Therapeutic outcomes of isatin and its derivatives against multiple diseases: Recent developments in drug discovery
Isatin (1 H indole 2, 3-dione) is a heterocyclic, endogenous lead molecule recognized in
humans and different plants. The isatin nucleus and its derivatives are owed the attention of …
humans and different plants. The isatin nucleus and its derivatives are owed the attention of …
Isatin–azole hybrids and their anticancer activities
Y Hou, C Shang, H Wang, J Yun - Archiv der Pharmazie, 2020 - Wiley Online Library
Isatin and azole moieties, which have the ability to form various noncovalent interactions
with different therapeutic targets, are common pharmacophores in drug development. Isatin …
with different therapeutic targets, are common pharmacophores in drug development. Isatin …
Synthesis, antitumor, and apoptosis-inducing activities of novel 5-arylidenethiazolidine-2, 4-dione derivatives: histone deacetylases inhibitory activity and molecular …
The antitumor activity of the newly synthesized 5-arylidenethiazolidine-2, 4-dione derivatives
18a–f and 19a–f was investigated, compared to doxorubicin (IC 50= 4.17–8.87 μM) and …
18a–f and 19a–f was investigated, compared to doxorubicin (IC 50= 4.17–8.87 μM) and …
Synthesis, cytotoxic evaluation, and molecular docking studies of novel quinazoline derivatives with benzenesulfonamide and anilide tails: Dual inhibitors of EGFR …
We synthesized a new series of 2-[(3-(4-sulfamoylphenethyl)-4 (3H)-quinazolinon-2-yl) thio]
anilide derivatives (2–16) and evaluated their cytotoxic activity against breast …
anilide derivatives (2–16) and evaluated their cytotoxic activity against breast …
Pharmacophore hybridization approach to discover novel pyrazoline-based hydantoin analogs with anti-tumor efficacy
N Upadhyay, K Tilekar, F Loiodice, NY Anisimova… - Bioorganic …, 2021 - Elsevier
In search for new and safer anti-cancer agents, a structurally guided pharmacophore
hybridization strategy of two privileged scaffolds, namely diaryl pyrazolines and …
hybridization strategy of two privileged scaffolds, namely diaryl pyrazolines and …
Design, synthesis, and antitumor activity of novel compounds based on 1, 2, 4-triazolophthalazine scaffold: apoptosis-inductive and PCAF-inhibitory effects
The antitumor activity of newly synthesised triazolophthalazines (L-45 analogues) 10–32
was evaluated in human hepatocellular carcinoma (HePG-2), breast cancer (MCF-7) …
was evaluated in human hepatocellular carcinoma (HePG-2), breast cancer (MCF-7) …
Design, synthesis, antitumor, and VEGFR-2 inhibition activities of novel 4-anilino-2-vinyl-quinazolines: Molecular modeling studies
The antitumor activity of newly synthesized 4-anilino-2-vinylquinazolines 8a-r was measured
comparable to sorafenib as a standard drug. The 2-vinylquinazolines 8a-r were evaluated …
comparable to sorafenib as a standard drug. The 2-vinylquinazolines 8a-r were evaluated …
[HTML][HTML] Design, synthesis, antitumor evaluation, and molecular docking of novel pyrrolo [2, 3-d] pyrimidine as multi-kinase inhibitors
In the last twenty years, protein kinases have been identified as important targets for cancer
therapy. In order to prevent unexpected toxicity, medicinal chemists have always focused on …
therapy. In order to prevent unexpected toxicity, medicinal chemists have always focused on …
Pharmacophore-based virtual screening, synthesis, biological evaluation, and molecular docking study of novel pyrrolizines bearing urea/thiourea moieties with …
In the current study, virtual screening of a small library of 1302 pyrrolizines bearing
urea/thiourea moieties was performed. The top-scoring hits were synthesised and evaluated …
urea/thiourea moieties was performed. The top-scoring hits were synthesised and evaluated …
Discovery of pyridine-sulfonamide hybrids as a new scaffold for the development of potential VEGFR-2 inhibitors and apoptosis inducers
MF Ahmed, EY Santali - Bioorganic Chemistry, 2021 - Elsevier
New sulfonamide derivatives have been synthesized and tested as antitumor agents. All
newly synthesized compounds were tested in vitro against 60 lines of human cancer cells …
newly synthesized compounds were tested in vitro against 60 lines of human cancer cells …