Design, synthesis, biological evaluation, and docking studies of novel triazolo[4,3-b]pyridazine derivatives as dual c-Met/Pim-1 potential inhibitors with antitumor activity DOI Creative Commons
Mohamed E. Mahmoud, Eman Ahmed,

Hamdy M. Ragab

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(41), P. 30346 - 30363

Published: Jan. 1, 2024

New series of triazolo[4,3- b ]pyridazine derivatives were created. Compounds 4a and 4g demonstrated extensive antiproliferative activity on various cell lines. Compound displayed higher dual inhibition c-Met Pim-1.

Language: Английский

Design, synthesis, and biological evaluation of novel thiazole derivatives as PI3K/mTOR dual inhibitors. DOI

Samar I. Faggal,

Yara El‐Dash, Amr Sonousi

et al.

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

Published: Jan. 1, 2024

The development of anticancer drugs targeting both PI3K and mTOR pathways is recognized as a promising cancer therapeutic approach. In the current study, we designed synthesized seventeen new thiazole compounds to investigate their effect on well anti-apoptotic activity. All thiazoles were investigated for antiproliferative activity panel 60 different cell lines at National Cancer Institute. Compounds 3b 3e selected further investigation five dose concentrations due effective growth inhibiting evaluated

Language: Английский

Citations

1
New S‐substituted‐3‐phenyltetrahydrobenzo[4,5]thieno[2,3‐d]pyrimidin‐4(3H)‐one scaffold with promising anticancer activity profile through the regulation and inhibition of mutated B‐RAF signaling pathway DOI Creative Commons

Safaa E. Seif,

Wagnat W. Wardakhan, Rasha A. Hassan

et al.

Drug Development Research, Journal Year: 2024, Volume and Issue: 85(7)

Published: Oct. 18, 2024

Abstract Novel 3‐phenyltetrahydrobenzo[4,5]thieno[2,3‐ d ]pyrimidine derivatives were synthesized and screened for their antiproliferative activity against a panel of 60 cancer cell lines. Derivatives 5b , 5f 9c showed significant antitumor at single dose with mean growth inhibition 55.62%, 55.79%, 71.40%, respectively. These compounds further investigated HCT‐116, colon line, FHC, normal line. Compound the highest IC 50 = 0.904 ± 0.03 µM SI 20.42 excelling doxorubicin which scored 2.556 0.09 6.19. was also most potent B‐RAF WT mutated V600E 0.145 0.005 0.042 0.002 µM, respectively in comparison vemurafenib 0.229 0.008 0.038 0.001 The cycle analysis that increased population induced an arrest HCT‐116 cells G0‐G1 stage 1.23‐fold. Apoptosis evaluation compound displayed 18.18‐fold elevation total apoptosis to control. content caspase‐3 by 3.52‐fold versus A molecular modeling study determined binding profile interaction active site.

Language: Английский

Citations

1
Advances in chalcone-based anticancer therapy: mechanisms, preclinical advances, and future perspectives DOI

Shefali Chowdhary,

Preeti Preeti,

Shekhar Shekhar

et al.

Expert Opinion on Drug Discovery, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 2, 2024

Introduction Cancerremains a leading cause of death worldwide with traditional treatments likechemotherapy, and radiotherapy becoming less effective due to multidrugresistance (MDR). This highlights the necessity for novel chemotherapeuticslike chalcone based compounds, which demonstrate broad anti-cancer propertiesand target multiple pathways. These compounds hold promise improving cancertreatment outcomes compared existing therapies.

Language: Английский

Citations

1
Tetrahydrocarbazoles incorporating 5-arylidene-4-thiazolinones as potential antileukemia and antilymphoma targeting tyrosine kinase and tubulin polymerase enzymes: Design, synthesis, structural, biological and molecular docking studies DOI

Basma S Ali,

Anber F. Mohammed, Benson M. Kariuki

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 153, P. 107817 - 107817

Published: Sept. 10, 2024

Language: Английский

Citations

0
Design, synthesis, biological evaluation, and docking studies of novel triazolo[4,3-b]pyridazine derivatives as dual c-Met/Pim-1 potential inhibitors with antitumor activity DOI Creative Commons
Mohamed E. Mahmoud, Eman Ahmed,

Hamdy M. Ragab

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(41), P. 30346 - 30363

Published: Jan. 1, 2024

New series of triazolo[4,3- b ]pyridazine derivatives were created. Compounds 4a and 4g demonstrated extensive antiproliferative activity on various cell lines. Compound displayed higher dual inhibition c-Met Pim-1.

Language: Английский

Citations

0