New pyrimidine-5-carbonitrile derivatives as EGFR inhibitors with anticancer and apoptotic activities: design, molecular modeling and synthesis

IA Osman, RR Ayyad, HA Mahdy - New Journal of Chemistry, 2022 - pubs.rsc.org
In connection with our efforts in the development of new anticancer agents, herein we report
the design and synthesis of new small pyrimidine-5-carbonitrile based derivatives. The …

Novel scaffold hopping of potent benzothiazole and isatin analogues linked to 1, 2, 3-triazole fragment that mimic quinazoline epidermal growth factor receptor …

N Rezki, MA Almehmadi, S Ihmaid, AM Shehata… - Bioorganic …, 2020 - Elsevier
A series of benzothiazole/isatin linked to 1, 2, 3-triazole moiety and terminal sulpha drugs 5a-
e and 6a-e were synthesized and evaluated for cytotoxic activity against a panel of cancer …

Discovery of 3, 3 a, 4, 5-tetrahydro-2 H-benzo [g] indazole containing quinoxaline derivatives as novel EGFR/HER-2 dual inhibitors

X Zong, J Cai, J Chen, C Sun, L Li, M Ji - RSC Advances, 2015 - pubs.rsc.org
In the present study, twenty-five pyrazole–quinoxaline derivatives (4a–4y) were designed
and synthesized, and their biological activity as potential EGFR or HER-2 kinase inhibitors …

In vitro Anticancer and Insilico Studies of Quinoxaline‐sulfonyl‐1, 2, 4‐triazole Hybrids

G Dasari, S Bandari, S Kumar Nukala… - …, 2022 - Wiley Online Library
Abstract New quinoxaline‐sulfonyl‐1, 2, 4‐triazole hybrids were synthesized (5 a–n) via
systematic step‐wise sequence. Later, the in vitro cytotoxicity screening of all these …

Design, synthesis, and antiproliferative activity of new indole/1, 2, 4‐triazole/chalcone hybrids as EGFR and/or c‐MET inhibitors

E Mahmoud, D Abdelhamid, BGM Youssif… - Archiv der …, 2024 - Wiley Online Library
A novel group of indolyl‐1, 2, 4‐triazole‐chalcone hybrids was designed, synthesized, and
assessed for their anticancer activity. The synthesized compounds exhibited significant …

Novel 1, 3, 5-triazine-based pyrazole derivatives as potential antitumor agents and EFGR kinase inhibitors: Synthesis, cytotoxicity, DNA binding, molecular docking …

MS Raghu, CBP Kumar, MK Prashanth… - New Journal of …, 2021 - pubs.rsc.org
We herein report the design and synthesis of new 1, 3, 5-triazine-based pyrazole derivatives
(5a–i) with anticancer activity targeting the epidermal growth factor (EGFR) tyrosine kinase …

New molecular hybrids containing benzimidazole, thiazolidine-2, 4-dione and 1, 2, 4-oxadiazole as EGFR directing cytotoxic agents

B Saritha, BBV Sailaja - Tetrahedron, 2022 - Elsevier
Herein, we, synthesized some new molecular hybrids (7a-o) having benzimidazole,
thiazolidine-2, 4-dione and 1, 2, 4-oxadiazole scaffolds from the commercially available 1 …

New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation

ET Warda, IA Shehata, MB El-Ashmawy… - Bioorganic & Medicinal …, 2020 - Elsevier
New series of isoxazole derivatives were synthesized and evaluated for in vitro antitumor
activity against HepG2, MCF-7 and HCT-116 cancer cells. Results showed that 4b and 25a …

Novel 2-(5-Aryl-4, 5-dihydropyrazol-1-yl) thiazol-4-one as EGFR inhibitors: synthesis, biological assessment and molecular docking insights

T Al-Warhi, AM El Kerdawy, MA Said… - Drug Design …, 2023 - Taylor & Francis
Introduction Epidermal growth factor receptor (EGFR) regulates several cell functions which
include cell growth, survival, multiplication, differentiation, and apoptosis. Currently, EGFR …

Novel 5-bromoindole-2-carboxylic acid derivatives as EGFR inhibitors: synthesis, docking study, and structure activity relationship

OM Hassan, A Kubba… - Anti-Cancer Agents in …, 2023 - ingentaconnect.com
Background: The indole backbone is encountered in a class of N-heterocyclic compounds
with physiological and pharmacological effects such as anti-cancer, anti-diabetic, and anti …