Synthesis of novel mono-and bis-pyrazolylthiazole derivatives as anti-liver cancer agents through EGFR/HER2 target inhibition
Bromoacetyl-4-(2-naphthoyl)-1-phenyl-1H-pyrazole (6) was synthesized from 2-
acetylnaphthalene and was used as a new key building block for constructing the title …
acetylnaphthalene and was used as a new key building block for constructing the title …
Synthesis of phthalazine-based derivatives as selective anti-breast cancer agents through EGFR-mediated apoptosis: in vitro and in silico studies
SM Emam, SME Rayes, IAI Ali, HA Soliman, MS Nafie - BMC chemistry, 2023 - Springer
Abstract The parent 2-(4-benzyl-1-oxophthalazin-2 (1 H)-yl)-acetohydrazide (4) has twenty-
nine compounds. The starting material for their corresponding mono, dipeptides and …
nine compounds. The starting material for their corresponding mono, dipeptides and …
Novel bis-amide-based bis-thiazoles as anti-colorectal cancer agents through Bcl-2 inhibition: synthesis, in vitro, and in vivo studies
Background: Some heterocycles having bisamide linkage are receiving much interest due to
their remarkable biological potencies and they are naturally occurring. Some bisamides and …
their remarkable biological potencies and they are naturally occurring. Some bisamides and …
Synthesis and Anti-Breast Cancer Potency of Mono- and Bis-(pyrazolyl[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine) Derivatives as EGFR/CDK-2 Target Inhibitors
The target mono-and bis-(6-pyrazolyltriazolo-thiadiazine) derivatives 4a-c and 6a-d were
synthesized using a straightforward protocol via reaction of 3-bromoacetylpyrazole 2 with 4 …
synthesized using a straightforward protocol via reaction of 3-bromoacetylpyrazole 2 with 4 …
New spiro-indeno[1,2-b]quinoxalines clubbed with benzimidazole scaffold as CDK2 inhibitors for halting non-small cell lung cancer; stereoselective synthesis …
A Barakat, S Alshahrani, AM Al-Majid… - Journal of Enzyme …, 2023 - Taylor & Francis
Despite the crucial role of CDK2 in tumorigenesis, few inhibitors reached clinical trials for
managing lung cancer, the leading cause of cancer death. Herein, we report combinatorial …
managing lung cancer, the leading cause of cancer death. Herein, we report combinatorial …
Synthesis and Evaluation of Bithiazole Derivatives As Potential α-Sarcoglycan Correctors
4′-Methyl-4, 5′-bithiazoles were previously identified as cystic fibrosis transmembrane
regulator (CFTR) correctors, thus being able to correct folding defective mutants of the …
regulator (CFTR) correctors, thus being able to correct folding defective mutants of the …
Design, Synthesis, Computational Investigations, and Antitumor Evaluation of N-Rhodanine Glycosides Derivatives as Potent DNA Intercalation and Topo II Inhibition …
Nitrogen and sulfur glycosylation was carried out via the reaction of rhodanine (1) with α-
acetobromoglucose 3 under basic conditions. Deacetylation of the protected nitrogen …
acetobromoglucose 3 under basic conditions. Deacetylation of the protected nitrogen …
Synthesis and biological evaluation of thiazole and thiadiazole derivatives as potential anticancer agents
S Ekrek, S Şenkardeş, Ö Erdoğan… - Phosphorus, Sulfur, and …, 2023 - Taylor & Francis
A new series of 4-methyl-2-{2-[(aryl) methylidene] hydrazinyl}-1, 3-thiazole (2a-i), N-(4-acetyl-
5-aryl) 4, 5-dihydro-1, 3, 4-thiadiazol-2-yl) acetamides (3a-b) and N-(5-(4-(substituted …
5-aryl) 4, 5-dihydro-1, 3, 4-thiadiazol-2-yl) acetamides (3a-b) and N-(5-(4-(substituted …
Design, synthesis and cytotoxic evaluation of novel bis-thiazole derivatives as preferential Pim1 kinase inhibitors with in vivo and in silico study
Bis-thiazole derivatives were synthesised conforming to the Pim1 pharmacophore model
following Hantzsch condensation. Pim1 has a major role in regulating the G1/S phase which …
following Hantzsch condensation. Pim1 has a major role in regulating the G1/S phase which …
Design, synthesis, molecular modelling and antitumor evaluation of S-glucosylated rhodanines through topo II inhibition and DNA intercalation
In the present study, 5-arylidene rhodanine derivatives 3a–f, N-glucosylation rhodanine 6, S-
glucosylation rhodanine 7, N-glucoside rhodanine 8 and S-glucosylation 5-arylidene …
glucosylation rhodanine 7, N-glucoside rhodanine 8 and S-glucosylation 5-arylidene …