b>) in good yields (63 to 77%) using different sulfonic acids and 4-(prop-2-yn-1-yl)thiomorpholine 1,1-dioxide through the <i>in situ</i> generated sulfonyl azides was developed. The structures of the newly synthesized compounds were confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR, mass spectrometry, and elemental analysis. The newly synthesized compounds were screened for <i>in vitro</i> antibacterial activity and free radical scavenging activity in terms of hydrogen donating or radical scavenging ability by the DPPH method. Among all, the compound <i>N</i>-(4-((4-((1,1-dioxidothiomorpholino) methyl)-1H-1,2,3-triazol-1-yl)sulfonyl)phenyl) acetamide (<b>5l</b>) was found to exhibit potent activity as compared to the standard drugs.