Novel 4-(2-arylidenehydrazineyl) thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico …

HA Elsebaie, EA El-Bastawissy, KM Elberembally… - Bioorganic …, 2023 - Elsevier
The current study discovered fifteen new thieno [2, 3-d] pyrimidine derivatives with potential
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …

Nicotinonitrile as an essential scaffold in medicinal chemistry: an updated review (2015–present)

H Hassan, M Hisham, M Osman… - Journal of Advanced …, 2023 - journals.ekb.eg
Many studies have been carried out to find synthetic pathways to nicotinonitriles (3-
cyanopyridines) and their analogs, which has resulted in a substantial amount of knowledge …

Synthesis and antimicrobial activity of pyrimidinyl 1, 3, 4-oxadiazoles, 1, 3, 4-thiadiazoles and 1, 2, 4-triazoles

MM Sekhar, U Nagarjuna, V Padmavathi… - European journal of …, 2018 - Elsevier
A new class of methylthio linked pyrimidinyl 1, 3, 4-oxadiazoles, 1, 3, 4-thiadiazoles and 1, 2,
4-triazoles were prepared under conventional and ultrasound irradiation methods. All the …

Synthesis, antimicrobial and cytotoxic activities of pyrimidinyl benzoxazole, benzothiazole and benzimidazole

D Seenaiah, PR Reddy, GM Reddy, A Padmaja… - European Journal of …, 2014 - Elsevier
A variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio,
methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic …

A Review: synthesis and medicinal importance of nicotinonitriles and their analogous

MA Gouda, BHM Hussein, MH Helal… - Journal of Heterocyclic …, 2018 - Wiley Online Library
The biological, therapeutic, and medicinal properties of nicotinonitriles (cyanopyridines) and
its analogues have prompted enormous research aimed at developing synthetic routes to …

Discovery of new cyanopyridine/chalcone hybrids as dual inhibitors of EGFR/BRAFV600E with promising antiproliferative properties

HA Abou‐Zied, EAM Beshr, HAM Gomaa… - Archiv der …, 2023 - Wiley Online Library
As dual EGFR and BRAFV600E inhibitors, 2‐(3‐cyano‐4, 6‐bis (aryl)‐2‐oxo‐1, 2‐
dihydropyridine‐1‐yl)‐N‐(4‐cinnamoylphenyl) acetamide derivatives 8–20 were developed …

Identification of 3‐(5‐cyano‐6‐oxo‐pyridin‐2‐yl) benzenesulfonamides as novel anticancer agents endowed with EGFR inhibitory activity

MA Shaldam, AF Khalil, H Almahli… - Archiv der …, 2024 - Wiley Online Library
Abstract New 5‐cyano‐6‐oxo‐pyridine‐based sulfonamides (6a–m and 8a–d) were
designed and synthesized to potentially inhibit both the epidermal growth factor receptor …

The cremeomycin biosynthetic gene cluster encodes a pathway for diazo formation

AJ Waldman, Y Pechersky, P Wang, JX Wang… - …, 2015 - Wiley Online Library
Diazo groups are found in a range of natural products that possess potent biological
activities. Despite longstanding interest in these metabolites, diazo group biosynthesis is not …

Computer-aided design, synthesis, and biological evaluation of new indole-2-carboxamide derivatives as PI3Kα/EGFR inhibitors

K Sweidan, DA Sabbah, S Bardaweel, KA Dush… - Bioorganic & medicinal …, 2016 - Elsevier
Abstract Structure-based drug design and molecular modeling were employed to identify a
new series of indole-2-carboxamides as potential anticancer agents. These compounds …

In vivo efficacy studies of novel quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors, in lung cancer xenografts (NCI-H1975) mice models

D Das, L Xie, J Wang, J Shi, J Hong - Bioorganic Chemistry, 2020 - Elsevier
Lung cancer is the most common cancer and leading cause of cancer-related deaths
worldwide. The first-generation reversible, ATP-competitive inhibitors gefetinib and elotinib …