Synthesis, Cytotoxic Activity and Molecular Docking Studies of New Condensed Thieno[2,3-d]Pyrimidines as Antitumor Agents

Kaliraj, S.; Jeyalakshmi, R.; Kathiravan, Muthu K.

doi:10.1007/s11094-020-02188-w

Cited by 5 publications

(3 citation statements)

References 19 publications

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“…The presence of ethyl, methyl, and ethyl-fused five-membered rings in the structure showed better activity in A431 than in H9c2 cells and in case of the six-membered structures, methyl-substituted cyclohexyl compounds inhibited A431 cell growth, although dimethyl substituted thiophene derivatives displayed better activity in H9c2 cells. Nitromethyl, cyclohexyl, and dimethyl substitution lowered activity compared to chloro substitution fused with seven membered rings and the methyl-substituted structures had better potency than the aryl substituted structures [108].…”

Section: Thieno Pyrimidine Derivatives Thieno[23-d]pyrimidinesmentioning

confidence: 93%

Pyrimidine: a review on anticancer activity with key emphasis on SAR

2021

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Background Cancer is a global health challenge, it impacts the quality of life and its treatment is associated with several side effects. Resistance of the cancer cells to the existing drugs has led to search for novel anticancer agents. Pyrimidine, a privileged scaffold, is part of living organisms and plays vital role in various biological procedures as well as in cancer pathogenesis. Due to resemblance in structure with the nucleotide base pair of DNA and RNA, it is recognized as valuable compound in the treatment of cancer. Main text Many novel pyrimidine derivatives have been designed and developed for their anticancer activity in the last few years. The present review aims to focus on the structure activity relationship (SAR) of pyrimidine derivatives as anticancer agent from the last decade. Conclusion This review intends to assist in the development of more potent and efficacious anticancer drugs with pyrimidine scaffold. Graphical abstract

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Section: Thieno Pyrimidine Derivatives Thieno[23-d]pyrimidinesmentioning

confidence: 93%

Pyrimidine: a review on anticancer activity with key emphasis on SAR

2021

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“…The lactam‐fused thienopyrimidine synthesis and biological studies are established in our previous work [21] . From the encouraging results, the trial on the synthesis of N‐(2,6‐dioxopiperidin‐3‐yl)‐3‐methyl‐4‐oxo‐4,6,7,8,9,10‐hexahydrothieno [2′,3′:4,5] pyrimido [1,2‐a] azepine‐2‐carboxamide ( 7 ) attempted from lactam fused thienopyrimidine ( 5 ) and 3‐aminopiperidine‐2,6‐dione.…”

Section: Resultsmentioning

confidence: 99%

“…The lactam-fused thienopyrimidine synthesis and biological studies are established in our previous work. [21] From the encouraging results, the trial on the synthesis of N-(2,6dioxopiperidin-3-yl)-3-methyl-4-oxo-4,6,7,8,9,10-hexahydrothieno [2',3':4,5] pyrimido [1,2-a] azepine-2-carboxamide (7) attempted from lactam fused thienopyrimidine (5) and 3-aminopiperidine-2,6-dione. The reaction's first step is ethyl ester hydrolysis followed by amide bond formation between 3-aminopiperidine-2,6-dione and lactam fused thienopyrimidine.…”

Section: Synthesis Of Dioxopiperidincarboxamide Substituted Lactam Fu...mentioning

confidence: 99%

Design, Synthesis of Dioxopiperidinamide Derivatives by Amide Coupling Reaction and Study of Their Biological Activity

Kaliraj

Jeyalakshmi

2023

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A series of fifteen dioxopiperidinamide derivatives synthesized and their spectra chemical data were reported. An alternative amide coupling reaction has been followed by using 3‐aminopiperidine‐2,6‐dione through amide bond functionalization between N‐Ethyl‐N′‐(3‐dimethylaminopropyl)carbodiimide hydrochloride (EDC.HCl) and Hydroxybenzotriazole (HOBt). All the designed compounds were docked in to the active sites of 2 A73: Human Complement Component C3. All the docked compounds is favorable to make both hydrogen and hydrophobic interaction with amino acids located at the binding site. The most of potential compounds (E)‐N‐(2,6‐dioxopiperidin‐3‐yl)‐3‐(m‐tolyl)acrylamide (4 g), (E)‐3‐(4‐bromophenyl)‐N‐(2,6‐dioxopiperidin‐3‐yl)acrylamide (4 h) and N‐(2,6‐dioxopiperidin‐3‐yl)‐3‐methyl‐4‐oxo‐4,6,7,8,9,10‐hexahydrothieno [2′,3′:4,5]pyrimido[1,2‐a]azepine‐2‐carboxamide (7) studied for their anticancer activity on the THP‐1 cancer cells line. It was also further established their Anti‐inflammatory activity and Antioxidant activity with the comparable efficiency against those of clinically used drugs.

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