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

TTFA-Platin Conjugate: Deciphering the Therapeutic Roles of Combo-Prodrug through Evaluating Stability–Activity Relationship DOI
Megha Biswas,

K. D. Chaudhary,

Swati Shree Padhi

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 29, 2024

This work introduces a novel Pt(II) based prodrug TTFA-Platin that integrates β-diketonate ligand TTFA with platinum scaffold to structurally resemble carboplatin and offers intermediate kinetic lability between cisplatin carboplatin, striking balance therapeutic efficacy safety. A comprehensive stability speciation study was conducted in various biological media, mapping the effects of TTFA-Platin. control molecule, TMK-Platin, synthesized further validate structural-stability relationship, which displayed poor activatable features systems.

Language: Английский

Citations

0
The interaction of isoquinoline alkaloid crebanine with immunoglobulin G and cytotoxic effects toward MCF-7 breast cancer cell line DOI

Shaorong Zhao,

Lu Yang, Wenzhu Li

et al.

International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: unknown, P. 139194 - 139194

Published: Dec. 1, 2024

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