Nitrophenyl-group-containing Heterocycles. 3. New Isoquinolines, as antiprolifative agents against MCF7and HEGP2 Cell lines. Synthesis, characterization and biological Evaluation. DOI Creative Commons
Etify A. Bakhite, Reda Hassanien, Nasser Farhan

et al.

Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 26, 2024

Abstract In this study, new tetrahydrosoquinoline compounds were synthesized by reacted with methyl iodide, chloro acetonitrile, ethyl chloroacetate, N-arylchloroacetamides N-and (benzthiazol-2-yl)-2-chloroacetamide reagents to gave tetrahydroiso-quinolin-3-ylthio) acetamides (5a-c) which can cyclized (6a-c) in excellent yields. The structures of all newly characterized elemental and spectral analyses. Also, most the evaluated for their anticancer activity MCF7 HEPG2 cell lines. From result we found that potent compound against lines was 9b, active 3. Then effects 3 on HEPG2 line investigated using an apoptotic Annexin V-FITC test flow cytometry. Compound induced a 59-fold increase apoptosis cycle arrested at G0-G1, G2/M phases. Moreover, molecular docking study applied showed 9b bind RET enzyme binding energies -6.8 kcal/mol comparison standard alectinib, exhibits energy -7.2 kcal/mol. HSP 90 (ΔG) -6.8 kcal/mol, is comparable Onalespib (-7.1 kcal/mol).

Language: Английский

New tetrahydroisoquinolines bearing nitrophenyl group targeting HSP90 and RET enzymes: synthesis, characterization and biological evaluation DOI Creative Commons
Etify A. Bakhite, Reda Hassanien, Nasser Farhan

et al.

BMC Chemistry, Journal Year: 2025, Volume and Issue: 19(1)

Published: Feb. 21, 2025

Abstract In this study, new tetrahydroisoquinoline compounds were synthesized by reaction of 7-Acetyl-4-cyano-1,6-dimethyl-6-hydroxy-8- (3-nitrophenyl or 4-nitrophenyl)-5,6,7,8-tetrahydrosoquinoline-3(2 H )-thiones with methyl iodide, chloro acetonitrile, ethyl chloroacetate to produce 3–5 and reacted N -arylchloroacetamides reagents gave tetrahydroisoquinolin-3-ylthio) acetamides 6a – c , 8a b which can cyclized 6,7,8,9-tetrahydrothieno[2,3-c]Isoquinoline-2-carboxamides 7a c, 9a . Also react -(benzthiazol-2-yl)-2-chloroacetamideto give compound 10 The structures all newly characterized elemental spectral analyses. Also, most the evaluated for their anticancer activities aganist MCF7 HEPG2 cell lines From result we found that active against was 8b, 3. Then effects 3 on line investigated using an apoptotic Annexin V-FITC test flow cytometry. Compound induced a 59-fold increase in apoptosis cycle arrested at G0-G1, G2/M phases. Moreover, molecular docking study applied showed 8b bind RET enzyme binding energies − 6.8 kcal/mol comparison standard alectinib exhibits energy 7.2 kcal/mol. HSP 90 (ΔG) kcal/mol, comparable Onalespib (− 7.1 kcal/mol). Graphical

Language: Английский

Citations

0
Nitrophenyl-group-containing Heterocycles. 3. New Isoquinolines, as antiprolifative agents against MCF7and HEGP2 Cell lines. Synthesis, characterization and biological Evaluation. DOI Creative Commons
Etify A. Bakhite, Reda Hassanien, Nasser Farhan

et al.

Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 26, 2024

Abstract In this study, new tetrahydrosoquinoline compounds were synthesized by reacted with methyl iodide, chloro acetonitrile, ethyl chloroacetate, N-arylchloroacetamides N-and (benzthiazol-2-yl)-2-chloroacetamide reagents to gave tetrahydroiso-quinolin-3-ylthio) acetamides (5a-c) which can cyclized (6a-c) in excellent yields. The structures of all newly characterized elemental and spectral analyses. Also, most the evaluated for their anticancer activity MCF7 HEPG2 cell lines. From result we found that potent compound against lines was 9b, active 3. Then effects 3 on HEPG2 line investigated using an apoptotic Annexin V-FITC test flow cytometry. Compound induced a 59-fold increase apoptosis cycle arrested at G0-G1, G2/M phases. Moreover, molecular docking study applied showed 9b bind RET enzyme binding energies -6.8 kcal/mol comparison standard alectinib, exhibits energy -7.2 kcal/mol. HSP 90 (ΔG) -6.8 kcal/mol, is comparable Onalespib (-7.1 kcal/mol).

Language: Английский

Citations

0